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KMID : 0614019890050010053
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Journal of Pharmaceutical Sciences (C.N.U.)
1989 Volume.5 No. 1 p.53 ~ p.60
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Cardiovascular Actions of KR-30006 and KR-1008, a New Dihydropyridine derivatives
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Lee Byung-Ho
Jung Yee-Sook
Kwon Kwang-Il
Zee Ok-Pyo
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Abstract
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KR-1008 and KR-30006 are 1,4-dihydropyridine derivatives, new vasodilatory calcium antagonists from KRICT. Calcium antagonistic properties of the compounds were studied in the isolated heart (Langendorff preparation), pulmonary artery (vasodilation), and in the papillary muscle (negative inotropic effect) of the guinea pig. Antihypertensive effect were also investigated after i.v. or oral administration in the SHR (spontaneously hypertensive rat).
They produced a sigificant inhibition of Ca-induced contraction in the guinea pig pulmonary artery at the concentrations of above 10^-8M. The negative inotropic effect of the electrically stimulated papillary muscle appeared from the concentration of 10^-6M, which is about hundred times higer than the concentration of vasodilation effect. Left ventricular pressure also decreased from the concentration of 3×10^-6M in KR-1008 and KR-3006 in the Langendorff heart preparations.
Coronary flow rate increased from 10^-6M in KR-1008 and nicardipine and appeared no change in KR-30006.
The antihypertensive effect of KR-1008 (EC 20:2.9 ㎍/㎏) was potent more than nicardipine (EC 20:3.4 ㎍/㎏) and than Kr-30006 (EC 20:6.8 ㎍/㎏) was, after i.v. bolus injection in the anesthetized SHR. The antihypertensive effect in the conscious SHR appeared 30 minutes after oral administration of 10 ㎎/㎏ and persisted 4 hrs in KR-1008 and 12 hrs in KR-30006. Heart rate tended to increase for 0.5-1 hr after oral administration of the test compounds.
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KEYWORD
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Dihydropyridine derivatives, guinea pig, calcium antagonistic properties, antihypertensive effect, KR-1008, KR-30006
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