A NON-OPIOID PATTERN CHARACTERIZES INHIBITION OF GROWTH-HORMONE RELEASING PEPTIDE BINDING BY DYNORPHIN-RELATED PEPTIDES

被引：10

作者：

CODD, EE ^{[1
]}

ALOYO, VJ ^{[1
]}

WALKER, RF ^{[1
]}

机构：

[1] MED COLL PENN,DEPT PHARMACOL,PHILADELPHIA,PA 19129

来源：

NEUROPEPTIDES | 1990年 / 15卷 / 03期

关键词：

D O I：

10.1016/0143-4179(90)90144-N

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

GHRP-6 (His-D-Trp-Ala-Trp-D-Phe-LysNH2; SK&F 110679) is a hexapeptide that specifically releases growth hormone. Although derived from methionine enkephalin, 3H-SK&F 110679 binding profiles suggest that it retains little mu or delta opioid activity. In the present study, dynorphin A was a potent inhibitor of SK&F 110679 binding. However, detailed structure-activity studies using dynorphin-related compounds suggest that the interaction between SK&F 110679 and dynorphin was non-opioid in nature. The non-opioid peptide des-Tyr-dynorphin was virtually as potent an inhibitor of 3H-SK&F 110679 binding as the intact dynorphin peptide. Additionally, the non-peptide, kappa selective ligand U-50,488 was a very weak inhibitor of 3H-SK&F 110679 binding. Since dynorphin but not U-50,488 has been reported to release growth hormone, the present results suggest that a non-opioid dynorphin site participates in SK&F 110679's growth hormone releasing action. © 1990.

引用

页码：133 / 137

页数：5

共 23 条

[1] PEPTIDE-INDUCED EXCESSIVE GROOMING IN THE RAT - THE ROLE OF OPIATE RECEPTORS [J].

ALOYO, VJ ;

SPRUIJT, B ;

ZWIERS, H ;

GISPEN, WH .

PEPTIDES, 1983, 4 (06) :833-836

[2] ON THE INVITRO AND INVIVO ACTIVITY OF A NEW SYNTHETIC HEXAPEPTIDE THAT ACTS ON THE PITUITARY TO SPECIFICALLY RELEASE GROWTH-HORMONE [J].

BOWERS, CY ;

MOMANY, FA ;

REYNOLDS, GA ;

HONG, A .

ENDOCRINOLOGY, 1984, 114 (05) :1537-1545

[3]

CHAO CC, 1988, LIFE SCI, V42, P701

[4] SPECIFIC RECEPTOR FOR THE OPIOID PEPTIDE DYNORPHIN - STRUCTURE-ACTIVITY-RELATIONSHIPS [J].

CHAVKIN, C ;

GOLDSTEIN, A .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1981, 78 (10) :6543-6547

[5] U50,488 - A KAPPA-SELECTIVE AGENT WITH POOR AFFINITY FOR MU-1 OPIATE BINDING-SITES [J].

CLARK, JA ;

PASTERNAK, GW .

NEUROPHARMACOLOGY, 1988, 27 (03) :331-332

[6] BINDING OF GROWTH HORMONE-RELEASING HORMONES AND ENKEPHALIN-DERIVED GROWTH HORMONE-RELEASING PEPTIDES TO MU-OPIOID AND DELTA-OPIOID RECEPTORS IN FOREBRAIN OF RAT [J].

CODD, EE ;

YELLIN, T ;

WALKER, RF .

NEUROPHARMACOLOGY, 1988, 27 (10) :1019-1025

[7]

CODD EE, 1989, IN PRESS NEUROPHARMA

[8] DYNORPHIN-RELATED PEPTIDES CAUSE MOTOR DYSFUNCTION IN THE RAT THROUGH A NON-OPIATE ACTION [J].

FADEN, AI ;

JACOBS, TP .

BRITISH JOURNAL OF PHARMACOLOGY, 1984, 81 (02) :271-276

[9] DYNORPHIN(1-13), A LONG-LASTING INHIBITOR OF OPIATE RECEPTOR-BINDING INVITRO [J].

GARZON, J ;

JEN, MF ;

SANCHEZBLAZQUEZ, P ;

LEE, NM .

LIFE SCIENCES, 1982, 31 (16-1) :1789-1792

[10] BINDING SELECTIVITY PROFILES FOR LIGANDS OF MULTIPLE RECEPTOR TYPES - FOCUS ON OPIOID RECEPTORS [J].

GOLDSTEIN, A .

TRENDS IN PHARMACOLOGICAL SCIENCES, 1987, 8 (12) :456-459

← 1 2 3 →