Effect of 3-substituted 1,4-benzodiazepin-2-ones on bradykinin-induced smooth muscle contraction

Biochemical properties of 3-substituted 1,4-benzodiazepine determined by the characteristics of their chemical structure. Influence of 3-substituted 1,4-benzodiazepin-2-ones on maximal normalized rate and amplitudes of isometric smooth muscle contraction in rats was investigated. Compounds MX-1775 a...

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Bibliographic Details
Published in:Ukrainian biochemical journal 2017, Vol.89 (1), p.31-37
Main Authors: Virych, P A, Shelyuk, O V, Kabanova, T A, Khalimova, E I, Martynyuk, V S, Pavlovsky, V I, Andronati, S A
Format: Article
Language:English
Subjects:
3-substituted 1_4-benzodiazepin-2-ones
Animals
Benzodiazepines - chemical synthesis
Benzodiazepines - chemistry
Benzodiazepines - pharmacology
bradykinin
Bradykinin - analogs & derivatives
Bradykinin - metabolism
Bradykinin - pharmacology
Dose-Response Relationship, Drug
force of contracti
Isometric Contraction - drug effects
Isometric Contraction - physiology
Male
maximal normalized rate
Muscle, Smooth - drug effects
Muscle, Smooth - physiology
Rats
Receptor, Bradykinin B2 - metabolism
Stomach - drug effects
Stomach - physiology
Structure-Activity Relationship
Tissue Culture Techniques
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Summary:Biochemical properties of 3-substituted 1,4-benzodiazepine determined by the characteristics of their chemical structure. Influence of 3-substituted 1,4-benzodiazepin-2-ones on maximal normalized rate and amplitudes of isometric smooth muscle contraction in rats was investigated. Compounds MX-1775 and MX-1828 demonstrated the similar inhibition effect on bradykinin-induced contraction of smooth muscle like competitive inhibitor des-arg9-bradykinin-acetate to bradykinin B2-receptors. MX-1626 demonstrated unidirectional changes of maximal normalized rate and force of smooth muscle that proportionally depended on bradykinin concentration in the range 10-10-10-6 M. MX-1828 has statistically significant decrease of normalized rate of smooth muscle contraction for bradykinin concentrations 10-10 and 10-9 M by 20.7 and 8.6%, respectively, but for agonist concentration 10-6 M, this parameter increased by 10.7% and amplitude was reduced by 29.5%. Compounds MX-2011, MX-1785 and MX-2004 showed no natural effect on bradykinin-induced smooth muscle contraction. Compounds MX-1775, MX-1828, MX-1626 were selected for further research of their influence on kinin-kallikrein system and pain perception.
ISSN:2409-4943
2409-4943
DOI:10.15407/ubj89.01.031