Cannabinoid receptors: Nomenclature and pharmacological principles

Progress in Neuro-Psychopharmacology and Biological Psychiatry

Volumn 38, Issue 1, 2012, Pages 4-15

  Console Bram, Linda ^a   Marcu, Jahan ^a   Abood, Mary E ^a  

^a TEMPLE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Cannabinoid; Cannabinoid receptor; Endocannabinoid; G protein coupled receptor; Pharmacology

Indexed keywords

2 ARACHIDONOYLGLYCEROL; 2,3 DIHYDRO 5 METHYL 3 (MORPHOLINOMETHYL) 6 (1 NAPHTHOYL)PYRROLO[1,2,3 DE][1,4]BENZOXAZINE; 4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; 5 (4 CHLORO 3 METHYLPHENYL) 1 (4 METHYLBENZYL) N (1,3,3 TRIMETHYLBICYCLO[2.2.1]HEPTAN 2 YL) 3 PYRAZOLECARBOXAMIDE; ANANDAMIDE; CANNABINOID 1 RECEPTOR; CANNABINOID 2 RECEPTOR; CANNABINOID RECEPTOR; CANNABINOID RECEPTOR AGONIST; CANNABINOID RECEPTOR ANTAGONIST; DRONABINOL; ENDOCANNABINOID; G PROTEIN COUPLED RECEPTOR; RIMONABANT;

ALLOSTERISM; ANTINOCICEPTION; CHEMICAL STRUCTURE; DRUG STRUCTURE; GENE OVEREXPRESSION; GENE STRUCTURE; GENETIC POLYMORPHISM; HUMAN; NOMENCLATURE; NONHUMAN; PROTEIN CONFORMATION; PROTEIN FAMILY; RECEPTOR DOWN REGULATION; RECEPTOR UPREGULATION; REVIEW; SPECIES DIFFERENCE; TRANQUILIZING ACTIVITY;

ANIMALS; BRAIN; CANNABINOIDS; POLYMORPHISM, GENETIC; RECEPTORS, CANNABINOID; SIGNAL TRANSDUCTION; TERMINOLOGY AS TOPIC;

EID: 84862900994     PISSN: 02785846     EISSN: 18784216     Source Type: Journal    
DOI: 10.1016/j.pnpbp.2012.02.009     Document Type: Review

References (168)

1. Abood M.E. Molecular biology of cannabinoid receptors. Handbook of experimental pharmacology 2005, 81-115.
2. Abood M.E., Ditto K.A., Noel M.A., Showalter V.M., Tao Q. Isolation and expression of mouse CB1 cannabinoid receptor gene: comparison of binding properties with those of native CB1 receptors in mouse brain and N18TG2 neuroblastoma cells. Biochem Pharmacol 1997, 53:207-214.
3. Agarwal N., Pacher P., Tegeder I., Amaya F., Constantin C.E., Brenner G.J., et al. Cannabinoids mediate analgesia largely via peripheral type 1 cannabinoid receptors in nociceptors. Nat Neurosci 2007, 10:870-879.
4. Ahmed S.A., Ross S.A., Slade D., Radwan M.M., Zulfiqar F., Matsumoto R.R., et al. Cannabinoid ester constituents from high-potency Cannabis sativa. J Nat Prod 2008, 71:536-542.
5. Baker S.J., Fearon E.R., Nigro J.M., Hamilton S.R., Preisinger A.C., Jessup J.M., et al. Chromosome 17 deletions and p53 gene mutations in colorectal carcinomas. Science 1989, 244:217-221.
6. Baker D., Pryce G., Davies W.L., Hiley C.R. In silico patent searching reveals a new cannabinoid receptor. Trends Pharmacol Sci 2006, 27:1-4. Epub 2005 Nov 2028.
7. Barrero F.J., Ampuero I., Morales B., Vives F., de Dios Luna Del Castillo J., Hoenicka J., et al. Depression in Parkinson's disease is related to a genetic polymorphism of the cannabinoid receptor gene (CNR1). Pharmacogenomics J 2005, 5:135-141.
8. Ben-Shabat S., Fride E., Sheskin T., Tamiri T., Rhee M.H., Vogel Z., et al. An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity. Eur J Pharmacol 1998, 353:23-31.
9. Bonner T. Molecular biology of cannabinoid receptors. J Neuroimmunol 1996, 69:15-23.
10. Bouaboula M., Poinot-Chazel C., Bourrie B., Canat X., Calandra B., Rinaldi-Carmona M., et al. Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1. Biochem J 1995, 312(Pt 2):637-641.
11. Bouaboula M., Perrachon S., Milligan L., Canat X., Rinaldi-Carmona M., Portier M., et al. A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin-like growth factor 1. J Biol Chem 1997, 272:22330-22339.
12. + exchanger NHE-1 isoform via Gi-mediated mitogen activated protein kinase signaling transduction pathways. FEBS Lett 1999, 449:61-65.
13. Bouaboula M., Desnoyer N., Carayon P., Combes T., Casellas P. Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation. Mol Pharmacol 1999, 55:473-480.
14. Bouaboula M., Dussossoy D., Casellas P. Regulation of peripheral cannabinoid receptor CB2 phosphorylation by the inverse agonist SR 144528. Implications for receptor biological responses. J Biol Chem 1999, 274:20397-20405.
15. Neuromethods 4: receptor binding 1986, Humana, Clifton, NJ. A.A. Boulton, G.B. Baker, P.D. Hrdina (Eds.).
16. Bradshaw H.B., Rimmerman N., Hu S.S., Benton V.M., Stuart J.M., Masuda K., et al. The endocannabinoid anandamide is a precursor for the signaling lipid N-arachidonoyl glycine by two distinct pathways. BMC Biochem 2009, 10:14.
17. Breivogel C.S., Griffin G., Di Marzo V., Martin B.R. Evidence for a new G protein-coupled cannabinoid receptor in mouse brain. Mol Pharmacol 2001, 60:155-163.
18. Brown S.M., Wager-Miller J., Mackie K. Cloning and molecular characterization of the rat CB2 cannabinoid receptor. Biochim Biophys Acta 2002, 1576:255-264.
19. Buckley N.E., McCoy K.L., Mezey E., Bonner T., Zimmer A., Felder C.C., et al. Immunomodulation by cannabinoids is absent in mice deficient for the cannabinoid CB(2) receptor. Eur J Pharmacol 2000, 396:141-149.
20. Busquets-Garcia A., Puighermanal E., Pastor A., de la Torre R., Maldonado R., Ozaita A. Differential role of anandamide and 2-arachidonoylglycerol in memory and anxiety-like responses. Biol Psychiatry 2011, 70:479-486.
21. Caenazzo L., Hoehe M., Hsieh W., Berrettini W., Bonner T., Gershon E. HindIII identifies a two allele DNA polymorphism of the human cannabinoid receptor gene (CNR). Nucleic Acids Res 1991, 19:4798.
22. Carrasquer A., Nebane N.M., Williams W.M., Song Z.H. Functional consequences of nonsynonymous single nucleotide polymorphisms in the CB2 cannabinoid receptor. Pharmacogenet Genomics 2010, 20:157-166.
23. Chakrabarti A., Onaivi E.S., Chaudhuri G. Cloning and sequencing of a cDNA encoding the mouse brain-type cannabinoid receptor protein. DNA Seq 1995, 5:385-388.
24. Comings D., Muhleman D., Gade R., Johnson P., Verde R., Saucier G., et al. Cannabinoid receptor gene (CNR1): association with i.v. drug use. Mol Psychiatry 1997, 2:161-168.
25. Conn P.J., Christopoulos A., Lindsley C.W. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 2009, 8:41-54.
26. Costa T., Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci U S A 1989, 86:7321-7325.
27. Cottone E., Salio C., Conrath M., Franzoni M.F. Xenopus laevis CB1 cannabinoid receptor: molecular cloning and mRNA distribution in the central nervous system. J Comp Neurol 2003, 464:487-496.
28. Coutts A., Brewster N., Ingram T., Razdan R., Pertwee R. Comparison of novel cannabinoid partial agonists and SR141716A in the guinea-pig small intestine. Br J Pharmacol 2000, 129:645-652.
29. De Petrocellis L., Ligresti A., Moriello A.S., Allara M., Bisogno T., Petrosino S., et al. Effects of cannabinoids and cannabinoid-enriched cannabis extracts on TRP channels and endocannabinoid metabolic enzymes. Br J Pharmacol 2011, 163:1479-1494.
30. Devane W.A., Dysarz F.A., Johnson M.R., Melvin L.S., Howlett A.C. Determination and characterization of a cannabinoid receptor in rat brain. Mol Pharmacol 1988, 34:605-613.
31. Devane W.A., Hanus L., Breuer A., Pertwee R.G., Stevenson L.A., Griffin G., et al. Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 1992, 258:1946-1949.
32. Di Marzo V., Fontana A., Cadas H., Schinelli S., Cimino G., Schwartz J.C., et al. Formation and inactivation of endogenous cannabinoid anandamide in central neurons. Nature 1994, 372:686-691.
33. Di Marzo V., Melck D., Bisogno T., De Petrocellis L. Endocannabinoids: endogenous cannabinoid receptor ligands with neuromodulatory action. Trends Neurosci 1998, 21:521-528.
34. Di Marzo V., Breivogel C.S., Tao Q., Bridgen D.T., Razdan R.K., Zimmer A.M., et al. Levels, metabolism, and pharmacological activity of anandamide in CB(1) cannabinoid receptor knockout mice: evidence for non-CB(1), non-CB(2) receptor-mediated actions of anandamide in mouse brain. J Neurochem 2000, 75:2434-2444.
35. Downer E.J. Cannabinoids and innate immunity: taking a toll on neuroinflammation. Sci World J 2011, 11:855-865.
36. Du H., Chen X., Zhang J., Chen C. Inhibition of COX-2 expression by endocannabinoid 2-arachidonoylglycerol is mediated via PPAR-gamma. Br J Pharmacol 2011, 163:1533-1549.
37. Eissenstat M.A., Bell M.R., D'Ambra T.E., Alexander E.J., Daum S.J., Ackerman J.H., et al. Aminoalkylindoles: structure-activity relationships of novel cannabinoid mimetics. J Med Chem 1995, 38:3094-3105.
38. Elphick M.R. Evolution of cannabinoid receptors in vertebrates: identification of a CB(2) gene in the puffer fish Fugu rubripes. Biol Bull 2002, 202:104-107.
39. Elphick M.R., Egertova M. The neurobiology and evolution of cannabinoid signalling. Philos Trans R Soc Lond B Biol Sci 2001, 356:381-408.
40. Elphick M.R., Satou Y., Satoh N. The invertebrate ancestry of endocannabinoid signalling: an orthologue of vertebrate cannabinoid receptors in the urochordate Ciona intestinalis. Gene 2003, 302:95-101.
41. Elsohly M.A., Slade D. Chemical constituents of marijuana: the complex mixture of natural cannabinoids. Life Sci 2005, 78:539-548.
42. Facci L., Toso R.D., Romanello S., Buriani A., Skaper S.D., Leon A. Mast cells express a peripheral cannabinoid receptor with differential sensitivity to anandamide and palmitoylethanolamide. Proc Natl Acad Sci U S A 1995, 92:3376-3380.
43. Felder C.C., Veluz J.S., Williams H.L., Briley E.M., Matsuda L.A. Cannabinoid agonists stimulate both receptor- and non-receptor-mediated signal transduction pathways in cells transfected with and expressing cannabinoid receptor clones. Mol Pharmacol 1992, 42:838-845.
44. Franklin A., Stella N. Arachidonylcyclopropylamide increases microglial cell migration through cannabinoid CB2 and abnormal-cannabidiol-sensitive receptors. Eur J Pharmacol 2003, 474:195-198.
45. Franklin A., Parmentier-Batteur S., Walter L., Greenberg D.A., Stella N. Palmitoylethanolamide increases after focal cerebral ischemia and potentiates microglial cell motility. J Neurosci 2003, 23:7767-7775.
46. Fredriksson R., Lagerstrom M.C., Lundin L.G., Schioth H.B. The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol 2003, 63:1256-1272.
47. Gadzicki D., Muller-Vahl K., Stuhrmann M. A frequent polymorphism in the coding exon of the human cannabinoid receptor (CNR1) gene. Mol Cell Probes 1999, 13:321-323.
48. Gerard C.M., Mollereau C., Vassart G., Parmentier M. Molecular cloning of a human cannabinoid receptor which is also expressed in testis. Biochem J 1991, 279:129-134.
49. Gonsiorek W., Lunn C., Fan X., Narula S., Lundell D., Hipkin R.W. Endocannabinoid 2-arachidonyl glycerol is a full agonist through human type 2 cannabinoid receptor: antagonism by anandamide. Mol Pharmacol 2000, 57:1045-1050.
50. Greasley P.J., Clapham J.C. Inverse agonism or neutral antagonism at G-protein coupled receptors: a medicinal chemistry challenge worth pursuing?. Eur J Pharmacol 2006, 553:1-9.
51. Griffin G., Tao Q., Abood M. Cloning and pharmacological characterization of the rat CB2 cannabinoid receptor. J Pharmacol Exp Ther 2000, 292.
52. Guindon J., Guijarro A., Piomelli D., Hohmann A.G. Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain. Br J Pharmacol 2011, 163:1464-1478.
53. Hajos N., Ledent C., Freund T.F. Novel cannabinoid-sensitive receptor mediates inhibition of glutamatergic synaptic transmission in the hippocampus. Neuroscience 2001, 106:1-4.
54. Hanus L., Gopher A., Almog S., Mechoulam R. Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor. J Med Chem 1993, 36:3032-3034.
55. Hanus L., Breuer A., Tchilibon S., Shiloah S., Goldenberg D., Horowitz M., et al. HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor. Proc Natl Acad Sci U S A 1999, 96:14228-14233.
56. Hejazi N., Zhou C., Oz M., Sun H., Ye J.H., Zhang L. Delta9-tetrahydrocannabinol and endogenous cannabinoid anandamide directly potentiate the function of glycine receptors. Mol Pharmacol 2006, 69:991-997.
57. Henstridge C.M., Balenga N.A., Kargl J., Andradas C., Brown A.J., Irving A., et al. Minireview: recent developments in the physiology and pathology of the lysophosphatidylinositol-sensitive receptor GPR55. Mol Endocrinol 2011, 25:1835-1848.
58. Hillard C., Muthian S., Kearn C. Effects of CB(1) cannabinoid receptor activation on cerebellar granule cell nitric oxide synthase activity. FEBS Lett 1999, 459:277-281.
59. Hillard C.J., Manna S., Greenberg M.J., DiCamelli R., Ross R.A., Stevenson L.A., et al. Synthesis and characterization of potent and selective agonists of the neuronal cannabinoid receptor (CB1). J Pharmacol Exp Ther 1999, 289:1427-1433.
60. Ho B.Y., Zhao J. Determination of the cannabinoid receptors in mouse×rat hybridoma NG108-15 cells and rat GH4C1 cells. Neurosci Lett 1996, 212:123-126.
61. Houston D.B., Howlett A.C. Differential receptor-G-protein coupling evoked by dissimilar cannabinoid receptor agonists. Cell Signal 1998, 10:667-674.
62. Howlett A.C. Pharmacology of cannabinoid receptors. Ann Rev Pharmacol Toxicol 1995, 35:607-634.
63. Howlett A.C., Barth F., Bonner T.I., Cabral G., Casellas P., Devane W.A., et al. International Union of Pharmacology. XXVII. Classification of cannabinoid receptors. Pharmacol Rev 2002, 54:161-202.
64. Howlett A.C., Reggio P.H., Childers S.R., Hampson R.E., Ulloa N.M., Deutsch D.G. Endocannabinoid tone versus constitutive activity of cannabinoid receptors. Br J Pharmacol 2011, 163:1329-1343.
65. Hsieh C., Brown S., Derleth C., Mackie K. Internalization and recycling of the CB1 cannabinoid receptor. J Neurochem 1999, 493-501.
66. Huang S.M., Bisogno T., Petros T.J., Chang S.Y., Zavitsanos P.A., Zipkin R.E., et al. Identification of a new class of molecules, the arachidonyl amino acids, and characterization of one member that inhibits pain. J Biol Chem 2001, 276:42639-42644.
67. Huang S.M., Bisogno T., Trevisani M., Al-Hayani A., De Petrocellis L., Fezza F., et al. An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors. Proc Natl Acad Sci U S A 2002, 99:8400-8405.
68. Huang Q.Y., Li G.H., Kung A.W. Multiple osteoporosis susceptibility genes on chromosome 1p36 in Chinese. Bone 2009, 44:984-988.
69. Hulme EC Receptor-ligand interactions. A Practical Approach 1992, Oxford Univ. Press, New York.
70. Hulme E.C., Birdsall N Strategy and tactics in receptor binding studies. Receptor-ligand interactions-a practical approach: Oxford 1992.
71. Hulme E.C., Trevethick M.A. Ligand binding assays at equilibrium: validation and interpretation. Br J Pharmacol 2010, 161:1219-1237.
72. Iliff H.A., Lynch D.L., Kotsikorou E., Reggio P.H. Parameterization of Org27569: An allosteric modulator of the cannabinoid CB(1) G protein-coupled receptor. J Comput Chem 2011.
73. Ishac E.J.N., Jiang L., Lake K.D., Varga K., Abood M.E., Kunos G. Inhibition of exocytotic noradrenaline release by presynaptic cannabinoid CB1 receptors on peripheral sympathetic nerves. Br J Pharmacol 1996, 118:2023-2028.
74. Jarai Z., Wagner J., Varga K., Lake K., Compton D., Martin B., et al. Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors. Proc Natl Acad Sci U S A 1999, 96:14136-14141.
75. Jin W., Brown S., Roche J., Hsieh C., Celver J., Kovoor A., et al. Distinct domains of the CB1 cannabinoid receptor mediate desensitization and internalization. J Neurosci 1999, 19:3773-3780.
76. Kapur A., Samaniego P., Thakur G.A., Makriyannis A., Abood M.E. Mapping the structural requirements in the CB1 cannabinoid receptor transmembrane helix II for signal transduction. J Pharmacol Exp Ther 2008, 325:341-348.
77. Kapur A., Zhao P., Sharir H., Bai Y., Caron M.G., Barak L.S., et al. Atypical responsiveness of the orphan receptor GPR55 to cannabinoid ligands. J Biol Chem 2009, 284:29817-29827.
78. Karsak M., Cohen-Solal M., Freudenberg J., Ostertag A., Morieux C., Kornak U., et al. Cannabinoid receptor type 2 gene is associated with human osteoporosis. Hum Mol Genet 2005, 14:3389-3396. Epub 2005 Oct 3384.
79. Karsak M., Malkin I., Toliat M.R., Kubisch C., Nurnberg P., Zimmer A., et al. The cannabinoid receptor type 2 (CNR2) gene is associated with hand bone strength phenotypes in an ethnically homogeneous family sample. Hum Genet 2009.
80. Kathmann M., Haug K., Heils A., Nothen M., Schlicker E. Exchange of three amino acids in the cannabinoid CB1 receptor (CNR1) of an epilepsy patient. 2000 Symposium on the Cannabinoids Burlington 2000, International Cannabinoid Research Society, Vermont.
81. Katzung B.G., Master S.B., Trevor A.J. Basic and clinical pharmacology 2009, Lange. Eleventh Edition.
82. Kenakin T.E. Pharmacologic analysis of drug receptor interactions 1993, Raven, New York.
83. Kenakin T. Inverse, protean, and ligand-selective agonism: matters of receptor conformation. FASEB J 2001, 15:598-611.
84. Kenakin T. Efficacy as a vector: the relative prevalence and paucity of inverse agonism. Mol Pharmacol 2004, 65:2-11.
85. Kohno M., Hasegawa H., Inoue A., Muraoka M., Miyazaki T., Oka K., et al. Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18. Biochem Biophys Res Commun 2006, 347:827-832.
86. Kreutz S., Koch M., Bottger C., Ghadban C., Korf H.W., Dehghani F. 2-Arachidonoylglycerol elicits neuroprotective effects on excitotoxically lesioned dentate gyrus granule cells via abnormal-cannabidiol-sensitive receptors on microglial cells. Glia 2009, 57:286-294.
87. Lambert D., DiPaolo F., Sonveaux P., Kanyonyo M., Govaerts S., Hermans E., et al. Analogues and homologues of N-palmitoylethanolamide, a putative endogenous CB(2) cannabinoid, as potential ligands for the cannabinoid receptors. Biochim Biophys Acta 1999, 1440:266-274.
88. Lamlum H., Papadopoulou A., Ilyas M., Rowan A., Gillet C., Hanby A., et al. APC mutations are sufficient for the growth of early colorectal adenomas. Proc Natl Acad Sci U S A 2000, 97:2225-2228.
89. Landsman R.S., Burkey T.H., Consroe P., Roeske W.R., Yamamura H.I. SR141716A is an inverse agonist at the human cannabinoid CB1 receptor. Eur J Pharmacol 1997, 334:R1-R2.
90. Ledent C., Valverde O., Cossu G., Petitet F., Aubert J., Beslot F., et al. Unresponsiveness to cannabinoids and reduced addictive effects of opiates in CB1 receptor knockout mice. Science 1999, 283:401-404.
91. Lefkowitz R.J., Cotecchia S., Samama P., Costa T. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 1993, 14:303-307.
92. Lenman A., Fowler C.J. Interaction of ligands for the peroxisome proliferator-activated receptor gamma with the endocannabinoid system. Br J Pharmacol 2007, 151:1343-1351.
93. Leurs R., Smit M., Alewijnse A., Timmerman H. Agonist-independent regulation of constitutively active G-protein-coupled receptors. Trends Biochem Sci 1998, 23:418-422.
94. Limbird L.E.E. Cell surface receptors: a short course on theory and methods 1986, Martinus Nijhoff, Boston, MA.
95. Lipton S.A. Failures and successes of NMDA receptor antagonists: molecular basis for the use of open-channel blockers like memantine in the treatment of acute and chronic neurologic insults. NeuroRx 2004, 1:101-110.
96. Liu Q.R., Pan C.H., Hishimoto A., Li C.Y., Xi Z.X., Llorente-Berzal A., et al. Species differences in cannabinoid receptor 2 (CNR2 gene): identification of novel human and rodent CB2 isoforms, differential tissue expression and regulation by cannabinoid receptor ligands. Genes Brain Behav 2009, 8:519-530.
97. Lopez-Moreno J.A., Gonzalez-Cuevas G., Moreno G., Navarro M. The pharmacology of the endocannabinoid system: functional and structural interactions with other neurotransmitter systems and their repercussions in behavioral addiction. Addict Biol 2008, 13:160-187.
98. Brain receptor methodologies. Part 1. General methods and concepts. Amines and acetylcholine 1984, Academic, Orlando, FL. P.J. Marangos, I.C. Campbell, R.M. Cohen (Eds.).
99. Marsicano G., Wotjak C.T., Azad S.C., Bisogno T., Rammes G., Cascio M.G., et al. The endogenous cannabinoid system controls extinction of aversive memories. Nature 2002, 418:530-534.
100. Marsicano G., Goodenough S., Monory K., Hermann H., Eder M., Cannich A., et al. CB1 cannabinoid receptors and on-demand defense against excitotoxicity. Science 2003, 302:84-88.
101. Matsuda L.A., Lolait S.J., Brownstein M.J., Young A.C., Bonner T.I. Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 1990, 346:561-564.
102. McAllister S., Griffin G., Satin L., Abood M. Cannabinoid receptors can activate and inhibit G protein-coupled inwardly rectifying potassium channels in a Xenopus oocyte expression system. J Pharmacol Exp Ther 1999, 291:618-626.
103. McAllister S.D., Hurst D.P., Barnett-Norris J., Lynch D., Reggio P.H., Abood M.E. Structural mimicry in class A G protein-coupled receptor rotamer toggle switches: the importance of the F3.36(201)/W6.48(357) interaction in cannabinoid CB1 receptor activation. J Biol Chem 2004, 279:48024-48037. Epub 42004 Aug 48023.
104. McHugh D., Hu S.S., Rimmerman N., Juknat A., Vogel Z., Walker J.M., et al. N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor. BMC Neurosci 2010, 11:44.
105. McHugh D., Page J., Dunn E., Bradshaw H.B. Delta(9)-THC and N-arachidonyl glycine are full agonists at GPR18 and cause migration in the human endometrial cell line, HEC-1B. Br J Pharmacol 2011, 2011:1476-5381.
106. McPartland J.M., Glass M. Functional mapping of cannabinoid receptor homologs in mammals, other vertebrates, and invertebrates. Gene 2003, 312:297-303.
107. McPartland J.M., Glass M., Matias I., Norris R.W., Kilpatrick C.W. A shifted repertoire of endocannabinoid genes in the zebrafish (Danio rerio). Mol Genet Genomics 2007, 277:555-570.
108. Mechoulam R., Fride E. The unpaved road to the endogenous cannabinoid ligand anandamide. Cannabinoids 1995, 233-258.
109. Mechoulam R., Ben-Shabat S., Hanus L., Ligumsky M., Kaminski N.E., Schatz A.R., et al. Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors. Biochem Pharmacol 1995, 50:83-90.
110. Monory K., Tzavara E.T., Lexime J., Ledent C., Parmentier M., Borsodi A., et al. Novel, not adenylyl cyclase-coupled cannabinoid binding site in cerebellum of mice. Biochem Biophys Res Commun 2002, 292:231-235.
111. Munro S., Thomas K.L., Abu-Shaar M. Molecular characterization of a peripheral receptor for cannabinoids. Nature 1993, 365:61-65.
112. Murphy W.J., Eizirik E., Johnson W.E., Zhang Y.P., Ryder O.A., O'Brien S.J. Molecular phylogenetics and the origins of placental mammals. Nature 2001, 409:614-618.
113. Naidu P.S., Booker L., Cravatt B.F., Lichtman A.H. Synergy between enzyme inhibitors of fatty acid amide hydrolase and cyclooxygenase in visceral nociception. J Pharmacol Exp Ther 2009, 329:48-56.
114. Ndong C., O'Donnell D., Ahmad S., Groblewski T. Cloning and pharmacological characterization of the dog cannabinoid CB(2) receptor. Eur J Pharmacol 2011.
115. Nie J., Lewis D.L. The proximal and distal C-terminal tail domains of the CB1 cannabinoid receptor mediate G protein coupling. Neuroscience 2001, 107:161-167.
116. Offertaler L., Mo F.M., Batkai S., Liu J., Begg M., Razdan R.K., et al. Selective ligands and cellular effectors of a G protein-coupled endothelial cannabinoid receptor. Mol Pharmacol 2003, 63:699-705.
117. Osei-Hyiaman D., Liu J., Zhou L., Godlewski G., Harvey-White J., Jeong W.I., et al. Hepatic CB1 receptor is required for development of diet-induced steatosis, dyslipidemia, and insulin and leptin resistance in mice. J Clin Invest 2008, 118:3160-3169.
118. 2+ currents by reversal of tonic CB1 cannabinoid receptor activity. Mol Pharmacol 1998, 54:1064-1072.
119. Pernia-Andrade A.J., Kato A., Witschi R., Nyilas R., Katona I., Freund T.F., et al. Spinal endocannabinoids and CB1 receptors mediate C-fiber-induced heterosynaptic pain sensitization. Science 2009, 325:760-764.
120. Pertwee R.G. Pharmacology of cannabinoid receptor ligands. Curr Med Chem 1999, 6:635-664.
121. Pertwee R.G., Howlett A.C., Abood M.E., Alexander S.P., Di Marzo V., Elphick M.R., et al. International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid receptors and their ligands: beyond CB and CB. Pharmacol Rev 2010, 62:588-631.
122. Porter A.C., Sauer J.M., Knierman M.D., Becker G.W., Berna M.J., Bao J., et al. Characterization of a novel endocannabinoid, virodhamine, with antagonist activity at the CB1 receptor. J Pharmacol Exp Ther 2002, 301:1020-1024.
123. Radwan M.M., Ross S.A., Slade D., Ahmed S.A., Zulfiqar F., Elsohly M.A. Isolation and characterization of new cannabis constituents from a high potency variety. Planta Med 2008, 74:267-272.
124. Rinaldi-Carmona M., Barth F., Heaulme M., Shire D., Calandra B., Congy C., et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994, 350:240-244.
125. Rinaldi-Carmona M., Duigou A.L., Oustric D., Barth F., Bouaboula M., Carayon P., et al. Modulation of CB1 cannabinoid receptor functions after a long-term exposure to agonist or inverse agonist in the chinese hamster ovary cell expression system. J Pharmacol Exp Ther 1998, 287:1038-1047.
126. Roche J., Bounds S., Brown S., Mackie K. A mutation in the second transmembrane region of the CB1 receptor selectively disrupts G protein signaling and prevents receptor internalization. Mol Pharmacol 1999, 56:611-618.
127. Rockwell C.E., Snider N.T., Thompson J.T., Vanden Heuvel J.P., Kaminski N.E. Interleukin-2 suppression by 2-arachidonyl glycerol is mediated through peroxisome proliferator-activated receptor gamma independently of cannabinoid receptors 1 and 2. Mol Pharmacol 2006, 70:101-111.
128. Romano M.R., Lograno M.D. Cannabinoid agonists induce relaxation in the bovine ophthalmic artery: evidences for CB1 receptors, nitric oxide and potassium channels. Br J Pharmacol 2006, 147:917-925.
129. Ross R.A. The enigmatic pharmacology of GPR55. Trends Pharmacol Sci 2009, 30:156-163.
130. Ross H.R., Gilmore A.J., Connor M. Inhibition of human recombinant T-type calcium channels by the endocannabinoid N-arachidonoyl dopamine. Br J Pharmacol 2009, 156:740-750.
131. Russo E.B. Clinical endocannabinoid deficiency (CECD): can this concept explain therapeutic benefits of cannabis in migraine, fibromyalgia, irritable bowel syndrome and other treatment-resistant conditions?. Neuro Endocrinol Lett 2008, 29:192-200.
132. Ryberg E., Vu H.K., Larsson N., Groblewski T., Hjorth S., Elebring T., et al. Identification and characterisation of a novel splice variant of the human CB1 receptor. FEBS Lett 2005, 579:259-264.
133. Ryberg E., Larsson N., Sjogren S., Hjorth S., Hermansson N.O., Leonova J., et al. The orphan receptor GPR55 is a novel cannabinoid receptor. Br J Pharmacol 2007, 152:1092-1101.
134. Sharir H., Abood M.E. Pharmacological characterization of GPR55, a putative cannabinoid receptor. Pharmacol Ther 2010, 126:301-313.
135. Shen C.P., Xiao J.C., Armstrong H., Hagmann W., Fong T.M. F200A substitution in the third transmembrane helix of human cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist. Eur J Pharmacol 2006, 531:41-46.
136. Sheskin T., Hanus L., Slager J., Vogel Z., Mechoulam R. Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor. J Med Chem 1997, 40:659-667.
137. Shire D., Carillon C., Kaghad M., Calandra B., Rinaldi-Carmona M., Fur G.L., et al. An amino-terminal variant of the central cannabinoid receptor resulting from alternative splicing. J Biol Chem 1995, 270:3726-3731.
138. Shire D., Calandra B., Rinaldi-Carmona M., Oustric D., Pessegue B., Bonnin-Cabanne O., et al. Molecular cloning, expression and function of the murine CB2 peripheral cannabinoid receptor. Biochim Biophys Acta 1996, 1307:132-136.
139. Showalter V.M., Compton D.R., Martin B.R., Abood M.E. 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 1996, 278:989-999.
140. Singh R., Hurst D.P., Barnett-Norris J., Lynch D.L., Reggio P.H., Guarnieri F. Activation of the cannabinoid CB1 receptor may involve a W6 48/F3 36 rotamer toggle switch. J Pept Res 2002, 60:357-370.
141. Sipe J.C., Arbour N., Gerber A., Beutler E. Reduced endocannabinoid immune modulation by a common cannabinoid 2 (CB2) receptor gene polymorphism: possible risk for autoimmune disorders. J Leukoc Biol 2005, 78:231-238. Epub 2005 Apr 2021.
142. Soderstrom K., Leid M., Moore F.L., Murray T.F. Behavioral, pharmacological, and molecular characterization of an amphibian cannabinoid receptor. J Neurochem 2000, 75:413-423.
143. Song Z.H., Bonner T.I. A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN55212-2. Mol Pharmacol 1996, 49:891-896.
144. Steffens M., Zentner J., Honegger J., Feuerstein T.J. Binding affinity and agonist activity of putative endogenous cannabinoids at the human neocortical CB1 receptor. Biochem Pharmacol 2005, 69:169-178.
145. Stella N. Cannabinoid and cannabinoid-like receptors in microglia, astrocytes, and astrocytomas. Glia 2010, 58:1017-1030.
146. Sugiura T. Physiological roles of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand. Biofactors 2009, 35:88-97.
147. Sugiura T., Kondo S., Kishimoto S., Miyashita T., Nakane S., Kodaka T., et al. Evidence that 2-arachidonoylglycerol but not N-palmitoylethanolamine or anandamide is the physiological ligand for the cannabinoid CB2 receptor. Comparison of the agonistic activities of various cannabinoid receptor ligands in hl-60 cells. J Biol Chem 2000, 275:605-612.
148. Sum C.S., Pyo N., Wells J.W. Apparent capacity of cardiac muscarinic receptors for different radiolabeled antagonists. Biochem Pharmacol 2001, 62:829-851.
149. Takenouchi R., Inoue K., Kambe Y., Miyata A. N-arachidonoyl glycine induces macrophage apoptosis via GPR18. Biochem Biophys Res Commun 2012, 418:366-371.
150. Thomas W., Qian H., Chang C., Karnik S. Agonist-induced phosphorylation of the angiotensin II (AT(1A)) receptor requires generation of a conformation that is distinct from the inositol phosphate-signaling state. J Biol Chem 2000, 275:2893-2900.
151. Turner C.E., Bouwsma O.J., Billets S., Elsohly M.A. Constituents of Cannabis sativa L. XVIII-electron voltage selected ion monitoring study of cannabinoids. Biomed Mass Spectrom 1980, 7:247-256.
152. Ujike H., Takaki M., Nakata K., Tanaka Y., Takeda T., Kodama M., et al. CNR1, central cannabinoid receptor gene, associated with susceptibility to hebephrenic schizophrenia. Mol Psychiatry 2002, 7:515-518.
153. Valk P.J.M., Hol S., Vankan Y., Ihle J.N., Askew D., Jenkins N.A., et al. The genes encoding the peripheral cannabinoid receptor and a-l-fucosidase are located near a newly identified common virus integration site. J Virol 1997, 71:6796-6804.
154. Vasquez C., Lewis D.L. The CB1 cannabinoid receptor can sequester G-proteins, making them unavailable to couple to other receptors. J Neurosci 1999, 19:9271-9280.
155. Wagner J., Varga K., Jarai Z., Kunos G. Mesenteric vasodilation mediated by endothelial anandamide receptors. Hypertension 1999, 33:429-434.
156. Walter L., Franklin A., Witting A., Wade C., Xie Y., Kunos G., et al. Nonpsychotropic cannabinoid receptors regulate microglial cell migration. J Neurosci 2003, 23:1398-1405.
157. Wang L., Martin B., Brenneman R., Luttrell L.M., Maudsley S. Allosteric modulators of G protein-coupled receptors: Future therapeutics for complex physiological disorders. J Pharmacol Exp Ther 2009, 331(2):340-348.
158. White R., Ho W.S., Bottrill F.E., Ford W.R., Hiley C.R. Mechanisms of anandamide-induced vasorelaxation in rat isolated coronary arteries. Br J Pharmacol 2001, 134:921-929.
159. Wiles A.L., Pearlman R.J., Rosvall M., Aubrey K.R., Vandenberg R.J. N-Arachidonyl-glycine inhibits the glycine transporter, GLYT2a. J Neurochem 2006, 99:781-786.
160. Receptor pharmacology and function 1989, Dekker, New York. M.R.A.G. Williams, P. Timmermans (Eds.).
161. Xie X.Q., Melvin L.S., Makryiannis A. The comformational properties of the highly selective cannabinoid receptor ligand CP-55,940. J Biol Chem 1996, 271:10640-10647.
162. Yamada Y., Ando F., Shimokata H. Association of candidate gene polymorphisms with bone mineral density in community-dwelling Japanese women and men. Int J Mol Med 2007, 19:791-801.
163. Yamaguchi F., Macrae A.D., Brenner S. Molecular cloning of two cannabinoid type-1 receptor genes from the puffer fish Fugu rubripes. Genomics 1996, 35:603-605.
164. Yamamura H., Enna SJ, Kuhar Michael Methods in neurotransmitter receptor analysis 1990, Raven Press, New York.
165. Yevenes G.E., Zeilhofer H.U. Molecular sites for the positive allosteric modulation of glycine receptors by endocannabinoids. PLoS One 2011, 6:e23886.
166. Zhang P.W., Ishiguro H., Ohtsuki T., Hess J., Carillo F., Walther D., et al. Human cannabinoid receptor 1: 5' exons, candidate regulatory regions, polymorphisms, haplotypes and association with polysubstance abuse. Mol Psychiatry 2004, 9:916-931.
167. Zimmer A., Zimmer A., Hohmann A., Herkenham M., Bonner T. Increased mortality, hypoactivity, and hypoalgesia in cannabinoid CB1 receptor knockout mice. Proc Natl Acad Sci U S A 1999, 5780-5785.
168. Zygmunt P., Petersson J., Andersson D., Chuang H., Sorgard M., DiMarzo V., et al. Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide. Nature 1999, 400:452-457.