Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists.

Hervé Geneste,Swati Bhowmik,Marcel M van Gaalen,Wilfried Hornberger,Charles W Hutchins,Astrid Netz,Thorsten Oost,Liliane Unger

Bioorganic & Medicinal Chemistry Letters（2018）

引用 4|浏览17

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摘要

•Novel V1b antagonists.•Markedly improved selectivity and pharmacokinetic profiles.•Improved half-life and brain penetration (rat PK).•In vivo efficacy at 3 mg/kg (ip, rat forced swim test).•High volume of distribution to mitigate high in vivo plasma clearance.

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关键词

Vasopressin 1b,V1b,SSR149415,Oxindole

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