A NEW APPROACH TO ENHANCE BIOAVAILABILITY OF BIOLOGICALLY-ACTIVE PEPTIDES - CONJUGATION OF A DELTA-OPIOID AGONIST TO BETA-CYCLODEXTRIN

被引：23

作者：

HRISTOVAKAZMIERSKI, MK

HORAN, P

DAVIS, P

YAMAMURA, HI

KRAMER, T

HORVATH, R

KAZMIERSKI, WM

PORRECA, F

HRUBY, VJ

机构：

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

[2] UNIV ARIZONA,DEPT PHARMACOL,TUCSON,AZ 85721

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(00)80675-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The cyclic delta opioid agonist [p-I-Phe4]DPDPE, 1, was conjugated to mono-6-amino-permethyl-beta-cyclodextrin at the C-terminus to improve the bioavailability of 1. In the rat brain binding assay, the conjugate 8 showed an IC50 = 134 nM vs. a delta ligand and IC50 > 10 muM at the mu receptor, making it less potent and selective than 1. However, 8 shows antinociceptive properties (i.v.) in the mouse tail flick test and prolonged activity.

引用

页码：831 / 834

页数：4

共 8 条

[1] SYNTHESIS OF CHEMICALLY MODIFIED CYCLODEXTRINS [J].