Cannabinoid antagonist

As discussed earlier, SR171614A, a selective cannabinoid antagonist that is highly competitive at CB1 binding sites, has been identified and synthesi2ed. 

Devane WA, Dysarz FA, Johnson MR, et al Determination and characterization of a cannabinoid receptor in rat brain. Mol Pharmacol 34 605—613, 1988 D Souza DC, Kosten TR Cannabinoid antagonists a treatment in search of an illness. Arch Gen Psychiatry 58 330—331,2001... 

Collins DR, Pertwee RG, Davies SN. Prevention by the cannabinoid antagonist, SR141716A, of cannabinoid-mediated blockade of long-term potentiation in the rat hippocampal slice. Br J Pharmacol 1995 115 869-870. 

Gifford AN, Ashby CR. 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 1996 277 1431-1436. 

Lichtman AH, Martin BR. (1997). The selective cannabinoid antagonist SR 141716A blocks cannabinoid-induced antinociception in rats. Pharmacol Biochem Behav. 57(1-2) 7-12. 

Colombo G, Agabio R, Diaz G, Lobina C, Reali R, Gessa GL. (1998). Appetite suppression and weight loss after the cannabinoid antagonist SR 141716. Life Sci. 63(8) PL113-17. 

Zickler, P. (2002). Cannabinoid Antagonist Reduces Marijuana s Effects in Humans. NIDA Notes 17 (3). http //www.drugabuse.gov/NIDA notes/NNVol17N3/ Cannabinoid.html)... 

Cannabinoid antagonists. Cannabinoid receptors are discussed in further detail in Chapter 13 on drug abuse. An antagonist to cannabinoid 1 (CB1) receptors, SR141716A, reduces the activity of mesolimbic dopamine neurons in animal models, suggesting possible antipsychotic actions in schizophrenia and leading to testing in schizophrenic patients. 

Takahashi KA, Castillo PE (2006) The CB1 cannabinoid receptor mediates glutamatergic synaptic suppression in the hippocampus. Neurosci 139(3) 795-802 Takahashi RN, Pamplona FA, Fernandes MS (2005) The cannabinoid antagonist SR141716A facilitates memory acquisition and consolidation in the mouse elevated T-maze. Neurosci Lett 380(3) 270-75... 

Murineddu, G., Ruiu, S., Loriga, G., Manca, 1., Lazzari, R, ReaU, R., Pani, L., Toma, L., Pinna, G. A. Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-l-(2, 4 -dichlorophenyl)-iV-piperidin-l-yl-l,4,5,6-tetrahydrobenzo [6,7]cyclohepta[l,2-c]pyrazole-3-carboxamide. J. Med. Chem. 2005, 4S(23), 7351-7362. 

Lan R, Gatley J, Lu Q, Fan P, Fernando SR, Volkow ND, Pertwee R, Makriyannis A (1999a) Design and synthesis of the CBl selective cannabinoid antagonist AM281 a potential human SPECT ligand. AAPS PharmSci 1 U13-U24... 

Barth F, Rinaldi-Carmona M (1999) The development of cannabinoid antagonists. Curr Med Chem 6 745-755... 

Batkai S, Pacher P, Jarai Z, Wagner JA, Kunos G (2004) Cannabinoid antagonist SR-141716 inhibits endotoxic hypotension by a cardiac mechanism not involving CBi or CB2 receptors. Am J Physiol Heart Circ Physiol 287 H595-H600... 

Aventis reported (Mignani et al. 2000) a new class of CBi receptor antagonists, which are represented by the diarylmethyleneazetidine analog 64 (Fig. 18). Very recently some novel 1,2,4-triazole derivatives were shown to behave as silent cannabinoid antagonists (Jagerovic et al. 2004). Although, these compounds bind... 

Jagerovic N, Hernandez-Folgado L, Alkorta I, Goya P, Navarro M, Serrano A, Rodriguez de Fonseca F, Dannert MT, Alsasua A, Suardiaz M, Pascual D, Martin MI (2004) Discovery of 5-(4-chlorophenyl)- l-(2,4-dichlorophenyl)-3-hexyl-lH-l,2,4-triazole, a novel in vivo cannabinoid antagonist containing a 1,2,4-triazole motif. J Med Chem 47 2939-2942... 

Pertwee R, Griffin G, Fernando S, Li X, HiU A, Makriyannis A (1995) AM630, a competitive cannabinoid antagonist. Life Sci 56 1949-1955... 

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