| 词条 | PSB-SB-487 |
| 释义 |
| IUPAC_name = 7-(1,1-Dimethyloctyl)-5-hydroxy-3-(2-hydroxybenzyl)-2H-chromen-2-one | image = PSB-SB-487_structure.png | width = 300 | tradename = | CAS_number = | PubChem = 70678101 | ChemSpiderID = 28667155 | C=26 | H=32 | O=4 | molecular_weight = 408.53 | smiles = OC1=C(CC2=CC3=C(C=C(C(C)(C)CCCCCCC)C=C3O)OC2=O)C=CC=C1 | StdInChI = 1S/C26H32O4/c1-4-5-6-7-10-13-26(2,3)20-16-23(28)21-15-19(25(29)30-24(21)17-20)14-18-11-8-9-12-22(18)27/h8-9,11-12,15-17,27-28H,4-7,10,13-14H2,1-3H3 | StdInChIKey = YNWOMOUVWNKICO-UHFFFAOYSA-N }}PSB-SB-487 is a coumarin derivative which is an antagonist at the former orphan receptor GPR55. Unlike older GPR55 antagonists such as O-1918, PSB-SB-487 has good selectivity over the related receptor GPR18, with an IC50 of 113nM at GPR55 vs 12500nM at GPR18.[1] However it has poorer selectivity over other related receptors, acting as a weak antagonist at CB1 with a Ki of 1170nM, and a partial agonist at CB2 with a Ki of 292nM.[2] See also
References1. ^{{Cite journal | last1 = Rempel | first1 = V. | last2 = Volz | first2 = N. | last3 = Gläser | first3 = F. | last4 = Nieger | first4 = M. | last5 = Bräse | first5 = S. | last6 = Müller | first6 = C. E. | title = Antagonists for the orphan G protein-coupled receptor GPR55 based on a coumarin scaffold | doi = 10.1021/jm4005175 | journal = Journal of Medicinal Chemistry | pages = 130516144836005 | year = 2013 | pmid = 23679955 | pmc = | volume=56 | issue=11}} {{Cannabinoids}}{{Cannabinoidergics}}2. ^Rempel V, Volz N, Hinz S, Karcz T, Meliciani I, Nieger M, Wenzel W, Bräse S, Müller CE. 7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists. Journal of Medicinal Chemistry. 2012 Sep 27;55(18):7967-77. {{PMID|22916707}} 1 : Cannabinoids |
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