Tetrandrine and Isotetrandrine, Two Bisbenzyltetrahydroisoquinoline Alkaloids from Menispermaceae, with Rat Uterine Smooth Muscle Relaxant Activity

6533b858fe1ef96bd12b5af5

RESEARCH PRODUCT

Tetrandrine and Isotetrandrine, Two Bisbenzyltetrahydroisoquinoline Alkaloids from Menispermaceae, with Rat Uterine Smooth Muscle Relaxant Activity

Pilar D'ocon Elsa Anselmi M. Amparo Blázquez Almudena Bermejo

subject

Stereochemistry Pharmaceutical Science In Vitro Techniques Pharmacology Oxytocin Benzylisoquinolines Uterine contraction Uterine Contraction chemistry.chemical_compound Alkaloids medicine Animals Pharmacology Dose-Response Relationship Drug business.industry Alkaloid Calcium channel Anti-Inflammatory Agents Non-Steroidal Uterus Muscle Smooth Rats Inbred Strains Stereoisomerism Biological activity Acetylcholine Rats Tetrandrine Oxytocin chemistry Depression Chemical Female medicine.symptom business Acetylcholine medicine.drug Muscle contraction

description

Abstract The effects of two bisbenzyltetrahydroisoquinoline alkaloids, 1S, 1′S tetrandrine and its isomer 1R, 1′S isotetrandrine, were investigated in rat isolated uterus in order to identify the mechanism of relaxant action and to study the influence of the absolute configuration on the activity of these alkaloids. Both inhibited the uterine contraction induced by high K+, acetylcholine and oxytocin. In Ca2+-free medium, isotetrandrine relaxed the sustained contraction induced by oxytocin but tetrandrine did not. The relaxant effects of the alkaloids may be due to blockade of calcium influx through specific channels. Tetrandrine and isotetrandrine modify the calcium channel in a nonreversible manner whilst only isotetrandrine acts intracellularly. Tetrandrine shows a more specific relaxant activity as a calcium entry blocker.

year	journal	country	edition	language
1992-07-01	Journal of Pharmacy and Pharmacology

https://doi.org/10.1111/j.2042-7158.1992.tb05468.x

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