Evaluation of myorelaxant activity of 7-substituted hexahydroquinoline derivatives in isolated rabbit gastric fundus

GÜNDÜZ, MİYASE; Ozturk, GÖKÇE; Vural, Ismail; ŞİMŞEK, RAHİME; Sarioglu, Yusuf; Safak, Cihat

doi:10.1016/j.ejmech.2007.04.012

Evaluation of myorelaxant activity of 7-substituted hexahydroquinoline derivatives in isolated rabbit gastric fundus

Atıf İçin Kopyala

GÜNDÜZ M. G., Ozturk G. S., Vural I. M., ŞİMŞEK R., Sarioglu Y., Safak C.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, cilt.43, sa.3, ss.562-568, 2008 (SCI-Expanded)

Yayın Türü: Makale / Tam Makale
Cilt numarası: 43 Sayı: 3
Basım Tarihi: 2008
Doi Numarası: 10.1016/j.ejmech.2007.04.012
Dergi Adı: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Sayfa Sayıları: ss.562-568
Gazi Üniversitesi Adresli: Evet

Özet

In this article, 16 new methyl(ethyl) 4-(dichlorophenyl)-2,7-dimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates and methyl(ethyl) 2-methyl-4-(dichlorophenyl)-5-oxo-7-phenyl-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate derivatives have been synthesized by the Hantzsch reaction and screened for their myorelaxant and potassium channel opening activities. The maximum relaxant effects (E-max) and pD(2) values on exogenous noradrenaline precontracted tissues and inhibitory effects on cholinergic neurotransmission of the compounds and pinacidil were determined on isolated strips of rabbit gastric fundus smooth muscle. Obtained results indicated that some compounds and pinacidil produced concentration-dependent relaxation on rabbit gastric fundus smooth muscle strips in the two test conditions. (c) 2007 Elsevier Masson SAS. All rights reserved.