正缬氨酸2-促甲状腺激素释放激素的心血管活性与催乳素释放活性的解离

Dissociation of the cardiovascular and prolactin-releasing activities of norvaline2-TRH.

作者信息

Labroo V M, Cohen L A, Lozovsky D, Siren A L, Feuerstein G

机构信息

Laboratory of Chemistry, National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, MD 20892.

出版信息

Neuropeptides. 1987 Jul;10(1):29-36. doi: 10.1016/0143-4179(87)90086-2.

DOI:10.1016/0143-4179(87)90086-2

PMID:3118236

Abstract

The effects of thyrotropin-releasing hormone (TRH) and norvaline2-TRH (Nva2-TRH) on blood pressure, heart rate and plasma prolactin levels in conscious rats have been compared. Systemic injection of TRH or Nva2-TRH (1 mg/kg or 5 mg/kg) produced equipotent increases in plasma prolactin. On the other hand, while TRH significantly increases blood pressure and heart rate, Nva2-TRH was essentially inactive. Thus, two contrasting analogues are now available: 4-NO2-Im-TRH (Neuropeptides, 8, 63, 1986) has full cardiovascular activity and no PRL-releasing activity, while Nva2-TRH has no cardiovascular activity and full PRL-releasing activity of TRH.

摘要

已比较促甲状腺激素释放激素（TRH）和去缬氨酸2-TRH（Nva2-TRH）对清醒大鼠血压、心率及血浆催乳素水平的影响。全身注射TRH或Nva2-TRH（1毫克/千克或5毫克/千克）可使血浆催乳素产生同等程度的升高。另一方面，虽然TRH能显著升高血压和心率，但Nva2-TRH基本无活性。因此，现在有两种截然不同的类似物：4-NO2-Im-TRH（《神经肽》，8卷，63页，1986年）具有完全的心血管活性且无催乳素释放活性，而Nva2-TRH无心血管活性且具有TRH的完全催乳素释放活性。