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Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio
Faculty of Science, Medicine and Health - Papers
  • Somayeh Jafari, University of Wollongong
  • Marc E Bouillon, University of Wollongong
  • Xu-Feng Huang, University of Wollongong
  • Stephen G Pyne, University of Wollongong
  • Francesca Fernandez-Enright, University of Wollongong
RIS ID
64933
Publication Date
1-1-2012
Publication Details

Jafari, S., Bouillon, M. E., Huang, X., Pyne, S. G. & Fernandez-Enright, F. 2012, 'Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio', BMC Pharmacology, vol. 12, no. June, pp. 1-8.

Abstract

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 (H1) 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 (5HT2A/D2) 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 5HT2A, D2, and H1 receptors. Conclusions We suggest that thienobenzodiazepines 8b and 8c with lower binding affinity for the H1 receptors, but similar 5HT2A/D2 receptor binding affinity ratios to those of olanzapine. These compounds may offer a better pharmacological profile than olanzapine for treating patients with schizophrenia.

Citation Information
Somayeh Jafari, Marc E Bouillon, Xu-Feng Huang, Stephen G Pyne, et al.. "Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio" (2012)
Available at: http://works.bepress.com/xhuang/112/