Orphenadrine hydrochloride

A muscarinic acetylcholine receptor antagonist

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100mg

￥537.00

430.00

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货号: ajce51644
CAS: 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
分子式: C18H24ClNO
分子量: 305.84
纯度: >98%
溶解度: DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 10 mg/ml
储存: Store at -20°C
库存: 现货

Background

Orphenadrine is a muscarinic acetylcholine receptor (mAChR) antagonist (K_ds = 48, 213, 120, 170, and 129 nM for M₁-M₅ receptors, respectively).¹ Orphenadrine (2-5 mg/kg, i.v.) decreases muscle activity induced by the mAChR agonist oxotremorine in rabbits.² It is also an NMDA receptor antagonist with a K_i value of 6 ?M in a radioligand binding assay in human postmortem frontal cortex and an IC₅₀ value of 16.2 ?M for inhibiting steady state currents in cultured superior colliculus neurons.³ Formulations containing orphenadrine have been used in the treatment of acute painful musculoskeletal conditions, including muscle spasms.

1.Stanton, T., Bolden-Watson, C., Cusack, B., et al.Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminicsBiochem. Pharmacol.45(11)2352-2354(1993) 2.Ban, T., and Hojo, M.A comparative study of the effects of anti-parkinson drugs on the oxotremorine-induced EEG and muscular activitiesPsychopharmacologia19(1)1-15(1971) 3.Kornhuber, J., Parsons, C.G., Hartmann, S., et al.Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: Binding and patch clamp studiesJ. Neural Transm. Gen. Sect.102(3)237-246(1995)