Clozapine has sub-micromolar affinity for 5-HT1A receptors in human brain tissue.
The affinities of a range of antipsychotic drugs at human hippocampal 5-HT1A receptors, defined by specific [3H]8-OH-DPAT binding, were determined. Clozapine demonstrated the highest affinity; all other antipsychotics studied demonstrated pK(i) values below 6.0 5-HT1A receptors are found on cortical glutamatergic neurons, a dysfunction of which may occur in schizophrenia. Binding at this site indicates a possible mechanism contributing to the unique efficacy of clozapine in the treatment of some schizophrenic patients.
Mason
S L
SL
Department of Biomedical Science, University of Sheffield, UK.
Reynolds
G P
GP
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000378:metabolism; D001921:Brain / Q000378:metabolism*; D003024:Clozapine / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D011985:Receptors, Serotonin / Q000378:metabolism*
D011985:Receptors, Serotonin; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D003024:Clozapine