熔点 | 223°C |
溶解性 | Soluble in water (160 mg/ml), methanol (286 mg/ml), ethanol (53.7 mg/ml), DMSO (205 mg/ml), and chloroform. |
应用 | A Ca2+ channel protein inhibitor and MOR activator. |
产品介绍 | Loperamide HCl是一种阿片受体激动剂,ED50为0.15 mg/kg。 |
备注 | Loperamide HCl is an opioid-receptor agonist with an ED50 of 0.15 mg/kg. |
生化机理 | Loperamide Hydrochloride is an opiate agonist with selectivity for the MOR (μ-opiod receptor). This specificity for μ-opioid receptors and limited penetrability into the brain prevent Loperamide from demonstrating central systemic effects generally associated with opiates, instead demonstrating localized action on the nociceptor and resultant antihyperalgesic action. Loperamide is shown to have an effect on the Ca2+ flux through high-voltage-activated calcium channels in response to high levels of extracellular K+, and at higher concentrations Loperamide is also a calcium channel protein inhibitor via the N-methyl-D-aspartate (NMDA) receptor-operated ion channel. |
别名 | 洛哌丁胺 盐酸盐;盐酸氯苯哌酰胺;4-(对氯苯基)-4-羟基-N,N-二甲基-α,α-二苯基-1-哌啶丁酰胺盐酸盐;盐酸洛哌丁胺;4-(p-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutyramide hydrochloride;Loperamide Hydrochloride;4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide Hydrochloride;Imodium |