Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F11%3A00360968" target="_blank" >RIV/61388963:_____/11:00360968 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1002/psc.1351" target="_blank" >http://dx.doi.org/10.1002/psc.1351</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/psc.1351" target="_blank" >10.1002/psc.1351</a>

Result language
angličtina
Original language name
Novel analogues of bradykinin conformationally restricted in the C-terminal part of the molecule
Original language description
Achiral non-coded amino acids (N-benzylglycine, 2-aminomethylphenylacetic acid or 3-aminophenylacetic acid) were substituted at position 7 of the B-2 receptor antagonist [D-Arg(0), Hyp(3), Thi(5,8), D-Phe(7)]-BK. The N-terminal amino group of the analogues was either free or acylated with 1-Aca or Aaa. Biological activity of the compounds was assessed in the in vitro rat uterus test and the in vivo rat blood pressure test. Substitution in position 7 resulted in a decrease in antagonistic potency or change of the activity into agonistic one. Acylation of the N-terminus enhanced antagonistic properties of the resulting peptides in the rat blood pressure test.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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Publication year
2011
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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