2-Hydroxysaclofen, a potent GABAB receptor antagonist, stimulates luteinizing hormone secretion in female rats.
An intraventricular injection of a potent GABAB receptor antagonist, 2-hydroxysaclofen, elicited luteinizing hormone (LH) secretion in a dose-dependent manner under the negative feedback condition in ovariectomized estrogen-primed rats. Significant reduction of the effect of 2-hydroxysaclofen by baclofen, a selective GABAB agonist, suggested that the antagonist stimulated LH secretion through interaction with the GABAB receptor. These results provide evidence that the endogenous GABA acting at the GABAB receptor plays a physiological role in controlling basal LH secretion.
Akema
T
T
Department of Physiology, St. Marianna University School of Medicine, Kawasaki, Japan.
Kimura
F
F
D000818:Animals; D001418:Baclofen / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D004967:Estrogens / Q000494:pharmacology; D005260:Female; D058787:GABA-A Receptor Antagonists; D007276:Injections, Intraventricular; D007986:Luteinizing Hormone / Q000097:blood*; D010052:Ovariectomy; D051381:Rats; D011919:Rats, Inbred Strains; D013268:Stimulation, Chemical
D004967:Estrogens; D058787:GABA-A Receptor Antagonists; D007986:Luteinizing Hormone; D001418:Baclofen; C057491:2-hydroxysaclofen