Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors.

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Taylor JE, Defeudis FV

Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors.

Neurochem Int. 1986;9(3):379-81.

PubMed ID

20493137 [ View in PubMed

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Abstract

Experiments conducted on membrane fractions of guinea-pig brain using ligand-binding techniques have shown that certain Ca(2+)-antagonists interact with histamine (H(1) or H(2)) receptors. Flunarizine (inhibition constant, K(i) ? 86 nM) was nearly as potent as diphenhydramine (K(i) ? 44 nM) in inhibiting [(3)H]pyrilamine binding to cerebellar H(1)-receptors, whereas verapamil, D 600 and nifedipine did not interact with this site. Regarding [(3)H]tiotidine binding to H(2)-receptors of cerebral cortex, verapamil (K(i) ? 1400 nM) and D 600 (K(i) ? 1240 nM) were nearly as potent as cimetidine (K(i) ? 910 nM) whereas flunarizine and nifedipine were inactive. The interaction of flunarizine with H(1)-receptors might explain, in part, its sedative side-effect. The interaction of verapamil with H(2)-receptors, demonstrated here for the first time, might be involved in the anti-arrhythmic action of this agent.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Flunarizine	Histamine H1 receptor	Protein	Humans	Unknown	Antagonist	Details