A comparison of the effects of midazolam and pentobarbital on the dose-response of GABA-gated Cl − influx in rat brain microsacs

γ-Aminobutyric acid (GABA)-gated Cl − influx was studied in a rat brain ‘microsac’ preparation. Midazolam (a benzodiazepine), at 0.1–10 μM, increased GABA potency (maximum 2-fold) without affecting its efficacy or exerting GABA-mimetic effect. Pentobarbital (10–500 μM) increased GABA potency (maximu...

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Veröffentlicht in:	Brain research 1988-06, Vol.451 (1), p.376-380
Hauptverfasser:	Yu, Onnfoh, Chiu, Ted H., Rosenberg, Howard C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Barbiturate Benzodiazepine Biological and medical sciences Chloride flux Chloride ion Chlorides - metabolism Dose-Response Relationship, Drug gamma-Aminobutyric Acid - metabolism Ions Male Medical sciences Midazolam Midazolam - pharmacology Neuropharmacology Pentobarbital Pentobarbital - pharmacology Pharmacology. Drug treatments Psycholeptics: tranquillizer, neuroleptic Psychology. Psychoanalysis. Psychiatry Psychopharmacology Rat brain Rats Rats, Inbred Strains γ-Aminobutyric acid
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Zusammenfassung:	γ-Aminobutyric acid (GABA)-gated Cl − influx was studied in a rat brain ‘microsac’ preparation. Midazolam (a benzodiazepine), at 0.1–10 μM, increased GABA potency (maximum 2-fold) without affecting its efficacy or exerting GABA-mimetic effect. Pentobarbital (10–500 μM) increased GABA potency (maximum 12-fold) and efficacy (maximum 40%). Pentobarbital exhibited GABA-mimetic effect at concentrations above 200 μM. The differential effects of midazolam and pentobarbital in modulating GABA-mediated responses may account for some of the differences between these two classes of drugs.
ISSN:	0006-8993 1872-6240
DOI:	10.1016/0006-8993(88)90788-3