LIPOPHILIC PEPTIDES - SYNTHESIS OF LAUROYL THYROTROPIN-RELEASING-HORMONE AND ITS BIOLOGICAL-ACTIVITY

被引：46

作者：

MURANISHI, S

SAKAI, A

YAMADA, K

MURAKAMI, M

TAKADA, K

KISO, Y

机构：

[1] YOSHITOMI PHARMACEUT IND LTD, RES LABS, FUKUOKA 871, JAPAN

[2] KYOTO PHARMACEUT UNIV, DEPT MED CHEM, YAMASHINA KU, KYOTO 607, JAPAN

来源：

PHARMACEUTICAL RESEARCH | 1991年 / 8卷 / 05期

关键词：

PEPTIDE DELIVERY; LIPOPHILIC PEPTIDE; THYROTROPIN-RELEASING HORMONE (TRH); LIPOPHILICITY; LAUROYL DERIVATIVE;

D O I：

10.1023/A:1015869126771

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Thyrotropin-releasing hormone (TRH) was derivatized by chemical attachment of lauric acid to the N-terminal pyroglutamyl group. The product was confirmed to be more lipophilic than TRH by high-performance liquid chromatography and measurement of partition coefficients. The central nervous system activity and endocrine activity of the lauroyl derivative were only slightly reduced, to 81 and 64% of the parent TRH, respectively. Lipophilic derivatization may be generally applicable to transmembrane delivery of peptides.

引用

页码：649 / 652

页数：4

共 14 条

[1]

Adibi S. A., 1981, PHYSL GASTROINTESTIN, P1073

[2] ZWEI UNIVERSALREAGENTIEN ZUR DUNNSCHICHTCHROMATOGRAPHIE [J].