Loperamide (hydrochloride)

Loperamide is an opiate which potently and selectively activates µ opioid receptors (Ki = 0.16 nM) exclusively in the periphery. Loperamide is an opiate which potently and selectively activates µ opioid receptors (Ki = 0.16 nM) exclusively in the periphery. It is a much weaker agonist of the delta opioid receptor (Ki = 50 nM). Through its actions in the gut wall, loperamide has antidiarrheal action by increasing transit time and by altering intestinal transport of water and electrolytes. It also blocks voltage-sensitive sodium channels (IC50 = 270 nM) and high voltage-activated calcium channels (IC50 = 900 nM), presumably through an inhibitory effect on calmodulin. Loperamide is comparable to morphine in blocking peripheral pain in rats.Formal Name: 4-(4-chlorophenyl)-4-hydroxy-N,N-dimethyl-alpha,alpha-diphenyl-1-piperidinebutanamide, monohydrochloride. CAS Number: 34552-83-5. Molecular Formula: C29H33ClN2O2 . HCl. Formula Weight: 513.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2.5 mg/ml, DMSO: 2.5 mg/ml, Ethanol: 10 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. SMILES: O=C(N(C)C)C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3CCC(C4=CC=C(Cl)C=C4)(O)CC3.Cl. InChi Code: InChI=1S/C29H33ClN2O2.ClH/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23,/h3-16,34H,17-22H2,1-2H3,1H. InChi Key: PGYPOBZJRVSMDS-UHFFFAOYSA-N.