Hirsch M D
Peptides. 1983 Mar-Apr;4(2):255-60. doi: 10.1016/0196-9781(83)90123-7.
In vitro thyrotropin releasing hormone (TRH) radioligand binding assays were performed using purified presynaptic and postsynaptic membranes derived from various regions of mouse brain. These studies revealed the pattern of central distribution of specific TRH binding sites. The highest concentrations of both types of membrane receptors were localized in the limbic forebrain. The brain stem contained a high density of only presynaptic receptors, and the cerebral cortex contained a moderate-high level of only postsynaptic receptors. Barbiturate analogues effectively competed for all forebrain and brain stem, but not cortical, TRH receptors, thus implicating these specific receptors in the neuromodulation of barbiturate anesthesia. The results of in vivo radioligand binding assays for [3H] TRH disposition after central infusions concomitant with barbiturate vs. saline challenges further support this viewpoint.
利用从小鼠脑不同区域提取的纯化突触前膜和突触后膜进行体外促甲状腺激素释放激素（TRH）放射性配体结合试验。这些研究揭示了特定TRH结合位点的中枢分布模式。两种类型的膜受体浓度最高的部位都在边缘前脑。脑干仅含有高密度的突触前受体，而大脑皮层仅含有中等偏高水平的突触后受体。巴比妥类类似物能有效竞争所有前脑和脑干而非皮层的TRH受体，因此表明这些特定受体参与巴比妥类麻醉的神经调节。与盐水激发相比，在中枢输注巴比妥类药物后进行体内放射性配体结合试验以检测[3H]TRH处置情况的结果进一步支持了这一观点。
