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Background  Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H 1 ) receptors is believed to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT 2A /D 2 ) receptor binding affinity ratios.    Results  We have synthesized novel olanzapine analogues  8a  and  8b  together with the already known derivative  8c  and we have examined their respective  in vitro  affinities for the 5HT 2A , D 2 , and H 1  receptors.    Conclusions  We suggest that thienobenzodiazepines  8b  and  8c  with lower binding affinity for the H 1  receptors, but similar 5HT 2A /D 2  receptor binding affinity ratios to those of olanzapine. These compounds may offer a better pharmacological profile than olanzapine for treating patients with schizophrenia.

Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio