Inhibition by DN-1417 (a TRH derivative) of [3H]GABA binding in the rat brain.
The administration of DN-1417, a synthetic derivative of TRH with more potent central action, significantly reduced specific [3H]GABA binding in the cerebellum, whereas [3H]GABA binding in the cerebral cortex was not changed. Scatchard analysis showed that the decreased [3H]GABA binding in the cerebellum was due to decreased binding sites of both high and low affinities. [3H]GABA binding to brain synaptic membranes was not affected by the addition of either TRH or DN-1417 in vitro. These findings suggest that TRH may play a role in regulating GABA receptors in the rat cerebellum.
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D018756:GABA Antagonists; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013570:Synaptic Membranes / Q000378:metabolism; D013973:Thyrotropin-Releasing Hormone / Q000031:analogs & derivatives* / Q000494:pharmacology; D014316:Tritium; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D018756:GABA Antagonists; D014316:Tritium; D005680:gamma-Aminobutyric Acid; D013973:Thyrotropin-Releasing Hormone; C029762:DN 1417