Receptors cannabinoid

Cannabinoid receptor Cannabis sativa Canna indica Canned foods... 

Gannabinoids. Like the BZ receptor, the cannabinoid receptor was initially identified using psychotropic alkaloids such as A -tetrahydrocannabinol (A-THC) (78) that were known to affect mammalian CNS function (see PsYCHOPHARMACOLOGiCALAGENTs). The CNS receptor,... 

CB, was identified by radioligand binding techniques and subsequently cloned. A second receptor subclass, CB2, has been identified in human spleen and also has been cloned (34). Table 5 Hsts cannabinoid receptor ligands. 

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... 

Bouaboula, M., Perrachon, S., Milligan, L., Canatt, X., Rinaldi-Carmona, M., Portier, M., Barth, F., Calandra, B., Pecceu, F., Lupker, J., Maffrand, J.-P., Le Fur, G., and Casellas, P. (1997). A selective inverse agonist for central cannabinoid receptor inhibits mitogen-activated protein kinase activation stimulated by insulin or insulin-like growth factor. J. Biol. Ckem. 272 22330-22339. 

A natural sythesised cannabinoid interacting with the cannabinoid receptor I and II. In addition, anandamide blocks receptor-independent all LVA-calcium channels. 

Group of compounds which naturally occur in the hemp plant, Cannabis saiiva. Most of them are unsoluble in water. The most abundant cannabinoids are A9--tetrahydrocannabinol (THC), its precursor cannabidiol and cannabinol, which is formed spontaneously from THC. Cannabinoids exert their effects through G-protein coupled cannabinoid receptors (CBi/CB2). 

Endogenous cannabinoids Endogenous agonists of cannabinoid receptors... 

Endocannabinoids are endogenous mediators acting via the binding to, and activation of, cannabinoid receptors, CBX and CB2 [1]. iV-arachidonoy 1-ethanol-amine (AEA, anandamide) and 2-arachidonoyl-glycerol (2-AG) (Fig. 1) are the two most studied endocannabinoids. In the nervous system, endocannabinoids act as... 

Based on the role of endocannabinoids and cannabinoid receptors in several pathological conditions, the pharmacological manipulation of their levels or action is being developed as a therapeutic strategy. Enhancement of endocannabinoid signalling when this plays uniquely a protective role can be effected in a safer way using (i) cannabis extracts in which the presence of non-psychotropic cannabinoids with therapeutic activity per... 

Howlett AC (2005) Cannabinoid receptor signaling. Handb Exp Pharmacol 168 53-79... 

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... 

Braida D, Pozzi M, Cavallini R, et al Intracerebral self-administration of the cannabinoid receptor agonist CP 55,940 in the rat interaction with the opioid system. EurJ Pharmacol 413 227-234, 2001... 

Cheer JF, Kendall DA, Marsden CA Cannabinoid receptors and reward in the rat a conditioned place preference study. Psychopharmacology (Berl) 151 25-30,2000... 

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... 

Johnston LD, O Malley PM, Bachman JG, et al Monitoring the Future National Results on Adolescent Drug Use Overview of Key Findings, 2003 (NIH Publ No 04—3506). Bethesda, MD National Institute on Drug Abuse, 2004 Jorda MA, Rayman N, Valk P, et al Identification, characterization, and function of a novel oncogene the peripheral cannabinoid receptor Cb2. Ann N Y Acad Sci 996 10-16, 2003... 

Martellotta MC, Cossu G, Fattore L, et al Self-administration of the cannabinoid receptor agonist WIN 55,212—2 in drug-naive mice. Neuroscience 85 327—330, 1998... 

Matsuda LA, Lolait SJ, Brownstein MJ, et al Structure of a cannabinoid receptor and functional expression of the cloned cDNA. Nature 364 561—564, 1990... 

Nowell KW, Pettit DA, Cabral WA, et al High-level expression of the human CB2 cannabinoid receptor using a baculovirus system. Biochem Pharmacol 55 1893— 1905, 1998... 

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... 

CP-55,940 (8.5) was developed during the search for novel analgesics [146]. Although it is more potent than morphine it was never approved. Nevertheless, in its tritium-labeled form it became a very important tool for research and helped in the first identification of the cannabinoid receptor. 

In the search for new anti-inflammatory drugs structurally derived from indomethacine [147], Pravadoline showed psychotropic side effects in clinical trials. It became apparent that these effects are mediated through the cannabinoid receptor. Optimization of the structure Anally led to WIN-55,212-2 (8.6), which has a higher affinity to the CBl receptor than THC [148]... 

HU-210 is (8.1) among the most potent cannabinoids known. Its enantiomer HU-211 (8.2) does not bind to the cannabinoid receptor and lacks psychotropic side effects (as long as optical purity is guaranteed). In animal models it shows analgesic and antiemetic activity. It also shows neuroprotec-tive effects after brain injury and was tested in humans as anti-traiuna agent, where it did not meet the expectations in a clinical phase III trial. 

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