Mixed antagonistic effects of bilobalide at rho1 GABAC receptor.
Neuroscience
; 137(2): 607-17, 2006.
Article
en En
| MEDLINE
| ID: mdl-16300902
ABSTRACT
Bilobalide was found to be a moderately potent antagonist with a weak use-dependent effect at recombinant human rho(1) GABA(C) receptors expressed in Xenopus oocytes using two-electrode voltage clamp methodology. Antagonism of bilobalide at homomeric rho(1) GABA(C) receptors appeared to be mixed. At low concentration, bilobalide (3 microM) caused a parallel right shift and surmountable GABA maximal response of the GABA dose-response curve characteristic of a competitive antagonist. At high concentrations, bilobalide (10-100 microM) caused nonparallel right shifts and reduced maximal GABA responses of GABA dose-response curves characteristic of a noncompetitive antagonist. The potency of bilobalide appears to be dependent on the concentrations of GABA and was more potent at lower GABA concentrations. The mechanism of action of bilobalide at rho(1) GABA(C) receptors appears to be similar to that of the chloride channel blocker picrotoxinin.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Oocitos
/
Extractos Vegetales
/
Receptores de GABA
/
Ciclopentanos
/
Diterpenos
/
Furanos
Límite:
Animals
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Female
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Humans
Idioma:
En
Revista:
Neuroscience
Año:
2006
Tipo del documento:
Article
País de afiliación:
Australia