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Interaction of clozapine with the histamine H 3 receptor in rat brain
Author(s) -
Rodrigues A. Alves,
Jansen F.P.,
Leurs R.,
Timmerman H.,
Prell G.D.
Publication year - 1995
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1995.tb14934.x
Subject(s) - clozapine , histamine h3 receptor , antagonist , histamine , pharmacology , histamine h1 receptor , chemistry , receptor , receptor antagonist , endocrinology , medicine , neuroscience , biology , schizophrenia (object oriented programming) , biochemistry , psychiatry
We examined possible interactions between neuroleptics and the histamine H 3 receptor and found an interaction of clozapine with this receptor. In competition binding experiments, using the H 3 antagonist, [ 125 I]‐iodophenpropit, we observed a K i of 236 ± 87 nM. Functionally, clozapine was studied on the H 3 ‐mediated inhibition of [ 3 H]‐5‐hydroxytryptamine ([ 3 H]‐5‐HT) release from rat brain cortex slices. Clozapine acts as an antagonist with an apparent K B value of 79.5 nM.