Effect of New Derivatives of Dihydropyridine on Rat Ileal Smooth Muscle in Vitro
محل انتشار: مجله دانشگاه علوم پزشکی کرمان، دوره: 9، شماره: 1
سال انتشار: 1382
نوع سند: مقاله ژورنالی
زبان: فارسی
مشاهده: 45
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شناسه ملی سند علمی:
JR_JKMU-9-1_002
تاریخ نمایه سازی: 19 اسفند 1402
چکیده مقاله:
In this research we evaluated the calcium channel antagonist activity of various diester analohues of nifedipine on rat ileal smooth muscle.in these analogues,the orthophenyl group at position ۴ was replaced by ۱ methyl ۲-meythylsulfonyl or methylthio ۵-imidazolyl.wistar rats(۱۸۰-۲۵۰g) were killed by a blow to the head.the intestine was removed above the ileucecal junction and longitudinal smooth muscle segments of ۲ cm length were maintained at ۳۷c in a ۱۰ ml jacket organ bath containing oxygenated intestinal krebs soluion.the contractions was recorded with a force displacement transducer connected to a physiograp.the contraction was elisited with ۸۰ mmol KCL.test compounds were cumulatively added to produse ۵۰% relaxation of contracted ileal smooth muscle (IC۵۰) THAT WAS DETERMINED FROM THE CINCENTRATION response trace recorded by physiograph.the IC۵۰ of nifedipine was (۱.۲۶+-۰.۳۷)*۱۰ and of compounds ۱,۲,۳,۴,۵ and ۶ was(۲.۵۷+_۰.۲۸)*۱۰,(۱.۰۳+_۰.۱۲)*۱۰,(۲.۵۵+_۰.۵۰)*۱۰,(۱.۳۲+_۰.۱۸)*۱۰,(۳.۱۶+_۰.۸۹)*۱۰, and (۱.۰۴+_۰.۲۹)*۱۰ mole respectively.the results indicate that replacement of ۲_ nitrophenyl at C۴ position of nifedipine with methyltion or methyl solfunyl imidazolyl reduces the activity.the comparison of the activites of symetrical esters(compounds No ۳&۶) indicated that increasing the length of methylen chain in C۳ and C۵ esters substituend decreases the avtivity.Comparison of the activities of asymetrical esters(compounds No۴&۵) indicates that,when at C۳ there is a small substituent,increasing the length of methylen chain increases activity.comparison of the activites of symetrical esters(compounds ۲ and ۳) with asymetrical esters(compounds ۱,۴.۵ and ۶) indicates that asymetrical esters are not always more potent than symmetrical esters.compound ۴ was the most potent new compound in this study.finally we can conclude that nifedipine was significantely more potent than all of these compounds.
کلیدواژه ها:
نویسندگان
M Rezvanipour
Assistant professor
H Sepehri
Associate professor
A.R Foromandi
Associate professor
GH.R Sepehri
Associate professor
H Najafi pour
Instructor
F Esmaeili
Other