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Analgesic activity of new derivatives of quinazolinone -4

[Experimental medicine]
Eleonora Manvelyan; Mikael Manvelyan; Ivan Kodonidi; Eduard Oganesian;

In the of study was investigated the antinociceptive action of derivatives of quinazolinone-4 in 187 male and 196 female rats, including females rats in the different stages of the estrous cycle: diestrus ½ and proestrus /estrus in models of nociceptive responses induced by chemical stimuli (formalin test, «acetic cramps»), to assess the level of organization of the peripheral pain sensation. Substances (laboratory code numbers: PGFA – I, II, III, IV, V, VI, VII) at a dose of 2/10 of the molecular weight in mg/kg, reference drugs: metamizole sodium and lidocaine was administered once intraperitoneally 40 minutes before administration of chemical irritants. Control and males received respectively solubilizate Tween-80 and saline (0.4 ml intraperitoneally) under similar conditions. The 4-quinazolinone derivatives compounds I–IV, VI, VII were investigated as potential analgesics. Substance I–IV, VI, VII exhibited analgesic activity in male and female rats. Substances I, VI, VII have analgesic effects on female rats in phase of the estrous cycle diestrus ½; substance I–IV, VI – in the stage of proestrus/estrus. Among the investigated derivatives of quinazolinone-4 compound VI is a leader in analgesic activity.

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Keywords: derivatives of quinazolinone-4, analgesic effect, formalin test, acetic cramps


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