IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F13/2023.1

Cannabinoid receptors in GtoPdb v.2023.1



Mary Abood1, Stephen P.H. Alexander2, Francis Barth3, Tom I. Bonner4, Heather Bradshaw5, Guy Cabral6, Pierre Casellas7, Ben F. Cravatt8, William A. Devane6, Vincenzo Di Marzo9, Maurice R. Elphick10, Christian C. Felder11, Peter Greasley12, Miles Herkenham4, Allyn C. Howlett13, George Kunos14, Ken Mackie15, Raphael Mechoulam16, Roger G. Pertwee17 and Ruth A. Ross18
  1. Temple University, USA
  2. University of Nottingham, UK
  3. Sanofi Synthelabo Recherche, France
  4. National Institute of Mental Health, USA
  5. Indiana University, USA
  6. Medical College of Virginia, USA
  7. Université de Montpellier, France
  8. Scripps Research Institute, USA
  9. CNR Institute of Biomolecular Chemistry, Italy
  10. Queen Mary University of London, UK
  11. Lilly Research Laboratories, USA
  12. AstraZeneca R&D Mölndal, Sweden
  13. North Carolina Central University, USA
  14. National Institutes of Health, USA
  15. University of Washington, USA
  16. Hebrew University, Israel
  17. University of Aberdeen, UK
  18. University of Toronto, Canada


Abstract

Cannabinoid receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Cannabinoid Receptors [119]) are activated by endogenous ligands that include N-arachidonoylethanolamine (anandamide), N-homo-γ-linolenoylethanolamine, N-docosatetra-7,10,13,16-enoylethanolamine and 2-arachidonoylglycerol. Potency determinations of endogenous agonists at these receptors are complicated by the possibility of differential susceptibility of endogenous ligands to enzymatic conversion [5].

There are currently three licenced cannabinoid medicines each of which contains a compound that can activate CB1 and CB2 receptors [111]. Two of these medicines were developed to suppress nausea and vomiting produced by chemotherapy. These are nabilone (Cesamet®), a synthetic CB1/CB2 receptor agonist, and synthetic Δ9-tetrahydrocannabinol (Marinol®; dronabinol), which can also be used as an appetite stimulant. The third medicine, Sativex®, contains mainly Δ9-tetrahydrocannabinol and cannabidiol, both extracted from cannabis, and is used to treat multiple sclerosis and cancer pain.

Contents

This is a citation summary for Cannabinoid receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts. For further details see [22].

Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

Cannabinoid receptors
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=13
Introduction to Cannabinoid receptors
https://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=13
    Receptors
            CB1 receptor
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=56
            CB2 receptor
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=57

References

  1. Abadji V, Lin S, Taha G, Griffin G, Stevenson LA, Pertwee RG and Makriyannis A. (1994) (R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability. J Med Chem 37: 1889-93 [PMID:8021930]
  2. Abood ME and Martin BR. (1992) Neurobiology of marijuana abuse. Trends Pharmacol Sci 13: 201-6 [PMID:1604713]
  3. Adam J-M, Bissantz C, Grether U, Kimbara A, Nettekoven M, Roever S and Rogers-Evans M. (2013) [1, 2, 3] triazolo [4, 5 -d] pyrimidine derivatives as agonists of the cannabinoid receptor 2 Patent number: WO2013068306A1. Assignee: Hoffmann-La Roche Ag. Priority date: 08/11/2011. Publication date: 16/05/2013.
  4. Adam L, Salois D, Rihakova L, Lapointe S, St-Onge S, Labrecque J and Payza K. (2007) Positive allosteric modulators of CB1 receptors. In 17th Annual Symposium of the Cannabinoids, St-Sauveur, Canada International Cannabinoid Research Society: 86
  5. Alexander SP and Kendall DA. (2007) The complications of promiscuity: endocannabinoid action and metabolism. Br J Pharmacol 152: 602-23 [PMID:17876303]
  6. Appendino G, De Petrocellis L, Trevisani M, Minassi A, Daddario N, Moriello AS, Gazzieri D, Ligresti A, Campi B and Fontana G et al.. (2005) Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic potential. J Pharmacol Exp Ther 312: 561-70 [PMID:15356216]
  7. Baek JH, Zheng Y, Darlington CL and Smith PF. (2008) Cannabinoid CB2 receptor expression in the rat brainstem cochlear and vestibular nuclei. Acta Otolaryngol 128: 961-7 [PMID:19086305]
  8. Banister SD, Stuart J, Kevin RC, Edington A, Longworth M, Wilkinson SM, Beinat C, Buchanan AS, Hibbs DE and Glass M et al.. (2015) Effects of bioisosteric fluorine in synthetic cannabinoid designer drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135. ACS Chem Neurosci 6: 1445-58 [PMID:25921407]
  9. Bauer M, Chicca A, Tamborrini M, Eisen D, Lerner R, Lutz B, Poetz O, Pluschke G and Gertsch J. (2012) Identification and quantification of a new family of peptide endocannabinoids (Pepcans) showing negative allosteric modulation at CB1 receptors. J Biol Chem 287: 36944-67 [PMID:22952224]
  10. Bayewitch M, Avidor-Reiss T, Levy R, Barg J, Mechoulam R and Vogel Z. (1995) The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling. FEBS Lett 375: 143-7 [PMID:7498464]
  11. Bayewitch M, Rhee MH, Avidor-Reiss T, Breuer A, Mechoulam R and Vogel Z. (1996) (-)-Delta9-tetrahydrocannabinol antagonizes the peripheral cannabinoid receptor-mediated inhibition of adenylyl cyclase. J Biol Chem 271: 9902-5 [PMID:8626625]
  12. Beltramo M, Bernardini N, Bertorelli R, Campanella M, Nicolussi E, Fredduzzi S and Reggiani A. (2006) CB2 receptor-mediated antihyperalgesia: possible direct involvement of neural mechanisms. Eur J Neurosci 23: 1530-8 [PMID:16553616]
  13. Ben-Shabat S, Fride E, Sheskin T, Tamiri T, Rhee MH, Vogel Z, Bisogno T, De Petrocellis L, Di Marzo V and Mechoulam R. (1998) An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity. Eur J Pharmacol 353: 23-31 [PMID:9721036]
  14. Blaazer AR, Lange JH, van der Neut MA, Mulder A, den Boon FS, Werkman TR, Kruse CG and Wadman WJ. (2011) Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity. Eur J Med Chem 46: 5086-98 [PMID:21885167]
  15. Bouaboula M, Bourrié B, Rinaldi-Carmona M, Shire D, Le Fur G and Casellas P. (1995) Stimulation of cannabinoid receptor CB1 induces krox-24 expression in human astrocytoma cells. J Biol Chem 270: 13973-80 [PMID:7775459]
  16. Bouaboula M, Poinot-Chazel C, Bourrié B, Canat X, Calandra B, Rinaldi-Carmona M, Le Fur G and Casellas P. (1995) Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1. Biochem J 312 ( Pt 2): 637-41 [PMID:8526880]
  17. Bouaboula M, Poinot-Chazel C, Marchand J, Canat X, Bourrié B, Rinaldi-Carmona M, Calandra B, Le Fur G and Casellas P. (1996) Signaling pathway associated with stimulation of CB2 peripheral cannabinoid receptor. Involvement of both mitogen-activated protein kinase and induction of Krox-24 expression. Eur J Biochem 237: 704-11 [PMID:8647116]
  18. Bowles NP, Karatsoreos IN, Li X, Vemuri VK, Wood JA, Li Z, Tamashiro KL, Schwartz GJ, Makriyannis AM and Kunos G et al.. (2015) A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome. Proc Natl Acad Sci USA 112: 285-90 [PMID:25535367]
  19. Breivogel CS, Sim LJ and Childers SR. (1997) Regional differences in cannabinoid receptor/G-protein coupling in rat brain. J Pharmacol Exp Ther 282: 1632-42 [PMID:9316881]
  20. Brown SM, Wager-Miller J and Mackie K. (2002) Cloning and molecular characterization of the rat CB2 cannabinoid receptor. Biochim Biophys Acta 1576: 255-264 [PMID:12084572]
  21. Buckley NE, McCoy KL, Mezey E, Bonner T, Zimmer A, Felder CC, Glass M and Zimmer A. (2000) Immunomodulation by cannabinoids is absent in mice deficient for the cannabinoid CB(2) receptor. Eur J Pharmacol 396: 141-9 [PMID:10822068]
  22. Buneman P, Christie G, Davies JA, Dimitrellou R, Harding SD, Pawson AJ, Sharman JL and Wu Y. (2020) Why data citation isn't working, and what to do about it Database 2020 [PMID:32367113]
  23. Cabral GA and Staab A. (2005) Effects on the immune system. Handb Exp Pharmacol: 385-423 [PMID:16596782]
  24. Calandra B, Portier M, Kernéis A, Delpech M, Carillon C, Le Fur G, Ferrara P and Shire D. (1999) Dual intracellular signaling pathways mediated by the human cannabinoid CB1 receptor. Eur J Pharmacol 374: 445-55 [PMID:10422789]
  25. Carlisle SJ, Marciano-Cabral F, Staab A, Ludwick C and Cabral GA. (2002) Differential expression of the CB2 cannabinoid receptor by rodent macrophages and macrophage-like cells in relation to cell activation. Int Immunopharmacol 2: 69-82 [PMID:11789671]
  26. Chakrabarti A, Onaivi ES and Chaudhuri G. (1995) Cloning and sequencing of a cDNA encoding the mouse brain-type cannabinoid receptor protein. DNA Seq 5: 385-8 [PMID:8777318]
  27. Childers SR and Deadwyler SA. (1996) Role of cyclic AMP in the actions of cannabinoid receptors. Biochem Pharmacol 52: 819-27 [PMID:8781498]
  28. Chin CN, Lucas-Lenard J, Abadji V and Kendall DA. (1998) Ligand binding and modulation of cyclic AMP levels depend on the chemical nature of residue 192 of the human cannabinoid receptor 1. J Neurochem 70: 366-73 [PMID:9422383]
  29. Chin CN, Murphy JW, Huffman JW and Kendall DA. (1999) The third transmembrane helix of the cannabinoid receptor plays a role in the selectivity of aminoalkylindoles for CB2, peripheral cannabinoid receptor. J Pharmacol Exp Ther 291: 837-44 [PMID:10525107]
  30. Cinar R, Iyer MR, Liu Z, Cao Z, Jourdan T, Erdelyi K, Godlewski G, Szanda G, Liu J and Park JK et al.. (2016) Hybrid inhibitor of peripheral cannabinoid-1 receptors and inducible nitric oxide synthase mitigates liver fibrosis. JCI Insight 1 [PMID:27525312]
  31. Das SK, Paria BC, Chakraborty I and Dey SK. (1995) Cannabinoid ligand-receptor signaling in the mouse uterus. Proc Natl Acad Sci USA 92: 4332-6 [PMID:7753807]
  32. De Vry J, Denzer D, Reissmueller E, Eijckenboom M, Heil M, Meier H and Mauler F. (2004) 3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects. J Pharmacol Exp Ther 310: 620-32 [PMID:15140913]
  33. Del Rio C, Cantarero I, Palomares B, Gómez-Cañas M, Fernández-Ruiz J, Pavicic C, García-Martín A, Luz Bellido M, Ortega-Castro R and Pérez-Sánchez C et al.. (2018) VCE-004.3, a cannabidiol aminoquinone derivative, prevents bleomycin-induced skin fibrosis and inflammation through PPARγ- and CB2 receptor-dependent pathways. Br J Pharmacol 175: 3813-3831 [PMID:30033591]
  34. Devane WA, Breuer A, Sheskin T, Järbe TU, Eisen MS and Mechoulam R. (1992) A novel probe for the cannabinoid receptor. J Med Chem 35: 2065-9 [PMID:1317925]
  35. Devane WA, Hanus L, Breuer A, Pertwee RG, Stevenson LA, Griffin G, Gibson D, Mandelbaum A, Etinger A and Mechoulam R. (1992) Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 258: 1946-1949 [PMID:1470919]
  36. Di Marzo V, Bisogno T, De Petrocellis L, Brandi I, Jefferson RG, Winckler RL, Davis JB, Dasse O, Mahadevan A, Razdan RK and Martin BR. (2001) Highly selective CB1 cannabinoid receptor ligands and novel CB1/VR1 vanilloid receptor "hybrid" ligands. Biochem Biophys Res Commun 281: 444-451 [PMID:11181068]
  37. Di Marzo V, De Petrocellis L and Bisogno T. (2005) The biosynthesis, fate and pharmacological properties of endocannabinoids. Handb Exp Pharmacol: 147-85 [PMID:16596774]
  38. Dow RL, Carpino PA, Hadcock JR, Black SC, Iredale PA, DaSilva-Jardine P, Schneider SR, Paight ES, Griffith DA and Scott DO et al.. (2009) Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. J Med Chem 52: 2652-5 [PMID:19351113]
  39. Edery H, Grunfeld Y, Ben-Zvi Z and Mechoulam R. (1971) Structural requirements for cannabinoid activity. Ann NY Acad Sci 191: 40-53
  40. Facci L, Dal Toso R, Romanello S, Buriani A, Skaper SD and Leon A. (1995) Mast cells express a peripheral cannabinoid receptor with differential sensitivity to anandamide and palmitoylethanolamide. Proc Natl Acad Sci USA 92: 3376-80 [PMID:7724569]
  41. Felder CC, Joyce KE, Briley EM, Glass M, Mackie KP, Fahey KJ, Cullinan GJ, Hunden DC, Johnson DW and Chaney MO et al.. (1998) LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J Pharmacol Exp Ther 284: 291-7 [PMID:9435190]
  42. Felder CC, Joyce KE, Briley EM, Mansouri J, Mackie K, Blond O, Lai Y, Ma AL and Mitchell RL. (1995) Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors. Mol Pharmacol 48: 443-50 [PMID:7565624]
  43. Felder CC, Veluz JS, Williams HL, Briley EM and Matsuda LA. (1992) Cannabinoid agonists stimulate both receptor- and non-receptor-mediated signal transduction pathways in cells transfected with and expressing cannabinoid receptor clones. Mol Pharmacol 42: 838-45 [PMID:1331766]
  44. Foloppe N, Benwell K, Brooks TD, Kennett G, Knight AR, Misra A and Monck NJ. (2009) Discovery and functional evaluation of diverse novel human CB(1) receptor ligands. Bioorg Med Chem Lett 19: 4183-90 [PMID:19520572]
  45. Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, Lao J, Yu H, Feng Y and Xiao JC et al.. (2007) Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents. J Pharmacol Exp Ther 321: 1013-22 [PMID:17327489]
  46. Gado F, Di Cesare Mannelli L, Lucarini E, Bertini S, Cappelli E, Digiacomo M, Stevenson LA, Macchia M, Tuccinardi T and Ghelardini C et al.. (2019) Identification of the First Synthetic Allosteric Modulator of the CB2 Receptors and Evidence of Its Efficacy for Neuropathic Pain Relief. J Med Chem 62: 276-287 [PMID:29990428]
  47. Galiègue S, Mary S, Marchand J, Dussossoy D, Carrière D, Carayon P, Bouaboula M, Shire D, Le Fur G and Casellas P. (1995) Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations. Eur J Biochem 232: 54-61 [PMID:7556170]
  48. Gaoni Y and Mechoulam R. (1964) Isolation, structure and partial synthesis of an active constituent of hashish. J Am Chem Soc 86: 1646-1647
  49. Gareau Y, Dufresne C, Gallant M, Rochette C, Sawyer N, Slipetz DM, Tremblay N, Weech PK, Metters KM and Labelle M. (1996) Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors. Bioorg Med Chem Lett 6: 189-194
  50. Gatley SJ, Lan R, Pyatt B, Gifford AN, Volkow ND and Makriyannis A. (1997) Binding of the non-classical cannabinoid CP 55,940, and the diarylpyrazole AM251 to rodent brain cannabinoid receptors. Life Sci 61: PL 191-7 [PMID:9335234]
  51. Gebremedhin D, Lange AR, Campbell WB, Hillard CJ and Harder DR. (1999) Cannabinoid CB1 receptor of cat cerebral arterial muscle functions to inhibit L-type Ca2+ channel current. Am J Physiol 276: H2085-93 [PMID:10362691]
  52. Glass M and Felder CC. (1997) Concurrent stimulation of cannabinoid CB1 and dopamine D2 receptors augments cAMP accumulation in striatal neurons: evidence for a Gs linkage to the CB1 receptor. J Neurosci 17: 5327-33 [PMID:9204917]
  53. Gong JP, Onaivi ES, Ishiguro H, Liu QR, Tagliaferro PA, Brusco A and Uhl GR. (2006) Cannabinoid CB2 receptors: immunohistochemical localization in rat brain. Brain Res 1071: 10-23 [PMID:16472786]
  54. Griffin G, Tao Q and Abood ME. (2000) Cloning and pharmacological characterization of the rat CB(2) cannabinoid receptor. J Pharmacol Exp Ther 292: 886-94 [PMID:10688601]
  55. Griffith DA, Hadcock JR, Black SC, Iredale PA, Carpino PA, DaSilva-Jardine P, Day R, DiBrino J, Dow RL and Landis MS et al.. (2009) Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. J Med Chem 52: 234-7 [PMID:19102698]
  56. Gérard C, Mollereau C, Vassart G and Parmentier M. (1990) Nucleotide sequence of a human cannabinoid receptor cDNA. Nucleic Acids Res 18: 7142 [PMID:2263478]
  57. Gérard CM, Mollereau C, Vassart G and Parmentier M. (1991) Molecular cloning of a human cannabinoid receptor which is also expressed in testis. Biochem J 279 ( Pt 1): 129-34 [PMID:1718258]
  58. Han S, Thatte J, Buzard DJ and Jones RM. (2013) Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists. J Med Chem 56: 8224-56 [PMID:23865723]
  59. Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH and Barden J et al.. (2017) Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain. ACS Med Chem Lett 8: 1309-1313 [PMID:29259753]
  60. Hanus L, Breuer A, Tchilibon S, Shiloah S, Goldenberg D, Horowitz M, Pertwee RG, Ross RA, Mechoulam R and Fride E. (1999) HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor. Proc Natl Acad Sci USA 96: 14228-33 [PMID:10588688]
  61. Henry DJ and Chavkin C. (1995) Activation of inwardly rectifying potassium channels (GIRK1) by co-expressed rat brain cannabinoid receptors in Xenopus oocytes. Neurosci Lett 186: 91-4 [PMID:7777206]
  62. Herkenham M, Lynn AB, Little MD, Johnson MR, Melvin LS, de Costa BR and Rice KC. (1990) Cannabinoid receptor localization in brain. Proc Natl Acad Sci USA 87: 1932-6 [PMID:2308954]
  63. Hillard CJ, Manna S, Greenberg MJ, DiCamelli R, Ross RA, Stevenson LA, Murphy V, Pertwee RG and Campbell WB. (1999) Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1). J Pharmacol Exp Ther 289: 1427-33 [PMID:10336536]
  64. Hirst RA, Almond SL and Lambert DG. (1996) Characterisation of the rat cerebella CB1 receptor using SR141716A, a central cannabinoid receptor antagonist. Neurosci Lett 220: 101-4 [PMID:8981483]
  65. Hoehe MR, Caenazzo L, Martinez MM, Hsieh WT, Modi WS, Gershon ES and Bonner TI. (1991) Genetic and physical mapping of the human cannabinoid receptor gene to chromosome 6q14-q15. New Biol 3: 880-5 [PMID:1931832]
  66. Hollister LE. (1986) Health aspects of cannabis. Pharmacol Rev 38: 1-20 [PMID:3520605]
  67. Horswill JG, Bali U, Shaaban S, Keily JF, Jeevaratnam P, Babbs AJ, Reynet C and Wong Kai In P. (2007) PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats. Br J Pharmacol 152: 805-14 [PMID:17592509]
  68. Howlett AC, Barth F, Bonner TI, Cabral G, Casellas P, Devane WA, Felder CC, Herkenham M, Mackie K and Martin BR et al.. (2002) International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol Rev 54: 161-202 [PMID:12037135]
  69. Howlett AC, Berglund BA and Melvin LS. (1995) Cannabinoid receptor agonists and antagonists. Curr Pharm Des 1: 343-354
  70. Howlett AC, Qualy JM and Khachatrian LL. (1986) Involvement of Gi in the inhibition of adenylate cyclase by cannabimimetic drugs. Mol Pharmacol 29: 307-13 [PMID:2869405]
  71. Hu Y, Ranganathan M, Shu C, Liang X, Ganesh S, Osafo-Addo A, Yan C, Zhang X, Aouizerat BE and Krystal JH et al.. (2020) Single-cell Transcriptome Mapping Identifies Common and Cell-type Specific Genes Affected by Acute Delta9-tetrahydrocannabinol in Humans. Sci Rep 10: 3450 [PMID:32103029]
  72. Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S and Ho JH et al.. (2017) Crystal structures of agonist-bound human cannabinoid receptor CB1. Nature 547: 468-471 [PMID:28678776]
  73. Hua T, Vemuri K, Pu M, Qu L, Han GW, Wu Y, Zhao S, Shui W, Li S and Korde A et al.. (2016) Crystal Structure of the Human Cannabinoid Receptor CB1. Cell 167: 750-762.e14 [PMID:27768894]
  74. Huffman JW, Liddle J, Yu S, Aung MM, Abood ME, Wiley JL and Martin BR. (1999) 3-(1',1'-Dimethylbutyl)-1-deoxy-delta8-THC and related compounds: synthesis of selective ligands for the CB2 receptor. Bioorg Med Chem 7: 2905-14 [PMID:10658595]
  75. Hung MS, Chang CP, Li TC, Yeh TK, Song JS, Lin Y, Wu CH, Kuo PC, Amancha PK and Wong YC et al.. (2010) Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist. ChemMedChem 5: 1439-43 [PMID:20652930]
  76. Ignatowska-Jankowska BM, Baillie GL, Kinsey S, Crowe M, Ghosh S, Owens RA, Damaj IM, Poklis J, Wiley JL and Zanda M et al.. (2015) A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No Psychoactive Effects. Neuropsychopharmacology 40: 2948-59 [PMID:26052038]
  77. Jackson AR, Hegde VL, Nagarkatti PS and Nagarkatti M. (2014) Characterization of endocannabinoid-mediated induction of myeloid-derived suppressor cells involving mast cells and MCP-1. J Leukoc Biol 95: 609-19 [PMID:24319288]
  78. Jansen EM, Haycock DA, Ward SJ and Seybold VS. (1992) Distribution of cannabinoid receptors in rat brain determined with aminoalkylindoles. Brain Res 575: 93-102 [PMID:1504787]
  79. Jarrahian A, Watts VJ and Barker EL. (2004) D2 dopamine receptors modulate Galpha-subunit coupling of the CB1 cannabinoid receptor. J Pharmacol Exp Ther 308: 880-6 [PMID:14634050]
  80. Jung M, Calassi R, Rinaldi Carmona M, Chardenot P, Le Fur G, Soubrie P and Oury-Donat F. (1997) Characterization of CB1 receptors on rat neuronal cell cultures: binding and functional studies using the selective receptor antagonist SR 141716A. J Neurochem 68: 402-409 [PMID:8978752]
  81. Khanolkar AD, Abadji V, Lin S, Hill WA, Taha G, Abouzid K, Meng Z, Fan P and Makriyannis A. (1996) Head group analogs of arachidonylethanolamide, the endogenous cannabinoid ligand. J Med Chem 39: 4515-9 [PMID:8893848]
  82. Khanolkar AD, Lu D, Ibrahim M, Duclos Jr RI, Thakur GA, Malan Jr TP, Porreca F, Veerappan V, Tian X and George C et al.. (2007) Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity. J Med Chem 50: 6493-500 [PMID:18038967]
  83. Kulkarni PM, Kulkarni AR, Korde A, Tichkule RB, Laprairie RB, Denovan-Wright EM, Zhou H, Janero DR, Zvonok N and Makriyannis A et al.. (2016) Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). J Med Chem 59: 44-60 [PMID:26529344]
  84. Kulkarni S, Nikas SP, Sharma R, Jiang S, Paronis CA, Leonard MZ, Zhang B, Honrao C, Mallipeddi S and Raghav JG et al.. (2016) Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues. J Med Chem 59: 6903-19 [PMID:27367336]
  85. Lan R, Gatley J, Lu Q, Fan P, Fernando SR, Volkow ND, Pertwee R and Makriyannis A. (1999) Design and synthesis of the CB1 selective cannabinoid antagonist AM281: a potential human SPECT ligand. AAPS PharmSci 1: E4 [PMID:11741201]
  86. Lan R, Liu Q, Fan P, Lin S, Fernando SR, McCallion D, Pertwee R and Makriyannis A. (1999) Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J Med Chem 42: 769-76 [PMID:10052983]
  87. Lange JH, Coolen HK, van Stuivenberg HH, Dijksman JA, Herremans AH, Ronken E, Keizer HG, Tipker K, McCreary AC and Veerman W et al.. (2004) Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J Med Chem 47: 627-43 [PMID:14736243]
  88. Laprairie RB, Bagher AM, Kelly ME and Denovan-Wright EM. (2015) Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor. Br J Pharmacol 172: 4790-805 [PMID:26218440]
  89. Laprairie RB, Kulkarni AR, Kulkarni PM, Hurst DP, Lynch D, Reggio PH, Janero DR, Pertwee RG, Stevenson LA and Kelly ME et al.. (2016) Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe. ACS Chem Neurosci 7: 776-98 [PMID:27046127]
  90. Laprairie RB, Kulkarni PM, Deschamps JR, Kelly MEM, Janero DR, Cascio MG, Stevenson LA, Pertwee RG, Kenakin TP and Denovan-Wright EM et al.. (2017) Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor. ACS Chem Neurosci 8: 1188-1203 [PMID:28103441]
  91. Lavey BJ, Kozlowski JA, Hipkin RW, Gonsiorek W, Lundell DJ, Piwinski JJ, Narula S and Lunn CA. (2005) Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies. Bioorg Med Chem Lett 15: 783-6 [PMID:15664857]
  92. Ledent C, Valverde O, Cossu G, Petitet F, Aubert JF, Beslot F, Böhme GA, Imperato A, Pedrazzini T and Roques BP et al.. (1999) Unresponsiveness to cannabinoids and reduced addictive effects of opiates in CB1 receptor knockout mice. Science 283: 401-4 [PMID:9888857]
  93. Li X, Hua T, Vemuri K, Ho JH, Wu Y, Wu L, Popov P, Benchama O, Zvonok N and Locke K et al.. (2019) Crystal Structure of the Human Cannabinoid Receptor CB2. Cell 176: 459-467.e13 [PMID:30639103]
  94. Lunn CA, Fine JS, Rojas-Triana A, Jackson JV, Fan X, Kung TT, Gonsiorek W, Schwarz MA, Lavey B and Kozlowski JA et al.. (2006) A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo. J Pharmacol Exp Ther 316: 780-8 [PMID:16258021]
  95. Mackie K and Hille B. (1992) Cannabinoids inhibit N-type calcium channels in neuroblastoma-glioma cells. Proc Natl Acad Sci USA 89: 3825-9 [PMID:1315042]
  96. Mackie K, Lai Y, Westenbroek R and Mitchell R. (1995) Cannabinoids activate an inwardly rectifying potassium conductance and inhibit Q-type calcium currents in AtT20 cells transfected with rat brain cannabinoid receptor. J Neurosci 15: 6552-6561 [PMID:7472417]
  97. Mailleux P, Parmentier M and Vanderhaeghen JJ. (1992) Distribution of cannabinoid receptor messenger RNA in the human brain: an in situ hybridization histochemistry with oligonucleotides. Neurosci Lett 143: 200-4 [PMID:1436667]
  98. Makriyannis A and Deng H. (2001) Cannabimimetic indole derivatives Patent number: WO2001028557. Assignee: University Of Connecticut. Priority date: 18/10/1999. Publication date: 26/04/2001.
  99. Maneuf YP and Brotchie JM. (1997) Paradoxical action of the cannabinoid WIN 55,212-2 in stimulated and basal cyclic AMP accumulation in rat globus pallidus slices. Br J Pharmacol 120: 1397-8 [PMID:9113356]
  100. Marini P, Cascio MG, King A, Pertwee RG and Ross RA. (2013) Characterization of cannabinoid receptor ligands in tissues natively expressing cannabinoid CB2 receptors. Br J Pharmacol 169: 887-99 [PMID:23711022]
  101. Martin BR, Balster RL, Razdan RK, Harris LS and Dewey WL. (1981) Behavioral comparisons of the stereoisomers of tetrahydrocannabinols. Life Sci 29: 565-74 [PMID:6268916]
  102. Martin BR, Compton DR, Thomas BF, Prescott WR, Little PJ, Razdan RK, Johnson MR, Melvin LS, Mechoulam R and Ward SJ. (1991) Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs. Pharmacol Biochem Behav 40: 471-8 [PMID:1666911]
  103. Matsuda LA, Lolait SJ, Brownstein MJ, Young AC and Bonner TI. (1990) Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 346: 561-4 [PMID:2165569]
  104. Mechoulam R, Ben-Shabat S, Hanus L, Ligumsky M, Kaminski NE, Schatz AR, Gopher A, Almog S, Martin BR and Compton DR et al.. (1995) Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors. Biochem Pharmacol 50: 83-90 [PMID:7605349]
  105. Munro S, Thomas KL and Abu-Shaar M. (1993) Molecular characterization of a peripheral receptor for cannabinoids. Nature 365: 61-5 [PMID:7689702]
  106. Navarro HA, Howard JL, Pollard GT and Carroll FI. (2009) Positive allosteric modulation of the human cannabinoid (CB) receptor by RTI-371, a selective inhibitor of the dopamine transporter. Br J Pharmacol 156: 1178-84 [PMID:19226282]
  107. O'Sullivan SE. (2007) Cannabinoids go nuclear: evidence for activation of peroxisome proliferator-activated receptors. Br J Pharmacol 152: 576-82 [PMID:17704824]
  108. Oka S, Wakui J, Ikeda S, Yanagimoto S, Kishimoto S, Gokoh M, Nasui M and Sugiura T. (2006) Involvement of the cannabinoid CB2 receptor and its endogenous ligand 2-arachidonoylglycerol in oxazolone-induced contact dermatitis in mice. J Immunol 177: 8796-805 [PMID:17142782]
  109. Pacheco M, Childers SR, Arnold R, Casiano F and Ward SJ. (1991) Aminoalkylindoles: actions on specific G-protein-linked receptors. J Pharmacol Exp Ther 257: 170-83 [PMID:1902257]
  110. Pertwee RG. (2000) Cannabinoid receptor ligands: clinical and neuropharmacological considerations, relevant to future drug discovery and development. Expert Opin Investig Drugs 9: 1553-71 [PMID:11060760]
  111. Pertwee RG. (2012) Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities. Philos Trans R Soc Lond, B, Biol Sci 367: 3353-63 [PMID:23108552]
  112. Pertwee RG. (1997) Pharmacology of cannabinoid CB1 and CB2 receptors. Pharmacol Ther 74: 129-80 [PMID:9336020]
  113. Pertwee RG. (1999) Pharmacology of cannabinoid receptor ligands. Curr Med Chem 6: 635-64 [PMID:10469884]
  114. Pertwee RG. (2010) Receptors and channels targeted by synthetic cannabinoid receptor agonists and antagonists. Curr Med Chem 17: 1360-81 [PMID:20166927]
  115. Pertwee RG. (2005) Pharmacological actions of cannabinoids. Handb Exp Pharmacol: 1-51 [PMID:16596770]
  116. Pertwee RG. (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci 76: 1307-24 [PMID:15670612]
  117. Pertwee RG. (2008) The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9-tetrahydrocannabinol, cannabidiol and delta9-tetrahydrocannabivarin. Br J Pharmacol 153: 199-215 [PMID:17828291]
  118. Pertwee RG. (2008) Ligands that target cannabinoid receptors in the brain: from THC to anandamide and beyond. Addict Biol 13: 147-59 [PMID:18482430]
  119. Pertwee RG, Howlett AC, Abood ME, Alexander SP, Di Marzo V, Elphick MR, Greasley PJ, Hansen HS, Kunos G and Mackie K et al.. (2010) International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB₁ and CB₂. Pharmacol Rev 62: 588-631 [PMID:21079038]
  120. Pertwee RG and Ross RA. (2002) Cannabinoid receptors and their ligands. Prostaglandins Leukot Essent Fatty Acids 66: 101-21 [PMID:12052030]
  121. Pertwee RG, Stevenson LA, Elrick DB, Mechoulam R and Corbett AD. (1992) Inhibitory effects of certain enantiomeric cannabinoids in the mouse vas deferens and the myenteric plexus preparation of guinea-pig small intestine. Br J Pharmacol 105: 980-984 [PMID:1324060]
  122. Petitet F, Marin L and Doble A. (1996) Biochemical and pharmacological characterization of cannabinoid binding sites using [3H]SR141716A. Neuroreport 7: 789-792 [PMID:8733746]
  123. Petrucci V, Chicca A, Glasmacher S, Paloczi J, Cao Z, Pacher P and Gertsch J. (2017) Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage. Sci Rep 7: 9560 [PMID:28842619]
  124. Pettit DA, Harrison MP, Olson JM, Spencer RF and Cabral GA. (1998) Immunohistochemical localization of the neural cannabinoid receptor in rat brain. J Neurosci Res 51: 391-402 [PMID:9486774]
  125. Pini A, Mannaioni G, Pellegrini-Giampietro D, Passani MB, Mastroianni R, Bani D and Masini E. (2012) The role of cannabinoids in inflammatory modulation of allergic respiratory disorders, inflammatory pain and ischemic stroke. Curr Drug Targets 13: 984-93 [PMID:22420307]
  126. Piscitelli F, Ligresti A, La Regina G, Coluccia A, Morera L, Allarà M, Novellino E, Di Marzo V and Silvestri R. (2012) Indole-2-carboxamides as allosteric modulators of the cannabinoid CB₁ receptor. J Med Chem 55: 5627-31 [PMID:22571451]
  127. Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G and Walker G et al.. (2005) Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol 68: 1484-95 [PMID:16113085]
  128. Razdan RK. (1986) Structure-activity relationships in cannabinoids. Pharmacol Rev 38: 75-149 [PMID:3018800]
  129. Rhee MH, Bayewitch M, Avidor-Reiss T, Levy R and Vogel Z. (1998) Cannabinoid receptor activation differentially regulates the various adenylyl cyclase isozymes. J Neurochem 71: 1525-34 [PMID:9751186]
  130. Rhee MH, Vogel Z, Barg J, Bayewitch M, Levy R, Hanus L, Breuer A and Mechoulam R. (1997) Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase. J Med Chem 40: 3228-33 [PMID:9379442]
  131. Rhee MH, Vogel Z, Barg J, Bayewitch M, Levy R, Hanus L, Breuer A and Mechoulam R. (1997) Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase. J Med Chem 40: 3228-33 [PMID:9379442]
  132. Rinaldi-Carmona M, Barth F, Congy C, Martinez S, Oustric D, Pério A, Poncelet M, Maruani J, Arnone M and Finance O et al.. (2004) SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization. J Pharmacol Exp Ther 310: 905-14 [PMID:15131245]
  133. Rinaldi-Carmona M, Barth F, Héaulme M, Shire D, Calandra B, Congy C, Martinez S, Maruani J, Néliat G and Caput D et al.. (1994) SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350: 240-4 [PMID:8070571]
  134. Rinaldi-Carmona M, Barth F, Millan J, Derocq JM, Casellas P, Congy C, Oustric D, Sarran M, Bouaboula M and Calandra B et al.. (1998) SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther 284: 644-50 [PMID:9454810]
  135. Rinaldi-Carmona M, Pialot F, Congy C, Redon E, Barth F, Bachy A, Breliere JC, Soubrie P and Le Fur G. (1996) Characterization and distribution of binding sites for [3H]-SR 141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain. Life Sci 58: 1239-1247 [PMID:8614277]
  136. Ross RA, Brockie HC, Stevenson LA, Murphy VL, Templeton F, Makriyannis A and Pertwee RG. (1999) Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. Br J Pharmacol 126: 665-672 [PMID:10188977]
  137. Ross RA, Coutts AA, McFarlane SM, Anavi-Goffer S, Irving AJ, Pertwee RG, MacEwan DJ and Scott RH. (2001) Actions of cannabinoid receptor ligands on rat cultured sensory neurones: implications for antinociception. Neuropharmacology 40: 221-32 [PMID:11114401]
  138. Roth SH. (1978) Stereospecific presynaptic inhibitory effect of delta9-tetrahydrocannabinol on cholinergic transmission in the myenteric plexus of the guinea pig. Can J Physiol Pharmacol 56: 968-75 [PMID:217512]
  139. Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, Tambaro S, Casti P, Vargiu R and Pani L. (2003) Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor. J Pharmacol Exp Ther 306: 363-70 [PMID:12663689]
  140. Schoeder CT, Hess C, Madea B, Meiler J and Müller CE. (2018) Pharmacological evaluation of new constituents of "Spice": synthetic cannabinoids based on indole, indazole, benzimidazole and carbazole scaffolds. Forensic Toxicol 36: 385-403 [PMID:29963207]
  141. Schuler GD, Boguski MS, Stewart EA, Stein LD, Gyapay G, Rice K, White RE, Rodriguez-Tomé P, Aggarwal A and Bajorek E et al.. (1996) A gene map of the human genome. Science 274: 540-6 [PMID:8849440]
  142. Selley DE, Stark S and Childers SR. (1996) Cannabinoid receptor stimulation of [35S]GTPγS binding in rat brain membranes. Life Sci 59: 659-668 [PMID:8761016]
  143. Shao Z, Yin J, Chapman K, Grzemska M, Clark L, Wang J and Rosenbaum DM. (2016) High-resolution crystal structure of the human CB1 cannabinoid receptor. Nature 540: 602-606 [PMID:27851727]
  144. Sharma MK, Murumkar PR, Barmade MA, Giridhar R and Yadav MR. (2015) A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents. Expert Opin Ther Pat 25: 1093-116 [PMID:26161824]
  145. Sheskin T, Hanus L, Slager J, Vogel Z and Mechoulam R. (1997) Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor. J Med Chem 40: 659-67 [PMID:9057852]
  146. Shire D, Calandra B, Delpech M, Dumont X, Kaghad M, Le Fur G, Caput D and Ferrara P. (1996) Structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A. J Biol Chem 271: 6941-6 [PMID:8636122]
  147. Shire D, Calandra B, Rinaldi-Carmona M, Oustric D, Pessègue B, Bonnin-Cabanne O, Le Fur G, Caput D and Ferrara P. (1996) Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor. Biochim Biophys Acta 1307: 132-6 [PMID:8679694]
  148. Shire D, Carillon C, Kaghad M, Calandra B, Rinaldi-Carmona M, Le Fur G, Caput D and Ferrara P. (1995) An amino-terminal variant of the central cannabinoid receptor resulting from alternative splicing. J Biol Chem 270: 3726-31 [PMID:7876112]
  149. Showalter VM, Compton DR, Martin BR and Abood ME. (1996) Evaluation of binding in a transfected cell line expressing a peripheral cannabinoid receptor (CB2): identification of cannabinoid receptor subtype selective ligands. J Pharmacol Exp Ther 278: 989-99 [PMID:8819477]
  150. Sim LJ, Hampson RE, Deadwyler SA and Childers SR. (1996) Effects of chronic treatment with delta9-tetrahydrocannabinol on cannabinoid-stimulated [35S]GTPgammaS autoradiography in rat brain. J Neurosci 16: 8057-66 [PMID:8987831]
  151. Sim LJ, Selley DE and Childers SR. (1995) In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5'-[gamma-[35S]thio]-triphosphate binding. Proc Natl Acad Sci USA 92: 7242-6 [PMID:7638174]
  152. Sink KS, McLaughlin PJ, Wood JA, Brown C, Fan P, Vemuri VK, Peng Y, Pang Y, Olszewska T and Olzewska T et al.. (2008) The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats. Neuropsychopharmacology 33: 946-55 [PMID:17581535]
  153. Skaper SD, Buriani A, Dal Toso R, Petrelli L, Romanello S, Facci L and Leon A. (1996) The ALIAmide palmitoylethanolamide and cannabinoids, but not anandamide, are protective in a delayed postglutamate paradigm of excitotoxic death in cerebellar granule neurons. Proc Natl Acad Sci USA 93: 3984-9 [PMID:8633002]
  154. Slipetz DM, O'Neill GP, Favreau L, Dufresne C, Gallant M, Gareau Y, Guay D, Labelle M and Metters KM. (1995) Activation of the human peripheral cannabinoid receptor results in inhibition of adenylyl cyclase. Mol Pharmacol 48: 352-61 [PMID:7651369]
  155. Song ZH and Bonner TI. (1996) A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2. Mol Pharmacol 49: 891-6 [PMID:8622639]
  156. Sugawara K, Zákány N, Hundt T, Emelianov V, Tsuruta D, Schäfer C, Kloepper JE, Bíró T and Paus R. (2013) Cannabinoid receptor 1 controls human mucosal-type mast cell degranulation and maturation in situ. J Allergy Clin Immunol 132: 182-93 [PMID:23453134]
  157. Sugiura T, Kodaka T, Kondo S, Tonegawa T, Nakane S, Kishimoto S, Yamashita A and Waku K. (1996) 2-Arachidonoylglycerol, a putative endogenous cannabinoid receptor ligand, induces rapid, transient elevation of intracellular free Ca2+ in neuroblastoma x glioma hybrid NG108-15 cells. Biochem Biophys Res Commun 229: 58-64 [PMID:8954083]
  158. Sugiura T, Kondo S, Sukagawa A, Nakane S, Shinoda A, Itoh K, Yamashita A and Waku K. (1995) 2-Arachidonoylglycerol: a possible endogenous cannabinoid receptor ligand in brain. Biochem Biophys Res Commun 215: 89-97 [PMID:7575630]
  159. Szabo B and Schlicker E. (2005) Effects of cannabinoids on neurotransmission. Handb Exp Pharmacol: 327-65 [PMID:16596780]
  160. Tam J, Cinar R, Liu J, Godlewski G, Wesley D, Jourdan T, Szanda G, Mukhopadhyay B, Chedester L and Liow JS et al.. (2012) Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metab 16: 167-79 [PMID:22841573]
  161. Thomas BF, Gilliam AF, Burch DF, Roche MJ and Seltzman HH. (1998) Comparative receptor binding analyses of cannabinoid agonists and antagonists. J Pharmacol Exp Ther 285: 285-92 [PMID:9536023]
  162. Thomas BF, Wei X and Martin BR. (1992) Characterization and autoradiographic localization of the cannabinoid binding site in rat brain using [3H]11-OH-delta 9-THC-DMH. J Pharmacol Exp Ther 263: 1383-90 [PMID:1335065]
  163. Tsou K, Brown S, Sanudo-Pena MC, Mackie K and Walker JM. (1998) Immunohistochemical distribution of cannabinoid CB1 receptors in the rat central nervous system. Neuroscience 83: 393-411 [PMID:9460749]
  164. Twitchell W, Brown S and Mackie K. (1997) Cannabinoids inhibit N- and P/Q-type calcium channels in cultured rat hippocampal neurons. J Neurophysiol 78: 43-50 [PMID:9242259]
  165. Van Sickle MD, Duncan M, Kingsley PJ, Mouihate A, Urbani P, Mackie K, Stella N, Makriyannis A, Piomelli D and Davison JS et al.. (2005) Identification and functional characterization of brainstem cannabinoid CB2 receptors. Science 310: 329-32 [PMID:16224028]
  166. Ward SJ, Mastriani D, Casiano F and Arnold R. (1990) Pravadoline: profile in isolated tissue preparations. J Pharmacol Exp Ther 255: 1230-1239 [PMID:2175798]
  167. Wiley JL and Martin BR. (2003) Cannabinoid pharmacological properties common to other centrally acting drugs. Eur J Pharmacol 471: 185-93 [PMID:12826237]
  168. Wotherspoon G, Fox A, McIntyre P, Colley S, Bevan S and Winter J. (2005) Peripheral nerve injury induces cannabinoid receptor 2 protein expression in rat sensory neurons. Neuroscience 135: 235-45 [PMID:16084654]
  169. Yao BB, Mukherjee S, Fan Y, Garrison TR, Daza AV, Grayson GK, Hooker BA, Dart MJ, Sullivan JP and Meyer MD. (2006) In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor? Br J Pharmacol 149: 145-54 [PMID:16894349]
  170. Zimmer A, Zimmer AM, Hohmann AG, Herkenham M and Bonner TI. (1999) Increased mortality, hypoactivity, and hypoalgesia in cannabinoid CB1 receptor knockout mice. Proc Natl Acad Sci USA 96: 5780-5 [PMID:10318961]
  171. Zygmunt PM, Petersson J, Andersson DA, Chuang H, Sørgård M, Di Marzo V, Julius D and Högestätt ED. (1999) Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide. Nature 400: 452-7 [PMID:10440374]