Interaction of flunarizine with dopamine D2 and D1 receptors.
Flunarizine dose dependently inhibits the binding of both [3H]spiperone and [3H]SCH 23390 with Ki values of 112 +/- 9 and 532 +/- 39 nM, respectively. The inhibition of [3H]spiperone binding by flunarizine was competitive as revealed by the Schild plot. The results indicate that flunarizine is a fairly potent dopamine D2 receptor antagonist and offer a possible explanation for the extrapyramidal side-effects observed in patients treated with the drug.
Ambrosio
C
C
Department of Neuroscience B.B. Brodie, University of Cagliari, Italy.
Stefanini
E
E
D000818:Animals; D001552:Benzazepines / Q000378:metabolism; D001667:Binding, Competitive; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D005444:Flunarizine / Q000378:metabolism / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000378:metabolism
D001552:Benzazepines; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; D013134:Spiperone; D005444:Flunarizine