Evaluation of myorelaxant activity of 7-substituted hexahydroquinoline derivatives in isolated rabbit gastric fundus.
In this article, 16 new methyl(ethyl) 4-(dichlorophenyl)-2,7-dimethyl-5-oxo-l,4,5,6,7,8-hexahydroquinoline-3-carboxylates and methyl(ethyl) 2-methyl-4-(dichlorophenyl)-5-oxo-7-phenyl-l,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.
Gündüz
Miyase Gözde
MG
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey.
Sevim Oztürk
Gökçe
G
Vural
Ismail Mert
IM
Simşek
Rahime
R
Sarioğlu
Yusuf
Y
Safak
Cihat
C
D000818:Animals; D004353:Drug Evaluation, Preclinical; D005748:Gastric Fundus / Q000187:drug effects* / Q000502:physiology*; D066298:In Vitro Techniques; D009126:Muscle Relaxation / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D009638:Norepinephrine / Q000494:pharmacology; D020110:Pinacidil / Q000494:pharmacology; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits
D011804:Quinolines; D020110:Pinacidil; D009638:Norepinephrine