非肽类神经肽Y Y1受体拮抗剂BIBP3226可阻断[亮氨酸31，脯氨酸34]神经肽Y诱导的大鼠孤束核中α2肾上腺素能受体的调节。

The non-peptide neuropeptide Y Y1 receptor antagonist BIBP3226 blocks the [Leu31,Pro34]neuropeptide Y-induced modulation of alpha 2-adrenoceptors in the nucleus tractus solitarii of the rat.

作者信息

Yang S N, Finnman U B, Fuxe K

机构信息

Department of Neuroscience, Karolinska Institute, Stockholm, Sweden.

出版信息

Neuroreport. 1996 Nov 4;7(15-17):2701-5. doi: 10.1097/00001756-199611040-00059.

DOI:10.1097/00001756-199611040-00059

PMID:8981451

Abstract

The potential blockade of the neuropeptide Y (NPY) Y1 receptor agonist [Leu31,Pro34]NPY-induced modulation of the characteristics of alpha 2-adrenoceptor agonist [3H]p-aminoclonidine binding sites by a selective non-peptide NPY Y1 receptor antagonist BIBP3226, was studied in the nucleus tractus solitarii of the rat by means of quantitative receptor autoradiography. [Leu31,Pro34]NPY at a concentration of 10 nM significantly increased the Kd value of [3H]p-aminoclonidine binding sites in the nucleus tractus solitarii without influencing the Bmax, suggesting the existence of an antagonistic modulation by NPY Y1 receptors of alpha 2-adrenoceptors in the nucleus tractus solitarii. BIBP3226 at 100 nM fully blocked the [Leu31,Pro34]NPY-induced increase in Kd of the [3H]p-aminoclonidine binding sites. The present results therefore provide evidence, by use of a NPY Y1 receptor antagonist, for the existence of a NPY Y1/alpha 2 receptor interaction in the nucleus tractus solitarii.

摘要

采用定量受体放射自显影术，在大鼠孤束核中研究了选择性非肽类神经肽Y（NPY）Y1受体拮抗剂BIBP3226对神经肽Y（NPY）Y1受体激动剂[Leu31，Pro34]NPY诱导的α2肾上腺素能受体激动剂[3H]对氨基可乐定结合位点特性调节的潜在阻断作用。浓度为10 nM的[Leu31，Pro34]NPY显著增加了孤束核中[3H]对氨基可乐定结合位点的解离常数（Kd）值，而不影响最大结合容量（Bmax），这表明孤束核中NPY Y1受体对α2肾上腺素能受体存在拮抗调节作用。100 nM的BIBP3226完全阻断了[Leu31，Pro34]NPY诱导的[3H]对氨基可乐定结合位点Kd值的增加。因此，本研究结果通过使用NPY Y1受体拮抗剂，为孤束核中存在NPY Y1/α2受体相互作用提供了证据。