Literature DB >> 7341523

Cyclic analogue of bradykinin possessing selective and prolonged biological activity.

G I Chipens, F K Mutulis, B S Katayev, V E Klusha, I P Misina, N V Myshlyiakova.   

Abstract

Cyclo-[(N epsilon 1-Lys1, Gly6)-bradykinin] and its deprotected non-cyclic precursor, PheGlyProPheArg LysProProGly, were synthesized using the conventional methods of peptide chemistry. Similar to bradykinin, the cyclopeptide elicits a depressor reaction in rats, as revealed by the experiments in vivo. Its duration of action, however, is greater by several orders of magnitude. At the same time, it appears to exhibit no myotropic activity when applied in vitro to extravasal smooth muscle preparations (uterus and ileum of the rat). The non-cyclic precursor lacks the depressor activity, but produces a slight myotropic effect (alpha = 0.6 +/- 0.09; pD2 = 5.9 +/- 0.17).

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Year:  1981        PMID: 7341523     DOI: 10.1111/j.1399-3011.1981.tb02985.x

Source DB:  PubMed          Journal:  Int J Pept Protein Res        ISSN: 0367-8377


  3 in total

1.  [half-Cys4,half-Cys10]-alpha-Melanocyte-stimulating hormone: a cyclic alpha-melanotropin exhibiting superagonist biological activity.

Authors:  T K Sawyer; V J Hruby; P S Darman; M E Hadley
Journal:  Proc Natl Acad Sci U S A       Date:  1982-03       Impact factor: 11.205

2.  Receptors mediating the increase in vascular permeability to kinins: comparative studies in rat, guinea-pig and rabbit.

Authors:  E T Whalley
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-07       Impact factor: 3.000

3.  The effect of kinin agonists and antagonists on the pain response of the human blister base.

Authors:  E T Whalley; S Clegg; J M Stewart; R J Vavrek
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-12       Impact factor: 3.000

  3 in total

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