Paper Information

Title: 

EVALUATION OF CALCIUM CHANNEL ANTAGONIST ACTIVITY OF SOME NEW 9,10 DIHYDRO- 7H,8H-CHROMENO [4,3-B] CHROMENE-6,11-DIONE BY MEANS OF GUINEA-PIG ILEAL SMOOTH MUSCLE

Type: SPEECH
Author(s): BAGHERI AZAM*,MIRI RAMIN,SHAFIEI ABAS,MOTAMEDI R.,SHARIFI MARYAM
 
 *MEDICINAL AND NATURAL PRODUCTS CHEMISTRY RESEARCH CENTER
 
Name of Seminar: IRANIAN CONGRESS OF PHYSIOLOGY AND PHARMACOLOGY
Type of Seminar:  CONGRESS
Sponsor:  PHYSIOLOGY AND PHARMACOLOGY SOCIETY, MASHHAD UNIVERSITY OF MEDICAL SCIENCE
Date:  2009Volume 19
 
 
Abstract: 

INTRODUCTION: 1,4-dihydropyridines (DHP) compounds are one of the most important classes of Calcium channel blockers (CCBs)that widely use for the treatment of HTN (increase in blood pressure).
MATERIAL & METHOD: Male guinea-pigs weighting 300 - 400 g were killed by a blow on the head. The animal was deprived from food 18 hours before sacrifice but had free access to water. As soon as they were killed the mid part of their ileum was removed and cut into 10-15 mm segments. All the stages of tissue study performed in physiological Tyrod solution. The Calcium Channel Antagonist Activity of compounds was evaluated by using high K+ concentration.(40Mm) in Guinea-Pig ileal longitudinal smooth muscle. This procedure was done by organ bath and Pan lab physiograph and the IC50±SEM of each compound compare with reference drug nifedipine. IC50 determination and statistical calculation were done by curve expert,sigma plot and spss softwareExistence of Cl substitute in meta position in this derivatives studied compounds show the most inhibitory effect and OCH3 substitute decrease Calcium Channel Antagonist Activity effect.
RESULT: Among this derivatives, compound RM-92-1(R1=OCH3,R2,R3=H) show the least [IC50 (2.00±2.00)10-4] and compound RM-81-2(R1,R3=H,R2=Cl) show  the most Calcium Channel Antagonist effect [IC50 (5.99±4.00)10-7]. To prove that DMSO as a solvent and the passage of time had no effect on the ileal contraction, we applied dose response experiments, showing statistically non significant differences.
CONCLUSION: Existence of Cl substitute in meta position in this derivatives studied compounds show the most inhibitory effect and OCH3 substitute decrease Calcium Channel Antagonist Activity effect.

 
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