Synthesis and GABAA receptor activity of A-homo analogues of neuroactive steroids

0346335 - ÚOCHB 2011 RIV FR eng J - Článek v odborném periodiku
Dansey, M. V. - Di Chenna, P. - Valeiro, A. S. - Krištofíková, Z. - Chodounská, Hana - Kasal, Alexander - Burton, G.
Synthesis and GABAA receptor activity of A-homo analogues of neuroactive steroids.
European Journal of Medicinal Chemistry. Roč. 45, č. 7 (2010), s. 3063-3069. ISSN 0223-5234. E-ISSN 1768-3254
Grant CEP: GA ČR(CZ) GA203/08/1498
Výzkumný záměr: CEZ:AV0Z40550506
Klíčová slova: A-homopregnane * neurosteroid * gamma-aminobutyric acid * GABAA receptor
Kód oboru RIV: CC - Organická chemie
Impakt faktor: 3.193, rok: 2010

A-Homo-5-pregnenes were prepared and their inhibition of binding TBPS to GABAA receptors was measured. 3alpha-Hydroxy and 4alpha-hydroxy analogues of allopregnanolone were slightly active while the 3beta-hydroxy analogue was almost as active as allopregnanolone. Reduction of the double bond of the latter compound resulted in a ten fold loss of activity.
Trvalý link: http://hdl.handle.net/11104/0187392