Synthesis and GABAA receptor activity of oxygen-bridged neurosteroid analogs

Three analogs of neuroactive steroids were prepared (4-6) in which 1,11- or 11,19-oxygen bridges give a constrained conformation. Their 3D structures were obtained by ab initio calculations and in the case of 3α-hydroxy-11,19-epoxypregn-4-ene-20-one (4), confirmed by X-ray analysis. Biological activ...

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Detalles Bibliográficos
Autores principales: Alvarez, L.D., Veleiro, A.S., Baggio, R.F., Garland, M.T., Edelsztein, V.C., Coirini, H., Burton, G.
Formato: JOUR
Materias:
γ-Aminobutyric acid
GABA
GABAA receptor
Neurosteroids
Steroids
3alpha hydroxy 11,19 epoxypregn 4 ene 20 one
3alpha hydroxy 1alpha,11alpha epoxy 5beta pregnan 20 one
3alpha hydroxy 1beta,11alpha epoxy 5alpha pregnan 20 one
3alpha hydroxy 5alpha pregnan 20 one
4 aminobutyric acid A receptor
eltanolone
neurosteroid
oxygen
tert butylbicycloorthobenzoate
tritium
unclassified drug
ab initio calculation
article
biological activity
controlled study
drug conformation
drug receptor binding
drug structure
in vitro study
isotope labeling
male
nonhuman
rat
X ray analysis
Animals
Male
Models, Molecular
Molecular Structure
Neurons
Oxygen
Rats
Rats, Sprague-Dawley
Receptors, GABA-A
Acceso en línea:http://hdl.handle.net/20.500.12110/paper_09680896_v16_n7_p3831_Alvarez
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

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