Tatsuoka Y, Kato Y, Imura H
Neurosci Lett. 1983 Dec 2;42(2):149-54. doi: 10.1016/0304-3940(83)90398-1.
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.
TRH的合成衍生物DN-1417具有更强的中枢作用，给予DN-1417可显著降低小脑内特异性[3H]GABA结合，而大脑皮质中的[3H]GABA结合未发生变化。Scatchard分析表明，小脑内[3H]GABA结合减少是由于高亲和力和低亲和力结合位点均减少所致。在体外，[3H]GABA与脑突触膜的结合不受TRH或DN-1417添加的影响。这些发现提示，TRH可能在调节大鼠小脑的GABA受体中发挥作用。
