NESS-0327 is a drug used in scientific research which acts as an extremely potent and selective antagonist of the cannabinoid receptorCB1. It is much more potent an antagonist, and more selective for the CB1 receptor over CB2, than the more commonly used ligand rimonabant, with a Ki at CB1 of 350fM (i.e. 0.00035nM) and a selectivity of over 60,000x for CB1 over CB2.[1] Independently, two other groups have described only modest nanomolar CB1 affinity for this compound (125nM[2] and 18.4nM[3]). Also unlike rimonabant, NESS-0327 does not appear to act as an inverse agonist at higher doses, instead being a purely neutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own.[4]
^Ruiu S, Pinna GA, Marchese G, Mussinu JM, Saba P, Tambaro S, et al. (July 2003). "Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor". The Journal of Pharmacology and Experimental Therapeutics. 306 (1): 363–70. doi:10.1124/jpet.103.049924. PMID 12663689. S2CID 32018707.
^Stoit AR, Lange JH, Hartog AP, Ronken E, Tipker K, Stuivenberg HH, et al. (August 2002). "Design, synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists". Chemical & Pharmaceutical Bulletin. 50 (8): 1109–13. doi:10.1248/cpb.50.1109. PMID 12192147.
^Zhang Y, Burgess JP, Brackeen M, Gilliam A, Mascarella SW, Page K, et al. (June 2008). "Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations". Journal of Medicinal Chemistry. 51 (12): 3526–39. doi:10.1021/jm8000778. PMID 18512901.
^Tambaro S, Mongeau R, Dessi C, Pani L, Ruiu S (November 2005). "Modulation of ATP-mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors". European Journal of Pharmacology. 525 (1–3): 150–3. doi:10.1016/j.ejphar.2005.09.058. PMID 16271359.
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ness, 0327, drug, used, scientific, research, which, acts, extremely, potent, selective, antagonist, cannabinoid, receptor, much, more, potent, antagonist, more, selective, receptor, over, than, more, commonly, used, ligand, rimonabant, with, 350fm, 00035nm, s. NESS 0327 is a drug used in scientific research which acts as an extremely potent and selective antagonist of the cannabinoid receptor CB1 It is much more potent an antagonist and more selective for the CB1 receptor over CB2 than the more commonly used ligand rimonabant with a Ki at CB1 of 350fM i e 0 00035nM and a selectivity of over 60 000x for CB1 over CB2 1 Independently two other groups have described only modest nanomolar CB1 affinity for this compound 125nM 2 and 18 4nM 3 Also unlike rimonabant NESS 0327 does not appear to act as an inverse agonist at higher doses instead being a purely neutral antagonist which blocks the CB1 receptor but does not produce any physiological effect of its own 4 NESS 0327IdentifiersCAS Number494844 07 4PubChem CID10435654ChemSpider8611079 NUNIIX1BQI2J97ICompTox Dashboard EPA DTXSID00439851Chemical and physical dataFormulaC 24H 23Cl 3N 4OMolar mass489 83 g mol 13D model JSmol Interactive imageSMILES Clc3cc Cl ccc3 n4c2 c1ccc Cl cc1CCCc2c n4 C O NN5CCCCC5InChI InChI 1S C24H23Cl3N4O c25 16 7 9 18 15 13 16 5 4 6 19 22 24 32 29 30 11 2 1 3 12 30 28 31 23 18 19 21 10 8 17 26 14 20 21 27 h7 10 13 14H 1 6 11 12H2 H 29 32 NKey NCXBPZJQQSNIRA UHFFFAOYSA N N N Y what is this verify See also EditDiscovery and development of Cannabinoid Receptor 1 Antagonists NESS 040C5References Edit Ruiu S Pinna GA Marchese G Mussinu JM Saba P Tambaro S et al July 2003 Synthesis and characterization of NESS 0327 a novel putative antagonist of the CB1 cannabinoid receptor The Journal of Pharmacology and Experimental Therapeutics 306 1 363 70 doi 10 1124 jpet 103 049924 PMID 12663689 S2CID 32018707 Stoit AR Lange JH Hartog AP Ronken E Tipker K Stuivenberg HH et al August 2002 Design synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists Chemical amp Pharmaceutical Bulletin 50 8 1109 13 doi 10 1248 cpb 50 1109 PMID 12192147 Zhang Y Burgess JP Brackeen M Gilliam A Mascarella SW Page K et al June 2008 Conformationally constrained analogues of N piperidinyl 5 4 chlorophenyl 1 2 4 dichlorophenyl 4 methyl 1H pyrazole 3 carboxamide SR141716 design synthesis computational analysis and biological evaluations Journal of Medicinal Chemistry 51 12 3526 39 doi 10 1021 jm8000778 PMID 18512901 Tambaro S Mongeau R Dessi C Pani L Ruiu S November 2005 Modulation of ATP mediated contractions of the rat vas deferens through presynaptic cannabinoid receptors European Journal of Pharmacology 525 1 3 150 3 doi 10 1016 j ejphar 2005 09 058 PMID 16271359 This cannabinoid related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title NESS 0327 amp oldid 1166942400, wikipedia, wiki, book, books, library,
