Role of D-tryptophan for affinity of MEN 10207 tachykinin antagonist at NK2 receptors.

Abstract:

:The role of the D-Trp residues in the sequence of the NK2-selective tachykinin antagonist, MEN 10207 (Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Arg-NH2). has been examined by replacement of each D-Trp with either the L-isomer or the residue naturally occurring in the same position of neurokinin A(4-10). The biological activity of the analogues thus obtained has been characterized, with special attention to the selectivity for the three tachykinin receptors and for the two subtypes of the NK2 receptor recently described. We conclude that the simultaneous presence of the three D-Trp residues of MEN 10207 is crucial both for affinity and for selectivity.

journal_name

Peptides

journal_title

Peptides

authors

Rovero P,Astolfi M,Renzetti AR,Patacchini R,Giachetti A,Maggi CA

doi

10.1016/0196-9781(91)90053-r

subject

Has Abstract

pub_date

1991-09-01 00:00:00

pages

1015-8

issue

5

eissn

0196-9781

issn

1873-5169

pii

0196-9781(91)90053-R

journal_volume

12

pub_type

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