Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT7) and 5-HT1A Receptor Activity

@article{Ishibashi2010PharmacologicalPO,
  title={Pharmacological Profile of Lurasidone, a Novel Antipsychotic Agent with Potent 5-Hydroxytryptamine 7 (5-HT7) and 5-HT1A Receptor Activity},
  author={Tadashi Ishibashi and Tomoko Horisawa and Kumiko Tokuda and Takeo Ishiyama and Masaaki Ogasa and Rie Tagashira and Kenji Matsumoto and Hiroyuki Nishikawa and Y{\^o}ko Ueda and Satoko Toma and Hitomi Oki and Norihiko. Tanno and Ikutaro Saji and Akira Ito and Yukihiro Ohno and Mitsutaka Nakamura},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2010},
  volume={334},
  pages={171 - 181}
}
Lurasidone [(3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione hydrochloride; SM-13496] is an azapirone derivative and a novel antipsychotic candidate. The objective of the current studies was to investigate the in vitro and in vivo pharmacological properties of lurasidone. Receptor binding affinities of lurasidone and several antipsychotic drugs were tested under comparable assay conditions using cloned… 

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Binding of lurasidone, a novel antipsychotic, to rat 5-HT7 receptor: Analysis by [3H]SB-269970 autoradiography
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TLDR
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TLDR
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Evaluation of dopamine D2/D3 and serotonin 5-HT2A receptor occupancy for a novel antipsychotic, lurasidone, in conscious common marmosets using small-animal positron emission tomography
TLDR
Compared with olanzapine, lurasidone preferentially binds to D2/D3 receptors rather than 5-HT2A receptors in common marmosets, suggesting that the contribution of in vivo 5- HT2A receptor blocking activity to the pharmacological profile of lurasIDone might differ from olanZapine in terms of the low risk of extrapyramidal syndrome and efficacy against negative symptoms.
Structural insight into receptor-selectivity for lurasidone
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