Taché Y, Ruisseau P D, Ducharme J R, Collu R
Eur J Pharmacol. 1977 Oct 15;45(4):369-76. doi: 10.1016/0014-2999(77)90276-x.
In adult male rats, injection of TRH into a lateral ventricle of the brain 5 min prior to pentobarbital (PB) administration caused a significant dose-related inhibition of prolactin (PRL) release, in doses ranging from 500 to 5 ng. Among 8 TRH analogues devoid of thyrotropin-releasing activity, 6 were found to significantly suppress PB-induced PRL secretion at an intraventricular dose level of 10 microgram, and the 3 most effective in this respect were also able to counteract growth hormone (GH) release elicited by PB. The derivative [1,3'-DCM2]TRH was still potent enough to block PB-induced PRL secretion at an intraventricular dosage of 50 ng. The peptide ACTH 4--10 was ineffective, whereas another ACTH derivative H-Met(O2)-Glu-His-Phe-D-Lys-Phe-OH (Org 2766) reduced PRL release. TRH did not affect the increase of plasma PRL induced by acute stress. alpha-Methyl-p-tyrosine (alpha-MT) failed to influence the inhibiting effect of TRH on GH secretion but significantly reduced that on PRL release. p-Chlorophenylalanine (PCPA) completely blocked the antagonistic effect of TRH on all PB-induced hormonal changes, suggesting that serotoninergic mechanisms may be involved in the extra-pituitary effect of TRH.
在成年雄性大鼠中，在给予戊巴比妥（PB）前5分钟向脑侧脑室注射促甲状腺激素释放激素（TRH），剂量范围为500至5纳克时，可引起与剂量相关的显著催乳素（PRL）释放抑制。在8种缺乏促甲状腺激素释放活性的TRH类似物中，发现6种在脑室内剂量为10微克时可显著抑制PB诱导的PRL分泌，其中在这方面最有效的3种还能够抵消PB引起的生长激素（GH）释放。衍生物[1,3'-二氯甲基2]TRH在脑室内剂量为50纳克时仍有足够的效力来阻断PB诱导的PRL分泌。促肾上腺皮质激素4-10肽无效，而另一种促肾上腺皮质激素衍生物H-甲硫氨酸（氧代2）-谷氨酸-组氨酸-苯丙氨酸-D-赖氨酸-苯丙氨酸-OH（Org 2766）可减少PRL释放。TRH不影响急性应激诱导的血浆PRL升高。α-甲基-对-酪氨酸（α-MT）未能影响TRH对GH分泌的抑制作用，但显著降低了其对PRL释放的抑制作用。对氯苯丙氨酸（PCPA）完全阻断了TRH对所有PB诱导的激素变化的拮抗作用，表明血清素能机制可能参与了TRH的垂体外作用。
