684238-37-7

684238-37-7 structure

Name: BMS 986187
Chemical Name: 684238-37-7
CAS Number: 684238-37-7
Molecular Formula: C₃₁H₃₄O₄
Molecular Weight: 470.599
Create Date: 2018-06-16 15:53:21
Modify Date: 2024-01-03 11:07:33
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM)[1].

Name	684238-37-7
Synonyms	1H-Xanthene-1,8(2H)-dione, 3,4,5,6,7,9-hexahydro-3,3,6,6-tetramethyl-9-[4-[(2-methylphenyl)methoxy]phenyl]- 3,3,6,6-Tetramethyl-9-{4-[(2-methylbenzyl)oxy]phenyl}-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8(2H)-dione

Description	BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM)[1].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
In Vitro	BMS-986187 (1 nM-100 uM) produces little or no activity in agonist mode, but in PAM mode (in the presence of an EC20 of leu-enkephalin (in CHO-OPRD1 cells) or endomorphin 1 (in CHO-OPRM1 cells)) produces a response with an EC50 of 48 nM in CHO-OPRD1 cells and 2 μM in CHO-OPRM1 cells[1].
References	[1]. Neil T Burford, et al. Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. J Med Chem. 2015 May 28;58(10):4220-9.