SYNTHESIS OF [D-ALA2, 4'-I-125-PHE3, GLU4]DELTORPHIN AND CHARACTERIZATION OF ITS DELTA-OPIOID RECEPTOR-BINDING PROPERTIES

被引：4

作者：

FANG, L ^{[1
]}

KNAPP, RJ ^{[1
]}

MATSUNAGA, T ^{[1
]}

WEBER, SJ ^{[1
]}

DAVIS, T ^{[1
]}

HRUBY, VJ ^{[1
]}

YAMAMURA, HI ^{[1
]}

机构：

[1] UNIV ARIZONA, DEPT CHEM, TUCSON, AZ 85721 USA

来源：

LIFE SCIENCES | 1992年 / 51卷 / 20期

关键词：

D O I：

10.1016/0024-3205(92)90628-3

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：

Both [D-Ala2, Glu4]Deltorphin and [D-Ala2, 4'-I-Phe3, Glu4]Deltorphin are highly selective ligands for delta, relative to mu, opioid receptors. Radiolabeled [D-Ala2, 4'-I-125-Phe3, Glu4]Deltorphin ([I-125]Deltorphin) was prepared with a specific activity of 2200 Ci/mmol from [D-Ala2, 4'-NH2-Phe3, Glu4]Deltorphin through a diazonium salt intermediate. The inhibition of [I-125]Deltorphin binding to rat brain membranes by ligands selective for mu, delta, and kappa opioid receptors is consistent with binding by the radioligand to a single site having the properties of a delta opioid receptor. The results of these studies are in good agreement with those obtained by structurally different delta opioid receptor ligands. The similarity between the delta receptor site labeled by [I-125]Deltorphin and those labeled by other delta receptor agonists, in contrast to differences seen by in vivo studies of their analgesic effects, is discussed.

引用

页码：PL189 / PL193

页数：5

共 17 条

[1] CHARACTERIZATION OF [H-3][ 2-D-PENICILLAMINE, 5-D-PENICILLAMINE] ENKEPHALIN BINDING TO DELTA-OPIATE RECEPTORS IN THE RAT-BRAIN AND NEUROBLASTOMA-GLIOMA HYBRID CELL-LINE (NG-108-15) [J].