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

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.
Mesh Terms:
Anticoagulants, Atrial Fibrillation, Benzimidazoles, Factor Xa, Factor Xa Inhibitors, Humans, Pyridines, Review Literature as Topic, Treatment Outcome, Venous Thromboembolism
Neurochem. Int.
Date: Jan. 01, 1986
Download Curated Data For This Publication
182154
Switch View:
  • Chemical Interactions 1