Antagonist cannabinoid receptor

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. 

Sanofi-Synthelabo researchers discovered pyrazole 53 and analogs to have potent Cannabinoid receptor-1 (CB-1) antagonist/inverse agonist activity and have progressed 53 into development for treatment of obesity and alcohol dependence. The synthesis of 53 was accomplished by heating the diketone sodium salt 51 with the aryl hydrazine hydrochloride in acetic acid to provide the intermediate 52, which was further derivatized... 

Aceto MD, Scares SM, Lowe JA, et al Cannabinoid precipitated withdrawal by the selective cannabinoid receptor antagonist, SR 141716A. Eur J Pharmacol 282 R1-R2, 1995... 

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... 

Teesson M, Lynskey M, Manor B, et al The psychometric properties of BSM-IV cannabis use disorders. Brug Alcohol Bepend 68 235—262, 2002 Tsou K, Patrick SL, Walker JM. Physical withdrawal in rats tolerant to delta 9-tetrahydrocannabinol precipitated by a cannabinoid receptor antagonist. Eur J Pharmacol 280 R13-R15, 1995... 

Mouse vas deferens (MVD) seems to express CB1 and at least one CB2-like cannabinoid receptor type, as is demonstrated by the presence of CB1 and CB2-like mRNA as well as by data collected from experiments with cannabinoid receptor selective agonists and antagonists (Pertwee, 1999). Furthermore, evidence indicates that a CBl-like receptor exists in vascular endothelium, which upon activation produces significant hypotension (Wagner, 1999). This receptor differs from CB1 in its pharmacological response to some well-characterized cannabimimetics. 

Pertwee RG, Griffin G, Fernando SR, Li X, Hill A, Makriyannis A. AM630, a competitive cannabinoid receptor antagonist. Life Sci 1995c 56 1949-1955. 

Rinaldi-Carmona M, Bath F, Heaulme M, Shire D, Calandra B, Congy C, Martinez S, Maruani J, Neliat G, Caput D, Ferrara P, Soubrie P, Breliere JC, Lefur G. SR14176A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994 350 240-244. 

Our development of [123I]AM281, an antagonist radioligand for brain cannabinoid receptors, has allowed us to image this receptor for the first time in vivo. Ex vivo autoradiographic experiments have been conducted in rodents, and SPECT studies have been conducted in baboons. Research... 

JC, Lefur G. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 1994 350 240-244. 

Lan R, Liu Q, Fan P, Lin S, Fernando SR, McCallion D, Pertwee R, Makriyannis A. Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J Med Chem 1999 42 769-776. 

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. 

Vinklerova, J., Novakova, J., Sulcova, A. Inhibition of methamphetamine self-administration in rats by cannabinoid receptor antagonist AM 251. J. Psychopharmacol. 16 139, 2002. 

Hodos W (1961) Progressive ratio as a measure of reward strength. Science 134 943-944 Huestis MA, GoreUck DA, Heishman SJ, Preston KL, Nelson RA, Moolchan ET, Frank RA (2001) Blockade of effects of smoked marijuana by the CB 1-selective cannabinoid receptor antagonist SR141716. Arch Gen Psychiatry 58 322-328... 

Black SC (2004) Cannabinoid receptor antagonists and obesity. Curr Opin Investig Drugs 5 389-394... 

Huestis, M.A. (2001, April) Blockade of Effects of Smoked Marijuana by the CB1-Selective Cannabinoid Receptor Antagonist SR141716. Jouma/ Archives of General Psychiatry 58 (4) 322-328. http //archpsyc.ama-assn.org/cgi/conieni/absiract/58/4/322 (for abstract)... 

---