The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABA_B receptor with a potential for treatment of anxiety, pain and spasticity

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• 作者：Mikhail Kalinichev ; ^{mikhail.kalinichev@ipsen.com} ; Franç ; oise Girard ; Hasnaà ; Haddouk ; Mé ; lanie Rouillier ; Eric Riguet ; Isabelle Royer-Urios ; Vincent Mutel ; Robert Lü ; tjens ; Sonia Poli
• 关键词：Allosteric modulator ; GABA ; Anxiety ; Pain ; Body temperature ; Baclofen ; Spasticity ; Clinical candidate
• 刊名：Neuropharmacology
• 出版年：2017
• 出版时间：1 March 2017
• 年：2017
• 卷：114
• 期：Complete
• 页码：34-47
• 全文大小：1686 K
• 卷排序：114

文摘

ADX71441 is a novel, potent, selective, orally bioavailable and brain-penetrant GABAB receptor positive allosteric modulator. In rodents ADX71441 exhibits high bioavailability, long half-life and large volume of distribution. In vivo, ADX71441 shows anxiolytic- and antinociceptive-like effects with a consistent in vitro/in vivo correlation.