PSB-SB-487
7-(1,1-Dimethyloctyl)-5-hydroxy-3-(2-hydroxybenzyl)-2H-chromen-2-one
PubChem CID ChemSpider Formula C 26 H 32 O 4 Molar mass 408.53 g·mol−1 3D model (JSmol )
OC1=C(CC2=CC3=C(C=C(C(C)(C)CCCCCCC)C=C3O)OC2=O)C=CC=C1
InChI=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
Key: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 [ ]
References [ ]
^ Rempel V, Volz N, Gläser F, Nieger M, Bräse S, Müller CE (June 2013). "Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold" . Journal of Medicinal Chemistry . 56 (11): 4798–810. doi :10.1021/jm4005175 . PMID 23679955 .
^ Rempel V, Volz N, Hinz S, Karcz T, Meliciani I, Nieger M, et al. (September 2012). "7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists". Journal of Medicinal Chemistry . 55 (18): 7967–77. doi :10.1021/jm3008213 . PMID 22916707 .
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α-Amyrin · β-Amyrin
A-796,260
A-834,735
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AZ-11713908
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L-759,633
L-759,656
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PF-03550096
S-444,823
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Agonists: 2-AGE (noladin ether)
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Receptor/signaling modulators
Cannabinoids (cannabinoids by structure)