BMS-986187 is a δ-opioid receptor selective orthosteric 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).
|Formula||C31 H34 O4|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Jesse J DiCello, et al. Am J Physiol Gastrointest Liver Physiol. Positive allosteric modulation of endogenous delta opioid receptor signaling in the enteric nervous system is a potential treatment for gastrointestinal motility disorders
 M Alexander Stanczyk, et al. Br J Pharmacol. The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist
 Kathryn E Livingston, et al. Mol Pharmacol. Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors
 Yi Shang, et al. ACS Chem Biol. Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors
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