CAS:596-51-0Glycopyrrolate

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Synonyms: Glycopyrrolate Bromide;Glycopyrronium Bromide;Gastrodyn

Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

596-51-0

储存条件

分子式

C19H28BrNO3

运输

蓝冰

分子量

398.33

别名

Glycopyrrolate Bromide;Glycopyrronium Bromide;Gastrodyn

溶解度

DMSO	95.0 mg/mL (238.5 mM)
Water	37.5 mg/mL (94.1 mM)

动物实验配方

生物活性

描述Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic. In competition studies, glycopyrrolate and ipratropium bromide bind human peripheral lung and human airway smooth muscle (HASM) muscarinic receptors with affinities in the nanomolar range (K1 values 0.5-3.6 nM). Similar to ipratropium bromide, glycopyrrolate showed no selectivity in its binding to the M1-M3 receptors. Glycopyrrolate bind human and guinea-pig airway muscarinic receptors with high affinity^[3]. Glycopyrrolate 1 mg was not superior to placebo, whereas 2 mg showed a significant clinical improvement of nocturnal sialorrhea compared with placebo. Glycopyrrolate seemed to be a tolerable anticholinergic agent in the treatment of clozapine-associated sialorrhea^[4]. It has now become common practice to use a dosage ratio of 0.2 mg glycopyrrolate to 1.0 mg neostigmine for NMB (reversal of neuromuscular blockade) reversal^[5]. Glycopyrrolate is virtually without side effects to the central nervous system because it penetrates the blood-brain barrier poorly. Glycopyrrolate has a slow and erratic absorption from the gastrointestinal system, but even low plasma levels are associated with a distinct and long-lasting antisialogic effect^[6].