PSB-SB-487

In this article, we will explore in detail the topic of PSB-SB-487, with the aim of providing our readers with a comprehensive vision of this relevant aspect in today's society. We will address various aspects, from its origin and evolution to its implications in daily life, in order to offer a comprehensive look that allows us to understand its importance and impact in different areas. Through an exhaustive analysis, we aim to provide an enriching perspective that contributes to knowledge and reflection on PSB-SB-487, inviting the audience to delve deeper into a topic of great relevance today.

PSB-SB-487
Identifiers
  • 7-(1,1-Dimethyloctyl)-5-hydroxy-3-(2-hydroxybenzyl)-2H-chromen-2-one
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H32O4
Molar mass408.538 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 an experimental drug which is used as a pharmacological research tool. It 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

  1. ^ 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.
  2. ^ 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.