Pharmacology of cannabinoid CB1 and CB2 receptors

Pharmacology & Therapeutics - Tập 74 Số 2 - Trang 129-180 - 1997
Roger G. Pertwee1
1Department of Biomedical Sciences, Institute of Medical Sciences, Foresterhill, UK.

Tóm tắt

Từ khóa


Tài liệu tham khảo

Abadji, 1994, (R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability, J. Med. Chem., 37, 1889, 10.1021/jm00038a020

Abood, 1993, Development of behavioral tolerance to Δ9-THC without alteration of cannabinoid receptor binding or mRNA levels in whole brain, Pharmacol. Biochem. Behav., 46, 575, 10.1016/0091-3057(93)90546-6

Adams, 1995, Evaluation of cannabinoid receptor binding and in vivo activities for anandamide analogs, J. Pharmacol. Exp. Ther., 273, 1172

Balster, 1992, Δ9-Tetrahydrocannabinol discrimination in rats as a model for cannabis intoxication, Neurosci. Biobehav. Revs., 16, 55, 10.1016/S0149-7634(05)80051-X

Barg, 1995, Cannabinomimetic behavioral effects of and adenylate cyclase inhibition by two new endogenous anandamides, Eur. J. Pharmacol., 287, 145, 10.1016/0014-2999(95)00487-4

Barrett, 1995, Pharmacological specificity of Δ9-tetrahydrocannabinol discrimination in rats, Psychopharmacology, 118, 419, 10.1007/BF02245942

Bayewitch, 1995, The peripheral cannabinoid receptor: adenylate cyclase inhibition and G protein coupling, FEBS Lett., 375, 143147, 10.1016/0014-5793(95)01207-U

Bayewitch, 1996, (−)-Δ9-Tetrahydrocannabinol antagonizes the peripheral cannabinoid receptor-mediated inhibition of adenylyl cyclase, J. Biol. Chem., 271, 9902, 10.1074/jbc.271.17.9902

Beal, 1995, Dronabinol as a treatment for anorexia associated with weight loss in patients with AIDS, J. Pain Sympt. Manag., 10, 89, 10.1016/0885-3924(94)00117-4

Belue, 1995, The ontogeny of cannabinoid receptors in the brain of postnatal and aging rats, Neurotoxicol. Teratol., 17, 25, 10.1016/0892-0362(94)00053-G

Bidaut-Russell, 1991, Cannabinoid receptor-regulated cyclic AMP accumulation in the rat striatum, J. Neurochem., 57, 1769, 10.1111/j.1471-4159.1991.tb06379.x

Bidaut-Russell, 1990, Cannabinoid receptors and modulation of cyclic AMP accumulation in the rat brain, J. Neurochem., 55, 21, 10.1111/j.1471-4159.1990.tb08815.x

Bouaboula, 1993, Cannabinoid-receptor expression in human leukocytes, Eur. J. Biochem., 214, 173, 10.1111/j.1432-1033.1993.tb17910.x

Bouaboula, 1995, Stimulation of cannabinoid receptor CB1 induces krox-24 expression in human astrocytoma cells, J. Biol. Chem., 270, 13973, 10.1074/jbc.270.23.13973

Bouaboula, 1995, Activation of mitogen-activated protein kinases by stimulation of the central cannabinoid receptor CB1, Biochem. J., 312, 637, 10.1042/bj3120637

Bouaboula, 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, 10.1111/j.1432-1033.1996.0704p.x

Bramblett, 1995, Construction of a 3D model of the cannabinoid CB1 receptor: determination of helix ends and helix orientation, Life Sci., 56, 1971, 10.1016/0024-3205(95)00178-9

Caenazzo, 1991, HindIII identifies a two allele DNA polymorphism of the human cannabinoid receptor gene (CNR), Nucl. Acids Res., 19, 4798, 10.1093/nar/19.17.4798-a

Casiano, 1990, Putative aminoalkylindoles (AAI) antagonists, NIDA Res. Monogr., 105, 295

Caulfield, 1992, Cannabinoid receptor agonists inhibit Ca current in NG108-15 neuroblastoma cells via a pertussis toxin-sensitive mechanism, Br. J. Pharmacol., 106, 231, 10.1111/j.1476-5381.1992.tb14321.x

Chakrabarti, 1995, Cloning and sequencing of a cDNA encoding the mouse brain-type cannabinoid receptor protein, DNA Seq.-J. Seq. Map., 5, 385, 10.3109/10425179509020870

Cheng, 1973, Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction, Biochem. Pharmacol, 22, 3099, 10.1016/0006-2952(73)90196-2

Childers, 1994, Effects of anandamide on cannabinoid receptors in rat brain membranes, Biochem. Pharmacol., 47, 711, 10.1016/0006-2952(94)90134-1

Compton, 1993, Cannabinoid structure-activity relationships: correlation of receptor binding and in vivo activities, J. Pharmacol. Exp. Ther., 265, 218

Compton, 1996, In vivo characterization of a specific cannabinoid receptor antagonist (SR141716A): inhibition of Δ9-tetrahydrocannabinol-induced responses and apparent agonist activity, J. Pharmacol. Exp. Ther., 277, 586

Condie, 1996, Cannabinoid inhibition of adenylate cyclase-mediated signal transduction and interleukin 2 (IL-2) expression in the murine T-cell line, EL4.IL-2, J. Biol. Chem., 271, 13175, 10.1074/jbc.271.22.13175

Coutts, 1996, Effect of cannabinoid agonists and SR141716A on acetylcholine release from the myenteric plexus of the guinea-pig small intestine, Br. J. Pharmacol., 119, 312P

Coutts, 1995, Evidence that guinea-pig small intestine contains CB1 cannabinoid receptors and possibly also a cannabinoid receptor ligand, Br. J. Pharmacol., 116, 46P

Daaka, 1996, Cannabinoid receptor proteins are increased in Jurkat, human T-cell line after mitogen activation, J. Pharmacol. Exp. Ther., 276, 776

Das, 1995, Cannabinoid ligand-receptor signaling in the mouse uterus, Proc. Natl. Acad. Sci. USA, 92, 4332, 10.1073/pnas.92.10.4332

Deadwyler, 1993, Cannabinoids modulate potassium current in cultured hippocampal neurons, Recept. Channels, 1, 121

Deadwyler, 1995, Functional significance of cannabinoid receptors in brain, 205

Deadwyler, 1995, Cannabinoids modulate voltage sensitive potassium A-current in hippocampal neurons via a cAMP-dependent process, J. Pharmacol. Exp. Ther., 273, 734

Deutsch, 1993, Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist, Biochem. Pharmacol., 46, 791, 10.1016/0006-2952(93)90486-G

Devane, 1988, Determination and characterization of a cannabinoid receptor in rat brain, Mol. Pharmacol., 34, 605

Devane, 1992, A novel probe for the cannabinoid receptor, J. Med. Chem., 35, 2065, 10.1021/jm00089a018

Devane, 1992, Isolation and structure of a brain constituent that binds to the cannabinoid receptor, Science, 258, 1946, 10.1126/science.1470919

Dewey, 1986, Cannabinoid pharmacology, Pharmacol. Revs., 38, 151

Diaz, 1993, Suppression of lymphocyte adenosine 3′:5′-cyclic monophosphate (cAMP) by delta-9-tetrahydrocannabinol, Int. J. Immunopharmacol., 15, 523, 10.1016/0192-0561(93)90067-9

Di Marzo, 1995, Arachidonic acid and eicosanoids as targets and effectors in second messenger interactions, Prostaglandins Leukot. Essent. Fatty Acids, 53, 239, 10.1016/0952-3278(95)90123-X

Di Marzo, 1994, Formation and inactivation of endogenous cannabinoid anandamide in central neurons, Nature, 372, 686, 10.1038/372686a0

Di Marzo, 1996, Biosynthesis of anandamide and related acylethanolamides in mouse J774 macrophages and N18 neuroblastoma cells, Biochem. J., 316, 977, 10.1042/bj3160977

Dove Pettit, 1994, Expression of a cannabinoid receptor in baculovirus-infected insect cells, Biochem. Pharmacol., 48, 1231, 10.1016/0006-2952(94)90161-9

Dutta, 1995, The synthesis and pharmacological evaluation of the cannabinoid antagonist SR141716A, Med. Chem. Res., 5, 54

Eissenstat, 1995, Aminoalkylindoles: structure-activity relationships of novel cannabinoid mimetics, J. Med. Chem., 38, 3094, 10.1021/jm00016a013

Evans, 1992, Ca2+-dependent release from rat brain of cannabinoid receptor binding activity, J. Neurochem., 58, 780, 10.1111/j.1471-4159.1992.tb09787.x

Evans, 1994, Endogenous cannabinoid receptor binding activity released from rat brain slices by depolarization, J. Pharmacol. Exp. Ther., 268, 1271

Facci, 1995, Mast cells express a peripheral cannabinoid receptor with differential sensitivity to anandamide and palmitoylethanolamide, Proc. Natl. Acad. Sci. USA, 92, 3376, 10.1073/pnas.92.8.3376

Fahey, 1995, The synthesis and biological activity of a novel class of antagonists for the brain CB1 cannabinoid receptor, Soc. Neurosci. Abstr., 21, 1144

Fan, 1996, Cannabinoid receptor down-regulation without alteration of the inhibitory effect of CP 55,940 on adenylyl cyclase in the cerebellum of CP 55,940-tolerant mice, Brain Res., 706, 13, 10.1016/0006-8993(95)01113-7

Fan, 1995, Cannabinoid agonists inhibit the activation of 5-HT3 receptors in rat nodose ganglion neurons, J. Neurophysiol., 73, 907, 10.1152/jn.1995.73.2.907

Feigenbaum, 1989, Nonpsychotropic cannabinoid acts as a functional N-methyl-D-aspartate receptor blocker, Proc. Natl. Acad. Sci. USA, 86, 9584, 10.1073/pnas.86.23.9584

Felder, 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

Felder, 1993, Anandamide, an endogenous cannabimimetic eicosanoid, binds to the cloned human cannabinoid receptor and stimulates receptor-mediated signal transduction, Proc. Natl. Acad. Sci. USA, 90, 7656, 10.1073/pnas.90.16.7656

Felder, 1995, Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors, Mol. Pharmacol., 48, 443

Felder, 1996, Isolation and measurement of the endogenous cannabinoid receptor agonist, anandamide, in brain and peripheral tissues of human and rat, FEBS Lett., 393, 231, 10.1016/0014-5793(96)00891-5

Fride, 1993, Pharmacological activity of the cannabinoid receptor agonist, anandamide, a brain constituent, Eur. J. Pharmacol., 231, 313, 10.1016/0014-2999(93)90468-W

Fride, 1995, Low doses of anandamides inhibit pharmacological effects of Δ9-tetrahydrocannabinol, J. Pharmacol. Exp. Ther., 272, 699

Galiègue, 1995, Expression of central and peripheral cannabinoid receptors in human immune tissues and leukocyte subpopulations, Eur. J. Biochem., 232, 54, 10.1111/j.1432-1033.1995.tb20780.x

Gaoni, 1964, Isolation, structure and partial synthesis of an active constituent of hashish, J. Am. Chem. Soc., 86, 1646, 10.1021/ja01062a046

Gareau, 1996, Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors, Bioorg. Med. Chem. Lett., 6, 189, 10.1016/0960-894X(95)00573-C

Gérard, 1991, Nucleotide sequence of a human cannabinoid receptor cDNA, Nucl. Acids Res., 18, 7142, 10.1093/nar/18.23.7142

Gérard, 1991, Molecular cloning of a human cannabinoid receptor which is also expressed in testis, Biochem. J., 279, 129, 10.1042/bj2790129

Gifford, 1996, Electrically evoked acetylcholine release from hippocampal slices is inhibited by the cannabinoid receptor agonist, WIN 55212-2, and is potentiated by the cannabinoid antagonist, SR 141716A, J. Pharmacol. Exp. Ther., 277, 1431

Glass, 1995, Induction of the Krox 24 transcription factor in striosomes by a cannabinoid agonist, Neuroreport, 6, 241, 10.1097/00001756-199501000-00004

Glass, 1993, Loss of cannabinoid receptors in the substantia nigra in Huntington's disease, Neuroscience, 56, 523, 10.1016/0306-4522(93)90352-G

Gold, 1992, A comparison of the discriminative stimulus properties of Δ9-tetrahydrocannabinol and CP 55,940 in rats and rhesus monkeys, J. Pharmacol. Exp. Ther., 262, 479

Hampson, 1995, Anandamide hydroxylation by brain lipoxygenase: metabolite structures and potencies at the cannabinoid receptor, Biochim. Biophys. Acta, 1259, 173, 10.1016/0005-2760(95)00157-8

Hanuš, 1993, Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor, J. Med. Chem., 36, 3032, 10.1021/jm00072a026

Henry, 1995, Activation of inwardly rectifying potassium channels (GIRK1) by co-expressed rat brain cannabinoid receptors in Xenopus oocytes, Neurosci. Lett., 186, 91, 10.1016/0304-3940(95)11289-9

Herkenham, 1995, Localization of cannabinoid receptors in brain and periphery, 145

Herkenham, 1990, Cannabinoid receptor localization in brain, Proc. Natl. Acad. Sci. USA, 87, 1932, 10.1073/pnas.87.5.1932

Herkenham, 1991, Neuronal localization of cannabinoid receptors and second messengers in mutant mouse cerebellum, Brain Res., 552, 301, 10.1016/0006-8993(91)90096-E

Herkenham, 1991, Neuronal localization of cannabinoid receptors in the basal ganglia of the rat, Brain Res., 547, 267, 10.1016/0006-8993(91)90970-7

Herkenham, 1991, Characterization and localization of cannabinoid receptors in rat brain: a quantitative in vitro autoradiographic study, J. Neurosci., 11, 563, 10.1523/JNEUROSCI.11-02-00563.1991

Hillard, 1995, Characterization of ligand binding to the cannabinoid receptor of rat brain membranes using a novel method: application to anandamide, J. Neurochem., 64, 677, 10.1046/j.1471-4159.1995.64020677.x

Hillard, 1995, Characterization of the kinetics and distribution of N-arachidonylethanolamine (anandamide) hydrolysis by rat brain, Biochim. Biophys. Acta, 1257, 249, 10.1016/0005-2760(95)00087-S

Hirst, 1995, Do SH-SY5Y human neuroblastoma cells express cannabinoid receptors?, Biochem. Soc. Trans., 23, 418S, 10.1042/bst023418s

Ho, 1996, Determination of the cannabinoid receptors in mouse x rat hybridoma NG108-15 cells and rat GH4C1 cells, Neurosci. Lett., 212, 123, 10.1016/0304-3940(96)12792-0

Hoehe, 1991, Genetic and physical mapping of the human cannabinoid receptor gene to chromosome-6q14-q15, New Biol., 3, 880

Hollister, 1986, Health aspects of cannabis, Pharmacol. Rev., 38, 1

Holsapple, 1996, Molecular mechanisms of toxicant-induced immunosuppression: role of second messengers, Annu. Rev. Pharmacol. Toxicol., 36, 131, 10.1146/annurev.pa.36.040196.001023

Hong, 1996, Inhibition of neuromuscular transmission in the myenteric plexus of guinea-pig ileum by ω-conotoxins GVIA, MVIIA, MVIIC and SVIB, Br. J. Pharmacol., 118, 797, 10.1111/j.1476-5381.1996.tb15470.x

Houston, 1993, Solubilization of the cannabinoid receptor from rat brain and its functional interaction with guanine nucleotide-binding proteins, Mol. Pharmacol., 43, 17

Howlett, 1984, Inhibition of neuroblastoma adenylate cyclase by cannabinoid and nantradol compounds, Life Sci., 35, 1803, 10.1016/0024-3205(84)90278-9

Howlett, 1985, Cannabinoid inhibition of adenylate cyclase. Biochemistry of the response in neuroblastoma cell membranes, Mol. Pharmacol., 27, 429

Howlett, 1987, Cannabinoid inhibition of adenylate cyclase: relative activity of constituents and metabolites of marihuana, Neuropharmacology, 26, 507, 10.1016/0028-3908(87)90035-9

Howlett, 1995, Pharmacology of cannabinoid receptors, Annu. Rev. Pharmacol. Toxicol., 33, 607, 10.1146/annurev.pa.35.040195.003135

Howlett, 1995, Cannabinoid compounds and signal transduction mechanisms, 167

Howlett, 1984, Cannabinoid inhibition of adenylate cyclase. Pharmacology of the response in neuroblastoma cell membranes, Mol. Pharmacol., 26, 532

Howlett, 1986, Involvement of G1 in the inhibition of adenylate cyclase by cannabimimetic drugs, Mol. Pharmacol., 29, 307

Howlett, 1988, Nonclassical cannabinoid analgetics inhibit adenylate cyclase: development of a cannabinoid receptor model, Mol. Pharmacol., 33, 297

Howlett, 1990, Stereochemical effects of 11-OH-Δ8-tetrahydro-cannabinol-dimethylheptyl to inhibit adenylate cyclase and bind to the cannabinoid receptor, Neuropharmacology, 29, 161, 10.1016/0028-3908(90)90056-W

Howlett, 1992, The cannabinoid receptor, 35

Huffman, 1996, Recent developments in the medicinal chemistry of cannabinoids, Curr. Med. Chem., 3, 101, 10.2174/092986730302220302094839

Huffman, 1994, Design, synthesis and pharmacology of cannabimimetic indoles, Bioorg. Med. Chem. Lett., 4, 563, 10.1016/S0960-894X(01)80155-4

Huffman, 1996, Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor, J. Med. Chem., 39, 3875, 10.1021/jm960394y

Ishac, 1996, Inhibition of exocytotic noradrenaline release by presynaptic cannabinoid CB1 receptors on peripheral sympathetic nerves, Br. J. Pharmacol., 118, 2023, 10.1111/j.1476-5381.1996.tb15639.x

Jansen, 1992, Distribution of cannabinoid receptors in rat brain determined with aminoalkylindoles, Brain Res., 575, 93, 10.1016/0006-8993(92)90428-C

Järbe, 1993, Discriminative stimulus effects and receptors binding of enantiomeric pairs of cannabinoids in rats and pigeons; a comparison, J. Pharmacol. Exp. Ther., 264, 561

Johnson, 1986, The discovery of non-classical cannabinoid analgetics, 121

Kaminski, 1992, Identification of a functionally relevant cannabinoid receptor on mouse spleen cells that is involved in cannabinoid-mediated immune modulation, Mol. Pharmacol., 42, 736

Kaminski, 1994, Suppression of the humoral immune response by cannabinoids is partially mediated through inhibition of adenylate cyclase by a pertussis toxin-sensitive G-protein coupled mechanism, Biochem. Pharmacol., 48, 1899, 10.1016/0006-2952(94)90588-6

Kenakin, 1993

Koutek, 1994, Inhibitors of arachidonoyl ethanolamide hydrolysis, J. Biol. Chem., 269, 22937, 10.1016/S0021-9258(17)31599-5

Kuster, 1993, Aminoalkylindole binding in rat cerebellum: selective displacement by natural and synthetic cannabinoids, J. Pharmacol. Exp. Ther., 264, 1352

Lainton, 1995, 1-Alkyl-3-(1-naphthoyl)pyrroles: a new class of cannabinoid, Tetrahedron Lett., 36, 1401, 10.1016/0040-4039(95)00016-6

Lee, 1995, Effects of putative cannabinoid receptor ligands, anandamide and 2-arachidonyl-glycerol, on immune function in B6C3F1 mouse splenocytes, J. Pharmacol. Exp. Ther., 275, 529

Lu, 1993, Roles of sulfhydryl and disulfide groups in the binding of CP-55,940 to rat brain cannabinoid receptor, Mol. Cell. Biochem., 121, 119, 10.1007/BF00925970

Lynn, 1994, Localization of cannabinoid receptors and nonsaturable high-density cannabinoid binding sites in peripheral tissues of the rat-implications for receptor-mediated immune modulation by cannabinoids, J. Pharmacol. Exp. Ther., 268, 1612

Mackie, 1992, Cannabinoids inhibit N-type calcium channels in neuroblastoma-glioma cells, Proc. Natl. Acad. Sci. USA, 89, 3825, 10.1073/pnas.89.9.3825

Mackie, 1993, Anandamide, an endogenous cannabinoid, inhibits calcium currents as a partial agonist in N18 neuroblastoma cells, Mol. Pharmacol., 44, 498

Mackie, 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, 10.1523/JNEUROSCI.15-10-06552.1995

Mailleux, 1992, Distribution of neuronal cannabinoid receptor in the adult rat brain: a comparative receptor binding radioautography and in situ hybridization histochemistry, Neuroscience, 48, 655, 10.1016/0306-4522(92)90409-U

Mailleux, 1992, Localization of cannabinoid receptor in the human developing and adult basal ganglia. Higher levels in the striatonigral neurons, Neurosci. Lett., 148, 173, 10.1016/0304-3940(92)90832-R

Mailleux, 1992, Initial observations on the distribution of cannabinoid receptor binding sites in the human adult basal ganglia using autoradiography, Neurosci. Lett., 139, 7, 10.1016/0304-3940(92)90845-X

Makriyannis, 1995, The role of cell membranes in cannabinoid activity, 87

Maneuf, 1996, Activation of the cannabinoid receptor by Δ9-tetrahydrocannabinol reduces γ-aminobutyric acid uptake in the globus pallidus, Eur. J. Pharmacol., 308, 161, 10.1016/0014-2999(96)00326-3

Mansbach, 1996, Effects of the cannabinoid CB1 receptor antagonist SR141716A on the behavior of pigeons and rats, Psychopharmacology, 124, 315, 10.1007/BF02247436

Martin, 1991, Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs, Pharmacol. Biochem. Behav., 40, 471, 10.1016/0091-3057(91)90349-7

Martin, 1995, Pharmacological evaluation of dimethylheptyl analogs of delta-9-THC: reassessment of the putative three-point cannabinoid-receptor interaction, Drug Alcohol Depend., 37, 231, 10.1016/0376-8716(94)01081-U

Martin, 1995, Structural requirements for cannabinoid receptor probes, 35

Matsuda, 1995, Molecular biology of the cannabinoid receptor, 117

Matsuda, 1990, Structure of a cannabinoid receptor and functional expression of the cloned cDNA, Nature, 346, 561, 10.1038/346561a0

McLaughlin, 1994, Cannabinoid receptors in developing rats: detection of mRNA and receptor binding, Drug Alcohol Depend., 36, 27, 10.1016/0376-8716(94)90006-X

Mechoulam, 1995, The unpaved road to the endogenous brain cannabinoid ligands, the anandamides, 233

Mechoulam, 1992, Cannabinoid geometry and biological activity, 1

Mechoulam, 1995, Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors, Biochem. Pharmacol., 50, 83, 10.1016/0006-2952(95)00109-D

Melvin, 1993, Structure-activity relationships for cannabinoid receptor-binding and analgesic activity: studies of bicyclic cannabinoid analogs, Mol. Pharmacol., 44, 1008

Milligan, 1995, Inverse agonism: pharmacological curiosity or potential therapeutic strategy?, Trends Pharmacol. Sci., 16, 10, 10.1016/S0165-6147(00)88963-4

Munro, 1993, Molecular characterization of a peripheral receptor for cannabinoids, Nature, 365, 61, 10.1038/365061a0

Nah, 1993, Cannabinoids inhibit agonist-stimulated formation of inositol phosphates in rat hippocampal cultures, Eur. J. Pharmacol. Mol. Pharmacol. Sect., 246, 19, 10.1016/0922-4106(93)90004-S

Okada, 1992, The facilitating and suppressing effects of Δ9-tetrahydrocannabinol on the rise in intrasynaptosomal Ca2+ concentration in rats, Neurosci. Lett., 140, 55, 10.1016/0304-3940(92)90680-6

Onaivi, 1996, Cannabinoid receptor genes, Prog. Neurobiol., 48, 275, 10.1016/0301-0082(95)00044-5

Onaivi, 1996, Neurobehavioral effects of Δ9-THC and cannabinoid (CB1) receptor gene expression in mice, Behav. Brain Res., 72, 115, 10.1016/0166-4328(96)00139-8

Oviedo, 1993, Chronic cannabinoid administration alters cannabinoid receptor binding in rat brain: a quantitative autoradiographic study, Brain Res., 616, 293, 10.1016/0006-8993(93)90220-H

Pacheco, 1991, Aminoalkylindoles: actions on specific G-protein-linked receptors, J. Pharmacol. Exp. Ther., 257, 170

Pacheco, 1993, Identification of cannabinoid receptors in cultures of rat cerebellar granule cells, Brain Res., 603, 102, 10.1016/0006-8993(93)91304-B

Pacheco, 1994, Differential requirements of sodium for coupling of cannabinoid receptors to adenylyl cyclase in rat brain membranes, J. Neurochem., 62, 1773, 10.1046/j.1471-4159.1994.62051773.x

Pan, 1996, Rat brain cannabinoid receptor modulates N-type Ca2+ channels in a neuronal expression system, Mol. Pharmacol., 49, 707

Paria, 1995, The preimplantation mouse embryo is a target for cannabinoid ligand-receptor signaling, Proc. Natl. Acad. Sci. USA, 92, 9460, 10.1073/pnas.92.21.9460

Paterson, 1993, Characterization of the cannabinoid binding site in the guinea-pig, Br. J. Pharmacol., 109, 82P

Pério, 1996, Central mediation of the cannabinoid cue: activity of a selective CB1 antagonist, SR 141716A, Behav. Pharmacol., 7, 65

Pertwee, 1988, The central neuropharmacology of psychotropic cannabinoids, Pharmacol. Ther., 36, 189, 10.1016/0163-7258(88)90106-4

Pertwee, 1991, Tolerance to and dependence on psychotropic cannabinoids, 231

Pertwee, 1993, The evidence for the existence of cannabinoid receptors, Gen. Pharmacol., 24, 811, 10.1016/0306-3623(93)90154-P

Pertwee, 1995, Pharmacological, physiological and clinical implications of the discovery of cannabinoid receptors: an overview, 1

Pertwee, 1996, Evidence for the presence of cannabinoid CB1 receptors in mouse urinary bladder, Br. J. Pharmacol., 118, 2053, 10.1111/j.1476-5381.1996.tb15643.x

Pertwee, 1995, A preliminary investigation of the mechanisms underlying cannabinoid tolerance in the mouse vas deferens, Eur. J. Pharmacol., 272, 67, 10.1016/0014-2999(94)00617-G

Pertwee, 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, 10.1111/j.1476-5381.1992.tb09088.x

Pertwee, 1993, In vitro effects of the cannabinoid, CP 55,940, and of its (+)-enantiomer, CP 56,667, 374

Pertwee, 1994, Effects of two endogenous fatty acid ethanolamides on mouse vasa deferentia, Eur. J. Pharmacol., 259, 115, 10.1016/0014-2999(94)90499-5

Pertwee, 1995, Effect of phenylmethylsulphonyl fluoride on the potency of anandamide as an inhibitor of electrically evoked contractions in two isolated tissue preparations, Eur. J. Pharmacol., 272, 73, 10.1016/0014-2999(94)00618-H

Pertwee, 1995, AM630, a competitive cannabinoid receptor antagonist, Life Sci., 56, 1949, 10.1016/0024-3205(95)00175-6

Pertwee, 1995, Pharmacological characterization of three novel cannabinoid receptor agonists in the mouse isolated vas deferens, Eur. J. Pharmacol., 284, 241, 10.1016/0014-2999(95)00318-F

Pertwee, 1996, Agonist-antagonist characterization of 6′-cyanohex-2′-yne-Δ8-tetrahydro-cannabinol in two isolated tissue preparations, Eur. J. Pharmacol., 315, 195, 10.1016/S0014-2999(96)00631-0

Pertwee, 1996, Further evidence for the presence of cannabinoid CB1 receptors in guinea-pig small intestine, Br. J. Pharmacol., 118, 2199, 10.1111/j.1476-5381.1996.tb15663.x

Pertwee, 1996, Further evidence for the presence of cannabinoid CB1 receptors in mouse vas deferens, Eur. J. Pharmacol., 296, 169, 10.1016/0014-2999(95)00790-3

Petitet, 1996, Biochemical and pharmacological characterization of cannabinoid binding sites using [3H]SR141716A, Neuroreport, 7, 789, 10.1097/00001756-199602290-00026

Pinto, 1994, Cannabinoid receptor binding and agonist activity of amides and esters of arachidonic acid, Mol. Pharmacol., 46, 516

Priller, 1995, Mead ethanolamide, a novel eicosanoid, is an agonist for the central (CB1) and peripheral (CB2) cannabinoid receptors, Mol. Pharmacol., 48, 288

Pugh, 1994, Modulation of free intracellular calcium and cAMP by morphine and cannabinoids, alone and in combination in mouse brain and spinal cord synaptosomes, Pharmacol. Biochem. Behav., 49, 1093, 10.1016/0091-3057(94)90270-4

Razdan, 1986, Structure-activity relationships in cannabinoids, Pharmacol. Revs., 38, 75

Reche, 1996, A role for central cannabinoid and opioid systems in peripheral Δ9-tetrahydrocannabinol-induced analgesia in mice, Eur. J. Pharmacol., 301, 75, 10.1016/0014-2999(96)00045-3

Reichman, 1991, Δ9-Tetrahydrocannabinol inhibits arachidonic acid acylation of phospholipids and triacylglycerols in guinea pig cerebral cortex slices, Mol. Pharmacol., 40, 547

Richfield, 1994, Selective vulnerability in Huntington's disease: preferential loss of cannabinoid receptors in lateral globus pallidus, Ann. Neurol., 36, 577, 10.1002/ana.410360406

Rinaldi-Carmona, 1994, SR141716A, a potent and selective antagonist of the brain cannabinoid receptor, FEBS Lett., 350, 240, 10.1016/0014-5793(94)00773-X

Rinaldi-Carmona, 1996, Characterization and distribution of binding sites for [3H]-SR141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain, Life Sci., 58, 1239, 10.1016/0024-3205(96)00085-9

Rodríguez de Fonseca, 1993, Presence of cannabinoid binding sites in the brain from early postnatal ages, Neuroreport, 4, 135, 10.1097/00001756-199302000-00005

Rodríguez de Fonseca, 1994, Downregulation of rat brain cannabinoid binding sites after chronic Δ9-tetrahydrocannabinol treatment, Pharmacol. Biochem. Behav., 47, 33, 10.1016/0091-3057(94)90108-2

Romero, 1995, Changes in rat brain cannabinoid binding sites after acute or chronic exposure to their endogenous agonist, anandamide, or to Δ9-tetrahydrocannabinol, Pharmacol. Biochem. Behav., 51, 731, 10.1016/0091-3057(95)00023-P

Rowley, 1990, Tetrahydrocannabinol inhibits adenyl cyclase in human leukemia cells, Life Sci., 46, 217, 10.1016/0024-3205(90)90107-3

Rubino, 1994, Chronic CP-55,940 alters cannabinoid receptor mRNA in the rat brain: an in situ hybridization study, Neuroreport, 5, 2493, 10.1097/00001756-199412000-00022

Santucci, 1996, Arousal-enhancing properties of the CB1 cannabinoid receptor antagonist SR141716A in rats as assessed by electroencephalographic spectral and sleep-waking cycle analysis, Life Sci., 58, PL103, 10.1016/0024-3205(95)02319-4

Schatz, 1992, Inhibition of adenylate cyclase by Δ9-tetrahydrocannabinol in mouse spleen cells: a potential mechanism for cannabinoid-mediated immunosuppression, Life Sci., 51, 25, 10.1016/0024-3205(92)90414-K

Selley, 1993, Modification of G protein-coupled functions by low-pH pretreatment of membranes from NG108-15 cells: increase in opioid agonist efficacy by decreased inactivation of G proteins, Mol. Pharmacol., 44, 731

Selley, 1996, Cannabinoid receptor stimulation of guanosine-5′-O-(3-[35S]thio) triphosphate binding in rat brain membranes, Life Sci., 59, 659, 10.1016/0024-3205(96)00347-5

Shire, 1995, An amino-terminal variant of the central cannabinoid receptor resulting from alternative splicing, J. Biol. Chem., 270, 3726, 10.1074/jbc.270.8.3726

Shire, 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, 10.1074/jbc.271.12.6941

Shire, 1996, Molecular cloning, expression and function of murine CB2 peripheral cannabinoid receptor, Biochim. Biophys. Acta, 1307, 132, 10.1016/0167-4781(96)00047-4

Shivachar, 1996, Anandamide- and Δ9-tetrahydrocannabinol-evoked arachidonic acid mobilization and blockade by SR141716A [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboximide hydrochloride], Biochem. Pharmacol., 51, 669, 10.1016/S0006-2952(95)02248-1

Shohami, 1995, Long-term effect of HU-211, a novel non-competitive NMDA antagonist, on motor and memory functions after closed head injury in the rat, Brain Res., 674, 55, 10.1016/0006-8993(94)01433-I

Showalter, 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

Sim, 1995, In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5′-[γ-[35S]thiol-triphosphate binding, Proc. Natl. Acad. Sci. USA, 92, 7242, 10.1073/pnas.92.16.7242

Sim, 1996, Differences in G-protein activation by μ- and δ-opioid, and cannabinoid receptors in rat striatum, Eur. J. Pharmacol., 307, 97, 10.1016/0014-2999(96)00211-7

Slipetz, 1995, Activation of the human peripheral cannabinoid receptor results in inhibition of adenylyl cyclase, Mol. Pharmacol., 48, 352

Song, 1996, A lysine residue of the cannabinoid receptor is critical for receptor recognition by several agonists but not WIN 55212-2, Mol. Pharmacol., 49, 891

Stubbs, 1996, The gene encoding the central cannabinoid receptor is located in proximal mouse Chromosome 4, Mamm. Genome, 7, 165, 10.1007/s003359900043

Sugiura, 1995, 2-Arachidonoyl-glycerol: a possible endogenous cannabinoid receptor ligand in brain, Biochem. Biophys. Res. Commun., 215, 89, 10.1006/bbrc.1995.2437

Terranova, 1996, Improvement of memory in rodents by the selective CB1 cannabinoid receptor antagonist, SR 141716, Psychopharmacology, 126, 165, 10.1007/BF02246352

Thomas, 1992, Characterization and autoradiographic localization of the cannabinoid binding site in rat brain using [3H]11-OH-Δ9-THC-DMH, J. Pharmacol. Exp. Ther., 263, 1383

Thomas, 1996, Structure-activity analysis of anandamide analogs: relationship to a cannabinoid pharmacophore, J. Med. Chem., 39, 471, 10.1021/jm9505167

Turkanis, 1991, Differential effects of delta-9-tetrahydrocannabinol and its 11-hydroxy metabolite on sodium current in neuroblastoma cells, Brain Res., 560, 245, 10.1016/0006-8993(91)91239-W

Turkanis, 1991, Delta-9-tetrahydrocannabinol depresses inward sodium current in mouse neuroblastoma cells, Neuropharmacology, 30, 73, 10.1016/0028-3908(91)90045-D

Vogel, 1993, Anandamide, a brain endogenous compound, interacts specifically with cannabinoid receptors and inhibits adenylate cyclase, J. Neurochem., 61, 352, 10.1111/j.1471-4159.1993.tb03576.x

Wartmann, 1995, The MAP kinase signal transduction pathway is activated by the endogenous cannabinoid anandamide, FEBS Lett., 359, 133, 10.1016/0014-5793(95)00027-7

Waterman, 1996, Multiple subtypes of voltage-gated calcium channel mediate transmitter release from parasympathetic neurons in the mouse bladder, J. Neurosci., 16, 4155, 10.1523/JNEUROSCI.16-13-04155.1996

Westlake, 1994, Cannabinoid receptor binding and messenger RNA expression in human brain: an in vitro receptor autoradiography and in situ hybridization histochemistry study of normal aged and Alzheimer's brains, Neuroscience, 63, 637, 10.1016/0306-4522(94)90511-8

Wiley, 1995, Discriminative stimulus effects of anandamide in rats, Eur. J. Pharmacol., 276, 49, 10.1016/0014-2999(95)00010-I

Wiley, 1995, Discriminative stimulus effects of CP 55,940 and structurally dissimilar cannabinoids in rats, Neuropharmacology, 34, 669, 10.1016/0028-3908(95)00027-4

Wiley, 1995, Pharmacological specificity of the discriminative stimulus effects of Δ9-tetrahydrocannabinol in rhesus monkeys, Drug Alcohol Depend., 40, 81, 10.1016/0376-8716(95)01193-5

Wiley, 1995, Antagonism of the discriminative stimulus effects of Δ9-tetrahydrocannabinol in rats and rhesus monkeys, J. Pharmacol. Exp. Ther., 275, 1

Wise, 1996, Synthesis and cannabinoid receptor binding activity of conjugated triene anandamide, a novel eicosanoid, Experientia, 52, 88, 10.1007/BF01922423

Wright, 1996, Effects of N-, P- and Q-type neuronal calcium channel antagonists on mammalian peripheral neurotransmission, Br. J. Pharmacol., 119, 49, 10.1111/j.1476-5381.1996.tb15676.x

Xie, 1995, Common cannabimimetic pharmacophoric requirements between aminoalkyl indoles and classical cannabinoids, Life Sci., 56, 1963, 10.1016/0024-3205(95)00177-8

Xie, 1996, The conformational properties of the highly selective cannabinoid receptor ligand CP-55,940, J. Biol. Chem., 271, 10640, 10.1074/jbc.271.18.10640

Zitko, 1972, Water-soluble derivatives of Δ1-tetrahydrocannabinol, Science, 177, 442, 10.1126/science.177.4047.442