Bms-986122 is a selective and effective positive allosteric regulator of μ -opioid receptor (µ-OR). Bms-986122 showed enhancement of β -inhibitory protein recruitment, adenylate cyclase inhibition and G-protein activation mediated by normal agonists. Bms-986122 enhances damGO-mediated [35S]GTPγS binding in mouse meninges.
|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.
|Solubility||DMSO ≥ 60 mg/mL|
|Related Opioid Receptor Products|
Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Dermorphin can be used to suppress neuralgia.
SR17018 is an mu-opioid-receptor (MOR) agonist, EC50 is 97 nM for binding with GTPγS.
Adrenorphin (Metorphamide) is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
CYT-1010 is a mu-opioid receptor agonist with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
|Dynorphin A (1-8)
Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. Dynorphin A (1-8) inhibited 3H-Bremazocine binding to the purified kappa receptor with IC50 of 303 nM.
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