[Effect of efonidipine hydrochloride (NZ-105), a new dihydropyridine calcium antagonist, on the experimental atherosclerosis in cholesterol-fed rabbits].
We studied the effect of efonidipine hydrochloride [NZ-105:(+-)-2-[benzyl(phenyl)amino]ethyl 1,4-dihydro-2,6-dimethyl-5- (5,5-dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-4-(3-nitrophenyl )-3-pyridine-carboxylate hydrochloride ethanol], a newly synthesized dihydropyridine calcium antagonist, on atherosclerosis in 1% cholesterol-fed rabbits. NZ-105 (10, 30 and 100 mg/kg) was orally administered to the animals twice a day for 10 weeks. NZ-105 did not cause any significant change in the plasma lipid levels. The area of atherosclerotic lesion was reduced by 37% (P < 0.05) in the aortic arch and by 54% (P > 0.05) in the thoracic aorta of rabbits administrated 100 mg/kg of NZ-105. The content of cholesterol ester in the aorta was also reduced by 64% (P < 0.05) in the aortic arch and by 73% (P > 0.05) in the thoracic aorta. These results suggest that NZ-105 may suppress the development of atherosclerosis without affecting the plasma lipids.
Toyoda
K
K
Shiraoka Research Station of Biological Science, Nissan Chemical Industries, Ltd., Saitama, Japan.
Kitahara
M
M
Yamashita
T
T
Shudo
C
C
Masuda
Y
Y
Sakashita
M
M
Tanaka
S
S
Saito
Y
Y
D000818:Animals; D001011:Aorta / Q000737:chemistry; D001018:Aortic Diseases / Q000473:pathology / Q000517:prevention & control; D001161:Arteriosclerosis / Q000097:blood / Q000473:pathology / Q000517:prevention & control*; D002118:Calcium / Q000037:antagonists & inhibitors*; D002784:Cholesterol / Q000032:analysis; D002791:Cholesterol, Dietary; D004036:Diet, Atherogenic; D004095:Dihydropyridines / Q000494:pharmacology*; D008055:Lipids / Q000097:blood; D009596:Nitrophenols; D009943:Organophosphorus Compounds / Q000494:pharmacology*; D011817:Rabbits
D002791:Cholesterol, Dietary; D004095:Dihydropyridines; D008055:Lipids; D009596:Nitrophenols; D009943:Organophosphorus Compounds; C066425:efonidipine; D002784:Cholesterol; D002118:Calcium