STRUCTURE-ACTIVITY STUDY OF THE C-TERMINAL RESIDUE OF MEN-10207 TACHYKININ ANTAGONIST

被引：9

作者：

ROVERO, P

QUARTARA, L

ASTOLFI, M

PATACCHINI, R

GIACHETTI, A

MAGGI, CA

机构：

[1] A MENARINI PHARMACEUT,DEPT CHEM,I-50131 FLORENCE,ITALY

[2] A MENARINI PHARMACEUT,DEPT PHARMACOL,I-50131 FLORENCE,ITALY

[3] MENARINI SUD,DEPT PHARMACOL,POMEZIA,ITALY

来源：

PEPTIDES | 1992年 / 13卷 / 01期

关键词：

NEUROKININ-A; NK-2 TACHYKININ RECEPTOR SUBTYPES; TACHYKININ ANTAGONISTS;

D O I：

10.1016/0196-9781(92)90164-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The role of the C-terminal residue in the sequence of the NK-2- selective tachykinin antagonist, MEN 10207 (Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Arg-NH2). has been examined by systematic amino acid substitutions. Biological activity has been measured on two in vitro preparations chosen as paradigms of the recently described NK-2 receptor subtypes, namely the rabbit pulmonary artery and the hamster trachea, in order to define the structural requirements necessary for antagonist subtype selectivity. We conclude that in the presence of a C-terminal hydrophilic residue, affinity is maximal for the NK-2A subtype. while hydrophobic. bulky and aromatic residues increase affinity for the NK-2B subtype.

引用

页码：207 / 208

页数：2

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