New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines

[Display omitted] 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....

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Published in:Bioorganic & medicinal chemistry letters 2020-09, Vol.30 (18), p.127417-127417, Article 127417
Main Authors: Bozó, Éva, Baska, Ferenc, Lövei, Klára, Szántó, Gábor, Domány-Kovács, Katalin, Kurkó, Dalma, Szondiné Kordás, Krisztina, Szokoli, Teodóra, Bata, Imre
Format: Article
Language:English
Subjects:
Antagonist
HTS
Synthesis
Triazolobenzazepines
V1a
Vasopressin
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Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127417