Samsonova V M, Babichev V N, Shvachkin Iu P, Smirnova A P
Probl Endokrinol (Mosk). 1980 Mar-Apr;26(2):48-52.
Comparative study of hormonal and antihypnotic activity of thyrotropine releasing hormone (TRH) and of its two analogues: pyroglutamine-serine-leucine amide (A-1) and pyroglutamine-serine-glycine amide (A-2) was carried out on male rats. Along with hormonal activity, TRH possessed distinct antagonistic action against nembutal, diminishing its toxicity. In the group of control animals given nembutal and physiological saline the LD50 for nembutal constituted 5.75 mg/100 g. Administration of TRH in a dose of 0.5 mg/kg increased this index to 8.0 mg/100 g, and in a dose of 1 mg/kg--to 11 mg/100 g. The analogues under study failed to influence the TRH secretion of the hypophysis, but differed in respect to their action on nembutal: A-1 decreased nembutal toxicity more intensively than TRH, whereas A-2 was ineffective. The problem of the neutropic action of TRH and A-1 is discussed.
对雄性大鼠进行了促甲状腺激素释放激素（TRH）及其两种类似物：焦谷氨酰-丝氨酰-亮氨酰胺（A-1）和焦谷氨酰-丝氨酰-甘氨酰胺（A-2）的激素活性和抗催眠活性的比较研究。除激素活性外，TRH对戊巴比妥具有明显的拮抗作用，可降低其毒性。在给予戊巴比妥和生理盐水的对照动物组中，戊巴比妥的半数致死量（LD50）为5.75mg/100g。以0.5mg/kg的剂量给予TRH可使该指标增至8.0mg/100g，以1mg/kg的剂量给予则增至11mg/100g。所研究的类似物对垂体的促甲状腺激素释放激素分泌没有影响，但在对戊巴比妥的作用方面存在差异：A-1比TRH更强烈地降低戊巴比妥毒性，而A-2则无效。讨论了TRH和A-1的中性作用问题。
