Caffeine-induced inhibition of calcium channel current in cultured smooth cells from pregnant rat myometrium.

Abstract:

:1. The inhibitory effect of caffeine on the calcium channel current was investigated in cultured myometrial cells isolated from pregnant rats. 2. Caffeine inhibited the calcium channel current elicited from a holding potential of -70 mV in a concentration-dependent manner. The IC50 was estimated to be 35 mM. 3. The caffeine inhibition was not enhanced when calcium channels were opened by a conditioning depolarizing pulse sequence or when the number of inactivated calcium channels was increased at depolarized holding potentials. 4. Caffeine antagonized the specific binding of (+)-[3H]-isradipine to myometrial membranes. The IC50 value found in binding experiments was similar to the IC50 value for half-maximal inhibition of calcium channel current. Caffeine decreased the maximal binding capacity of (+)-[3H]-isradipine to myometrial membranes without any significant change in the dissociation constant. 5. The results indicate that caffeine interacts with a site closely associated with the voltage-dependent calcium channels in myometrial cells and, in turn, inhibits calcium influx.

journal_name

Br J Pharmacol

authors

Martin C,Dacquet C,Mironneau C,Mironneau J

doi

10.1111/j.1476-5381.1989.tb12622.x

subject

Has Abstract

pub_date

1989-10-01 00:00:00

pages

493-8

issue

2

eissn

0007-1188

issn

1476-5381

journal_volume

98

pub_type

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