Your browser doesn't support javascript.
loading
Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist.
Baska, Ferenc; Bozó, Éva; Szeleczky, Zsolt; Szántó, Gábor; Vukics, Krisztina; Szakács, Zoltán; Domány-Kovács, Katalin; Kurkó, Dalma; Vass, Elemér; Thán, Márta; Vastag, Mónika; Temesvári, Krisztina; Lévai, Sándor; Halász, Attila Sándor; Szondiné Kordás, Krisztina; Román, Viktor; Greiner, István; Bata, Imre.
Afiliación
  • Baska F; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Bozó É; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Szeleczky Z; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Szántó G; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Vukics K; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Szakács Z; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Domány-Kovács K; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Kurkó D; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Vass E; Institute of Chemistry, Eötvös Loránd University, Pázmány Péter sétány 1/A, Budapest H-1117, Hungary.
  • Thán M; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Vastag M; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Temesvári K; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Lévai S; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Halász AS; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Szondiné Kordás K; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Román V; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Greiner I; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
  • Bata I; Gedeon Richter Plc, PO Box 27, Budapest H-1475, Hungary.
J Med Chem ; 67(1): 643-673, 2024 01 11.
Article en En | MEDLINE | ID: mdl-38165765
ABSTRACT
The V1a receptor is a major contributor in mediating the social and emotional effects of arginine-vasopressin (AVP); therefore it represents a promising target in the treatment of several neuropsychiatric conditions. The aim of this research was to design and synthesize novel and selective V1a antagonists with improved in vitro and in vivo profiles. Through optimization and detailed SAR studies, we developed low nanomolar antagonists, and further characterizations led to the discovery of the clinical candidate compound 43 (RGH-122). The CNS activity of the compound was determined in a 3-chamber social preference test of autism in which RGH-122 successfully enhanced social preference with the lowest effective dose of 1.5 mg/kg.
Asunto(s)
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Arginina Vasopresina / Receptores de Vasopresinas Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Hungria Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Arginina Vasopresina / Receptores de Vasopresinas Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Hungria Pais de publicación: Estados Unidos