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Orphenadrine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Orphenadrine hydrochloride图片
CAS NO:341-69-5
包装:100mg
市场价:446元

产品介绍
Orphenadrine盐酸盐是非竞争性的NMDA受体拮抗剂,Ki值为6.0±0.7μM。
Cas No.341-69-5
别名盐酸奥芬那君;盐酸邻甲苯海拉明;奥芬那君盐酸盐
Canonical SMILESCC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C.[H]Cl
分子式C18H24ClNO
分子量305.84
溶解度DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Orphenadrine hydrochloride is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 6.0 ±0.7 μM.IC50 value: 6.0 ±0.7 μM (Ki)Target: NMDA ReceptorOrphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug. Orphenadrine inhibits [3H]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cortex with a Ki-value of 6.0 ±0.7 μM. The NMDA receptor antagonistic effects of orphenadrine were assessed using concentration- and patch-clamp techniques on cultured superior colliculus neurones. Orphenadrine blocked open NMDA receptor channels with fast kinetics and in a strongly voltage-dependent manner. The IC50-value against steady state currents at -70 mV was 16.2 ± 1.6 μM (n = 6). [1]. Orphenadrine competitively inhibited [3H]nisoxetine binding in rat vas deferens membranes (Ki = 1.05 ±0.20 μM). It can be concluded that orphenadrine, at low micromolar concentrations, interacts with the noradrenaline reuptake system inhibiting its functionality and thus potentiating the effect of noradrenaline [2].

[1]. Kornhuber, J., et al., Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect, 1995. 102(3): p. 237-46. [2]. Pubill, D., et al., Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol, 1999. 51(3): p. 307-12.