CHARACTERIZATION OF NK-3 BINDING-SITES IN RAT AND GUINEA-PIG CORTICAL MEMBRANES BY THE SELECTIVE LIGAND [H-3] SENKTIDE

被引：27

作者：

RENZETTI, AR ^{[1
]}

BARSACCHI, P ^{[1
]}

CRISCUOLI, M ^{[1
]}

LUCACCHINI, A ^{[1
]}

机构：

[1] IST POLICATTEDRA DISCIPLINE BIOL,PISA,ITALY

来源：

NEUROPEPTIDES | 1991年 / 18卷 / 03期

关键词：

D O I：

10.1016/0143-4179(91)90101-N

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

We have used [H-3] Senktide, a selective Neurokinin B receptor ligand, for the characterization of NK-3 receptors in rat and guinea pig CNS membranes. Scatchard analysis of saturation binding studies in cerebral cortex membranes indicated that this ligand bound to a single site with apparent high affinity (K(D) = 4.6 +/- 1.6 and 3.1 +/- 0.37 nM, Bmax = 13.7 +/- 1.6 and 21.8 +/- 2.2 fmol/mg protein in rat and guinea pig membranes, respectively). However, in competition studies with a group of neurokinins and related peptides two different rank orders of affinities were obtained, as follows: NKB > [MePhe7]-NKB greater-than-or-equal-to Arg0-NKB greater-than-or-equal-to Senktide >> NKA > SP, in rat membranes, and [MePhe7]NKB > Senktide = NKB > Arg0-NKB >> SP > NKA, in guinea pig membranes.

引用

页码：107 / 114

页数：8

共 23 条

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[2]

BERGSTROM L, 1987, MOL PHARMACOL, V32, P764

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