RX 77368（促甲状腺激素释放激素的一种稳定类似物）在体内激发催乳素和促甲状腺激素分泌的能力。

The ability of RX 77368 - a stabilised analogue of TRH - to provoke the secretion of prolactin and TSH in vivo.

作者信息

Dettmar P W, Lynn A G, Metcalf G, Clifford J M

出版信息

Neuropeptides. 1982 Oct;3(1):1-8. doi: 10.1016/0143-4179(82)90060-9.

Abstract

RX 77368, a stabilised analogue of TRH, has been evaluated for its ability to provoke the release of TSH and prolactin in vivo after intravenous administration to rats and human volunteers. The analogue caused a dose-related release of TSH in both species. In rats the compound caused release of prolactin but the dose-response relationship was bi-phasic, so that large doses caused only a diminished response. The prolactin response in human volunteers was equivocal and further experiments will be necessary to define the effect. Despite its greater biological stability the potency, efficacy and duration of effect with RX 77368 was similar to that of TRH in both species. The manner in which further endocrine investigations may aid the clinical development of RX 77368 is discussed.

摘要

RX 77368是促甲状腺激素释放激素（TRH）的一种稳定类似物，已对其在静脉注射给大鼠和人类志愿者后，在体内激发促甲状腺激素（TSH）和催乳素释放的能力进行了评估。该类似物在两个物种中均引起了与剂量相关的TSH释放。在大鼠中，该化合物引起了催乳素的释放，但剂量-反应关系呈双相性，因此大剂量仅导致反应减弱。人类志愿者中的催乳素反应不明确，需要进一步实验来确定其作用。尽管RX 77368具有更高的生物稳定性，但其在两个物种中的效力、功效和作用持续时间与TRH相似。文中讨论了进一步的内分泌研究可能有助于RX 77368临床开发的方式。