SMOOTH-MUSCLE EFFECTS OF NEWLY SYNTHESIZED AMINO-METHYL PIPERIDINONES

作者：Mateeva Polina^*; Burdzhiev Nikola; Stanoeva Elena; Baramov Todor; Zamfirova Rositsa

来源：Comptes Rendus de l Academie Bulgare des Sciences, 2010, 63(11): 1675-1680.

• 5-aminomethylpiperidinones
• antihistamine activity
• anti-SP activity

Here, we report the results of the investigation of antihistaminic and anti-SP activity of new 5-aminomethylpiperidinones 2-6. According to the structural requirements for antihistamine and anti-SP activity, the compounds investigated incorporate an amino-group as part of a piperazino substituent (2, 3) or as peptide bond to a tryptophan moiety (4-6). Experiments have been performed on guinea-pig smooth-muscle preparations. The effects of the new compounds on smooth-muscle contractility and their influence on histamine-induced contractions (on ileum segments) and anti-SP activity (on trachea) were tested. All compounds studied (in concentrations 10(-6)M, 10(-5)M, and 10(-4)M) have shown a well-expressed concentration-dependent inhibitory effect on HA-induced ileal contractions, but did not affect the SP-evoked tracheal responses.

• 出版日期2010