Effects of a novel phosphodiesterase 10A inhibitor in non-human primates: A therapeutic approach for schizophrenia with improved side effect profile
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- 作者：Gunasingh J. Masilamonia ; Subramanian Uthayathasa ; Gerhard Koenigb ; Liza Leventhalb ; Stella M. Papaa ; c ; spapa@emory.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：PDE10A inhibitor ; Phosphodiesterase ; Schizophrenia ; Striatum ; FDG PET imaging
- 刊名：Neuropharmacology
- 出版年：2016
- 出版时间：November 2016
- 年：2016
- 卷：110
- 期：part_PA
- 页码：449-457
- 全文大小：1465 K
文摘
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A new PDE10A inhibitor is profiled in primates as a candidate for antipsychotic therapy.
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FRM-6308 is highly selective and potent for PDE10A, and has good PK profile.
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FRM 6308 induced only mild sedation and dyskinesia at the highest dose tested (1 mg/kg).
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A range of (s.c.) doses of FRM-6308 has shown excellent tolerability in the primate.
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Non-sedative doses of FRM 6308 increased the striatal activity as measured by FDG-PET.