Analgesic Effects of 3-Substituted Derivatives of 1,4-Benzodiazepines and their Possible Mechanisms

Мова статті: 
Автор(и) статті: 
V. I. Pavlovsky, O. V. Tsymbalyuk, V. S. Martynyuk, T. A. Kabanova, E. A. Semenishyna, E. I. Khalimova, and S. A. Andronati
Вихідні данні статті: 
Neurophysiology, Vol. 45, Nos. 5/6, 2013
Назва журналу: 
Рік публікації: 
Ключові слова: 
3-substituted 1,4-benzodiazepines, analgesia, smooth muscles of the stomach, edema, tensometric studies, bradykinin (BK) receptors
Ключове слово: 
3-substituted 1,4-benzodiazepines
Ключове слово: 
Ключове слово: 
smooth muscles of the stomach
Ключове слово: 
Ключове слово: 
tensometric studies
Ключове слово: 
bradykinin (BK) receptors
In experiments on mice, we studied the analgesic activity of some 3-substituted derivatives of 1,4-benzodiazepines, including 3-propoxy-7-bromo-5-(2’-chloro)phenyl-1,2-dihydro-3Н-1,4-benzodiazepin-2-one (compound 6). This compound demonstrated clearly pronounced anti-inflammatory and antinociceptive properties in the acetic acid-induced writhing test (induction of visceral pain) in mice, test with carrageenan-induced paw edema in rats, and formalin test in mice. On multicellular preparations of circular smooth muscles from the fundal part of the rat stomach, we estimated the value of affinity of compound 6 (рK В = 6.41). We hypothesize that the mechanism underlying inhibition of bradykinin (BK) receptors by compound 6 is mostly competitive. Therefore, compound 6 can be considered a promising basis for the development and synthesis of antagonists of BK receptors, which can be applied in clinical practice.
Назва підрозділу: 
Кафедра молекулярної біології, біотехнології та біофізики
Pavlovsky_eng.pdf584.43 КБ
ІНСТИТУТ ВИСОКИХ ТЕХНОЛОГІЙ Матеріали дозволено використовувати на умовах GNU FDL без незмінюваних секцій та Creative Commons Attribution/Share-Alike
Дизайн: Інститут високих технологій
Ivan Ivanov