Synthesis and GABAA receptor activity of a 6,19-oxido analogue of pregnanolone

3α-Hydroxy-6,19-oxidopregn-4-ene-20-one (4) was prepared in seven steps from pregnanolone acetate. At 0.1 μM concentration 4 significantly increased GABA induced 36Cl- influx in hamster cerebral cortex synaptoneurosomes while at 20 mg/kg it decreased the percentage of hamsters showing seizures induc...

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Guardado en:
Detalles Bibliográficos
Publicado: 2003
Materias:
3 mercaptopropionic acid
3alpha hydroxy 6,19 oxidopregn 4 en 20 one
4 aminobutyric acid A receptor
acetic acid derivative
anticonvulsive agent
chloride ion
eltanolone
unclassified drug
animal cell
animal experiment
article
brain cortex
brain synaptosome
chloride transport
concentration response
controlled study
dose response
drug activity
drug synthesis
hamster
nonhuman
seizure
3-Mercaptopropionic Acid
Animals
Cerebral Cortex
Convulsants
Cricetinae
Indicators and Reagents
Pregnanolone
Receptors, GABA-A
Seizures
Stereoisomerism
Structure-Activity Relationship
Synaptosomes
Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0960894X_v13_n3_p343_Veleiro
http://hdl.handle.net/20.500.12110/paper_0960894X_v13_n3_p343_Veleiro
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires
Descripción
Sumario:3α-Hydroxy-6,19-oxidopregn-4-ene-20-one (4) was prepared in seven steps from pregnanolone acetate. At 0.1 μM concentration 4 significantly increased GABA induced 36Cl- influx in hamster cerebral cortex synaptoneurosomes while at 20 mg/kg it decreased the percentage of hamsters showing seizures induced by 3-mercaptopropionic acid. © 2002 Elsevier Science Ltd. All rights reserved.

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