Synthesis and some pharmacological properties of three new bradykinin antagonists

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Title:Synthesis and some pharmacological properties of three new bradykinin antagonists
Creators:
Lammek, Bernard
Wang, Yi-Xin
Gavras, Haralambos
Journal or Publication Title:
Collection of Czechoslovak Chemical Communications, 56, 7, pp. 1539-1544

Abstract

Three new analogues of bradykinin (BK) were designed, synthesized and bio assayed in conscious, unrestrained rats. The analogues were designed by modifying the [D-Arg<sup>0</sup>, Hyp<sup>3</sup>, hi<sup>5,8</sup>, D-Phe<sup>7</sup>]-BK which was previously synthesized by the Steward group and was considered to be one of the most potent antagonists of BK known to date. It has been reported herein that the introduction of additional D-Arg residue or acylation with propionic acid of the N-terminus of [D-Arg<sup>0</sup>, Hyp<sup>3</sup>, Thi<sup>5,8</sup>, D-Phe<sup>7</sup>]BK (model peptide) results in analogues with similar or weaker antagonistic potency as compared to the model, respectively. However, the acylation with 1-adamantaneacetic acid results in an analogue with more than ten times enhanced potency and efficacy. All peptides were synthesized by the solid phase method.

Title:Synthesis and some pharmacological properties of three new bradykinin antagonists
Creators:
Lammek, Bernard
Wang, Yi-Xin
Gavras, Haralambos
Divisions:Life and Chemical Sciences > Institute of Organic Chemistry and Biochemistry > Collection of Czechoslovak Chemical Communications
Journal or Publication Title:Collection of Czechoslovak Chemical Communications
Volume:56
Number:7
Page Range:pp. 1539-1544
ISSN:0010-0765
E-ISSN:1212-6950
Publisher:Institute of Organic Chemistry and Biochemistry
Related URLs:
URLURL Type
http://dx.doi.org/10.1135/cccc19911539UNSPECIFIED
ID Code:5077
Item Type:Article
Deposited On:22 Feb 2010 11:29
Last Modified:22 Feb 2010 10:30

Citation

Lammek, Bernard; Wang, Yi-Xin; Gavras, Haralambos (1991) Synthesis and some pharmacological properties of three new bradykinin antagonists. Collection of Czechoslovak Chemical Communications, 56 (7). pp. 1539-1544. ISSN 0010-0765

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