The discovery of a series of new non-indole 5HT1D agonists

Autor:	Marcel Frans Leopold De Bruyn, W. J. Janssens, Wim Gaston Verschueren, Josée E. Leysen, Jan Verrelst, Guy Van Lommen, Marc Francis Josephine Schroven
Rok vydání:	1995
Předmět:	Indole test Series (mathematics) Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Alniditan Biochemistry Affinities chemistry.chemical_compound chemistry medicine.artery Drug Discovery Basilar artery medicine Molecular Medicine Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 5:2649-2654
ISSN:	0960-894X
DOI:	10.1016/0960-894x(95)00473-7
Popis:	The synthesis and SAR of a series of non-indole 5HT1D agonists is described. The most interesting molecule of this series is compound 13, alniditan. It is active as a constrictor of the saphenous vein of the dog and of the pig basilar artery with ED50 values of 9.09×10−9M and 2.29×10−8M respectively, and it has high affinities to the 5HT1D-receptor and to the 5HT1D-receptor with pKi values of 8.6 and 8.3 respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::d024e8d6f0f545203b92aba50ede6927 https://doi.org/10.1016/0960-894x(95)00473-7 Zobrazit plný text záznamu Full Text from ScienceDirect