Comparison of the Effect of Substances (VN 008 a VN 014) from the Group of Quinazoline Derivatives on the Model of Isolated Trachea

Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Zuzana Pramuková Supervisor: PharmDr. Marie Vopršalová, CSc. Title of thesis: Comparison of the effect of substances (VN 008 a VN 014) from the group of quinazoline derivatives on the model of isolated trachea. The aim of this study was to determine the structural relaxation activity of quinazoline variations on the isolated rat's tracheal smooth muscle (in vitro). Synthetic substances VN 008 (N-(2-morfolinoetyl) quinazolin-4-amin) and VN 014 (4 - [3 - (piperidin- 1-yl) propyloxy] quinazoline) are derived from alkaloids obtained from the Justicia Adhatoda shrub (vasicine and vasicinone). The isolated trachea, after a previous contraction of carbachol in a concentration of 10-5M, we studied the cumulative relaxation of single doses of the test compounds VN 008 and VN 014. The results obtained (ED50 values ± SEM [mmol / l]) shows that both the test substances induced relaxation of tracheal smooth muscle. Substance VN 008 is comparable with standard active substance theophylline. Greater effects shows derivative with propyloxy fragment VN 014. Keywords: asthma, Justicia Adhatoda, vasicine, vasicinone, theophylline