一种神经降压素类似物对灌注大鼠心脏中神经降压素诱导的冠状血管收缩的选择性阻断作用。

Selective blockade of neurotensin-induced coronary vessel constriction in perfused rat hearts by a neurotensin analogue.

作者信息

Quirion R, Rioux F, Regoli D, St-Pierre S

出版信息

Eur J Pharmacol. 1980 Feb 8;61(3):309-12. doi: 10.1016/0014-2999(80)90133-8.

Abstract

[D-Trp11]-NT, an analogue of neurotensin (NT) in which Tyr11 was replaced with D-Trp, was found to antagonize selectively NT-induced coronary vessel constriction in perfused rat hearts, in concentrations varying between 1.3 x 10(-7) and 1.1 x 10(-6) M. Higher concentrations of [D-Trp11]-NT displayed NT-like activity. In rat stomach strips and guinea pig atria, [D-Trp11]-NT exhibits full intrinsic activity, markedly reduced affinity for NT receptors, but no inhibitory effect against NT. These results suggest that the receptors mediating the constrictor action of NT in the coronary vessels of rat hearts are pharmacologically distinct from those subserving the stimulant effects of NT in rat stomach strips and guinea pig atria.

摘要

[D-色氨酸11]-神经降压素（[D-Trp11]-NT）是神经降压素（NT）的一种类似物，其中酪氨酸11被D-色氨酸取代，发现在灌注大鼠心脏中，其浓度在1.3×10⁻⁷至1.1×10⁻⁶ M之间时，能选择性拮抗NT诱导的冠状动脉收缩。更高浓度的[D-Trp11]-NT表现出类似NT的活性。在大鼠胃条和豚鼠心房中，[D-Trp11]-NT表现出完全的内在活性，对NT受体的亲和力显著降低，但对NT没有抑制作用。这些结果表明，介导NT在大鼠心脏冠状动脉中收缩作用的受体在药理学上与那些介导NT在大鼠胃条和豚鼠心房中刺激作用的受体不同。