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促甲状腺激素释放激素(TRH)的氟化类似物对心血管系统和催乳素释放的差异作用。

Differential effect of fluorinated analogs of TRH on the cardiovascular system and prolactin release.

作者信息

Feuerstein G, Lozovsky D, Cohen L A, Labroo V M, Kirk K L, Kopin I J, Faden A I

出版信息

Neuropeptides. 1984 Jun;4(4):303-10. doi: 10.1016/0143-4179(84)90004-0.

DOI:10.1016/0143-4179(84)90004-0
PMID:6433221
Abstract

The effects of thyrotropin-releasing hormone (TRH) and the TRH-analogs, 4-fluoro-Im-TRH (4-F-TRH) and 2-trifluoromethyl-Im-TRH (2-TFM-TRH), on the cardiovascular system and prolactin (PRL) release were examined in conscious rats. TRH (2.8 or 28 nmol) injected into the anterior hypothalamus produced dose-dependent increments in blood pressure and heart rate; plasma PRL was increased twofold after the higher dose of TRH. 4-F-TRH had effects similar to those of TRH on both the cardiovascular and PRL response. In contrast, the 2-TFM-TRH was significantly less active than TRH or 4-F-TRH in eliciting tachycardia, yet was noticeably more potent in affecting PRL release. These data suggest that the receptors for TRH-induced PRL release may be different from TRH-receptors which mediate central cardiovascular responses.

摘要

在清醒大鼠中研究了促甲状腺激素释放激素(TRH)及其类似物4-氟-Im-TRH(4-F-TRH)和2-三氟甲基-Im-TRH(2-TFM-TRH)对心血管系统和催乳素(PRL)释放的影响。向下丘脑前部注射TRH(2.8或28 nmol)可使血压和心率呈剂量依赖性增加;较高剂量的TRH使血浆PRL增加两倍。4-F-TRH对心血管和PRL反应的影响与TRH相似。相比之下,2-TFM-TRH诱发心动过速的活性明显低于TRH或4-F-TRH,但在影响PRL释放方面的效力明显更强。这些数据表明,TRH诱导PRL释放的受体可能与介导中枢心血管反应的TRH受体不同。

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Differential effect of fluorinated analogs of TRH on the cardiovascular system and prolactin release.促甲状腺激素释放激素(TRH)的氟化类似物对心血管系统和催乳素释放的差异作用。
Neuropeptides. 1984 Jun;4(4):303-10. doi: 10.1016/0143-4179(84)90004-0.
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The cardiovascular and subjective effects of thyrotropin releasing hormone (TRH) and a stable analogue, dimethyl proline-TRH, in healthy volunteers.促甲状腺激素释放激素(TRH)及其稳定类似物二甲基脯氨酸-TRH对健康志愿者的心血管及主观影响。
Br J Clin Pharmacol. 1995 Sep;40(3):223-9. doi: 10.1111/j.1365-2125.1995.tb05777.x.