Orphanin FQ: Receptor binding and analog structure activity relationships in rat brain

被引：89

作者：

Dooley, CT ^{[1
]}

Houghten, RA ^{[1
]}

机构：

[1] TORREY PINES INST MOL STUDIES,SAN DIEGO,CA 92121

来源：

LIFE SCIENCES | 1996年 / 59卷 / 01期

关键词：

orphanin FQ; nociceptin; analog; receptor binding assay;

D O I：

10.1016/0024-3205(96)00261-5

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

A tritiated form of orphanin FQ (a heptadecapeptide also known as Nociceptin) has been prepared. This radioligand (33 Ci/mmole) was used to develop a radioreceptor assay using rat brain homogenates. Binding was observed to be saturable, and analyses of the binding data indicate the presence of a single binding site with a dissociation constant of 5 +/- 1.1 nM and Bmax of 535 +/- 85 fmoles/mg protein. Thirty-four analogues of orphanin FQ, including a complete alanine ''scan'' of orphanin FQ, and truncation analogues from both the N- and C- terminals were synthesized and tested. The data obtained indicate that the N-terminus plays a more critical role in binding than the C-terminus and that residues 1, 2, 4, and 8 are essential for binding.

引用

页码：PL23 / PL29

页数：7

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