BINDING PROFILE OF BENEXTRAMINE AT NEUROPEPTIDE-Y RECEPTOR SUBTYPES IN RAT-BRAIN AREAS

被引：10

作者：

MELCHIORRE, C ^{[1
]}

ROMUALDI, P ^{[1
]}

BOLOGNESI, ML ^{[1
]}

DONATINI, A ^{[1
]}

FERRI, S ^{[1
]}

机构：

[1] UNIV BOLOGNA,DEPT PHARMACOL,I-40126 BOLOGNA,ITALY

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1994年 / 265卷 / 1-2期

关键词：

NEUROPEPTIDE Y; BENEXTRAMINE; NONPEPTIDE ANTAGONIST; NEUROPEPTIDE Y RECEPTOR SUBTYPE; BINDING AFFINITY;

D O I：

10.1016/0014-2999(94)90228-3

中图分类号：

R9 [药学];

学科分类号：

1007 [药学];

摘要：

Binding studies in rat whole brain, frontoparietal cortex and brainstem membrane preparations revealed that benextramine displaced [H-3]neuropeptide Y specific binding from a low and a high affinity site with IC50 values in the mu M (36 +/- 2, 4.4 +/- 1.4 and 300 +/- 120 mu M, respectively) and the pM (29.3 +/- 12.1, 0.35 +/- 0.11 and 0.42 +/- 0.03 pM, respectively) range, whereas in rat hippocampus benextramine displaced [H-3]neuropeptide Y specific binding from one site only with an IC50 value of 22.8 +/- 5.7 mu M. With the exception of frontoparietal cortex binding assay, benextramine was not able to completely inhibit [H-3]neuropeptide Y specific binding revealing the presence of a benextramine nonsensitive third binding site. Benextramine pretreatment followed by membrane washing demonstrated that benextramine inhibited irreversibly both high and low affinity sites.

引用

页码：93 / 98

页数：6

共 15 条

[1]

BENEXTRAMINE - A LONG-LASTING NEUROPEPTIDE-Y RECEPTOR ANTAGONIST [J].