NEW POTENT ENKEPHALIN ANALOGS CONTAINING TRIFLUOROMETHYL-AMINO ACID RESIDUES

被引：23

作者：

OJIMA, I

KATO, K

JAMEISON, FA

CONWAY, J

NAKAHASHI, K

HAGIWARA, M

MIYAMAE, T

RADUNZ, HE

机构：

[1] FUJI CHEM IND CO LTD,TAKAOKA,TOYAMA 933,JAPAN

[2] E MERCK AG,W-6100 DARMSTADT,GERMANY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(01)81068-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new methionine-enkephalin analogs containing trifluoronorvaline (TFNV) or trifluoronorleucine (TFNL) in place of Gly2 or Gly3 are synthesized. The new analogs bearing (D)-TFNV in place of Gly2 exhibit ca. 100,000 times enhancement in in vivo analgesic activity in comparison with methionine-enkephalin. The in vitro binding assays for mu, delta and kappa receptors reveal that this enhancement is not based on the much stronger binding to these receptors, but mainly due to the extremely efficient inhibition of degradation by aminopeptidase(s).

引用

页码：219 / 222

页数：4