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GW1229是一种新型神经肽Y Y1受体拮抗剂,可抑制仓鼠微循环中神经肽Y的血管收缩作用。

GW1229, a novel neuropeptide Y Y1 receptor antagonist, inhibits the vasoconstrictor effect on neuropeptide Y in the hamster microcirculation.

作者信息

Bitran M, Daniels A J, Boric M P

机构信息

Departamento de Fisiología, Facultad de Ciencias Biológicas, Pontificia Universidad Católica de Chile, Santiago 1, Chile.

出版信息

Eur J Pharmacol. 1997 Jan 14;319(1):43-7. doi: 10.1016/s0014-2999(96)00832-1.

DOI:10.1016/s0014-2999(96)00832-1
PMID:9030896
Abstract

We studied the effect of GW1229, a novel neuropeptide Y Y1 receptor antagonists, on the vasoconstriction induced by neuropeptide Y and structurally related analogs in the hamster cheek pouch microcirculation. Changes in arteriolar diameter and microvascular conductance were assessed by intravital microscopy and measurement of sodium22 clearance. GW1229 did not affect basal vascular conductance but inhibited, concentration dependently, the reduction in arteriolar diameter and vascular conductance induced by 100 nM neuropeptide Y. GW1229 also counteracted the vasoconstrictor effect of 100 nM [Leu31,Pro34]neuropeptide Y, and that of 300 nM neuropeptide Y-[(13-36). In contrast, GW1229 had no effect on the vasoconstriction induced by noradrenaline. We conclude that the vasoconstrictor effect on neuropeptide Y in the hamster cheek pouch is mediated by neuropeptide Y Y1 receptors. The maintenance of physiological tone in this vascular bed does not involve the participation of endogenous neuropeptide Y.

摘要

我们研究了新型神经肽Y Y1受体拮抗剂GW1229对仓鼠颊囊微循环中神经肽Y及结构相关类似物诱导的血管收缩的影响。通过活体显微镜检查和测量22钠清除率来评估小动脉直径和微血管传导率的变化。GW1229不影响基础血管传导率,但浓度依赖性地抑制100 nM神经肽Y诱导的小动脉直径减小和血管传导率降低。GW1229还可对抗100 nM [Leu31,Pro34]神经肽Y以及300 nM神经肽Y-[(13-36)]的血管收缩作用。相比之下,GW1229对去甲肾上腺素诱导的血管收缩没有影响。我们得出结论,仓鼠颊囊中神经肽Y的血管收缩作用是由神经肽Y Y1受体介导的。该血管床生理张力的维持不涉及内源性神经肽Y的参与。

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Eur J Pharmacol. 1997 Jan 14;319(1):43-7. doi: 10.1016/s0014-2999(96)00832-1.
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