| 词条 | VCHSR |
| 释义 |
| verifiedrevid = 448099272 | IUPAC_name = 5-(4-chlorophenyl)- 3-[(E)-2-cyclohexylethenyl]- 1-(2,4-dichlorophenyl)- 4-methyl- 1H-pyrazole | image = VCHSR.png | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID = 21378331 | chemical_formula = | C=24 | H=23 | Cl=3 | N=2 | molecular_weight = 445.811 | smiles = C4CCCCC4C=Cc(c(C)c1-c(cc3)ccc3Cl)nn1-c2ccc(Cl)cc2Cl | StdInChI = 1S/C24H23Cl3N2/c1-16-22(13-7-17-5-3-2-4-6-17)28-29(23-14-12-20(26)15-21(23)27)24(16)18-8-10-19(25)11-9-18/h7-15,17H,2-6H2,1H3/b13-7+ | StdInChIKey = UMOLSRBHNLXWGD-NTUHNPAUSA-N }}VCHSR is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It is derived from the widely used CB1 antagonist rimonabant, and has similar potency and selectivity for the CB1 receptor, but has been modified to remove the hydrogen bonding capability in the C-3 substituent region, which removes the inverse agonist effect that rimonabant produces at high doses, so that VCHSR instead acts as a neutral antagonist, blocking the receptor but producing no physiological effect of its own.[1][2] References1. ^{{cite journal | last1 = Hurst | first1 = DP | last2 = Lynch | first2 = DL | last3 = Barnett-Norris | first3 = J | last4 = Hyatt | first4 = SM | last5 = Seltzman | first5 = HH | last6 = Zhong | first6 = M | last7 = Song | first7 = ZH | last8 = Nie | first8 = J | last9 = Lewis | first9 = D | last10 = Reggio | first10 = P. H. | title = N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A) interaction with LYS 3.28(192) is crucial for its inverse agonism at the cannabinoid CB1 receptor | journal = Molecular Pharmacology | volume = 62 | issue = 6 | pages = 1274–87 | year = 2002 | pmid = 12435794 | doi = 10.1124/mol.62.6.1274 | display-authors = 8 }} {{Cannabinoids}}{{cannabinoid-stub}}2. ^{{cite journal | last1 = Hurst | first1 = D | last2 = Umejiego | first2 = U | last3 = Lynch | first3 = D | last4 = Seltzman | first4 = H | last5 = Hyatt | first5 = S | last6 = Roche | first6 = M | last7 = McAllister | first7 = S | last8 = Fleischer | first8 = D | last9 = Kapur | first9 = A | last10 = Abood | first10 = Mary | last11 = Shi | first11 = Shanping | last12 = Jones | first12 = Jannie | last13 = Lewis | first13 = Deborah | last14 = Reggio | first14 = Patricia | title = Biarylpyrazole inverse agonists at the cannabinoid CB1 receptor: importance of the C-3 carboxamide oxygen/lysine3.28(192) interaction | journal = Journal of Medicinal Chemistry | volume = 49 | issue = 20 | pages = 5969–87 | year = 2006 | pmid = 17004712 | doi = 10.1021/jm060446b | display-authors = 8 }} 4 : Cannabinoids|CB1 receptor antagonists|Pyrazoles|Chloroarenes |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。