TOPIC

New V1a Receptor Antagonist. Part 2. Identification and Optimization of Triazolobenzazepines

Journal

Bioorganic & Medicinal Chemistry Letters

Author(s)

Éva Bozó, Ferenc Baska, Klára Lövei, Gábor Szántó, Katalin Domány-Kovács, Dalma Kurkó, Krisztina Szondiné Kordás, Teodóra Szokoli, Imre Bata

Year

2020

Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a receptor antagonists which can improve deteriorated social behavior in humans and can treat the core symptoms of autistic behavior, as well. Our aim was to identify new chemical entities with antagonizing effects on vasopressin V1a receptors. Continuing our previous work, we found an in vitro and in vivo orally active V1a selective antagonist molecule (40) among [1,2,4]triazolo[4,3-a][1]benzazepines.

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