Manidipine 2HCl - CAS 89226-75-5
Catalog number:
89226-75-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C35H38N4O6·2HCl
Molecular Weight:
683.62
COA:
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Targets:
Calcium Channel
Description:
Manidipine 2HCl, a HCl salt form of Manidipine, is a calcium channel blocker with IC50 of 2.6 nM.
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Purity:
>98%
Synonyms:
CV-4093
MSDS:
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1.Calcium channel blocking action of franidipine hydrochloride (CV-4093.2HCl) in vitro and in vivo.
Shibouta Y1, Kitayoshi T, Kitoh G, Nishikawa K. Jpn J Pharmacol. 1988 Dec;48(4):463-72.
The calcium-channel blocking action of franidipine (CV-4093.2HCl) was investigated in vitro and in vivo. CV-4093.2HCl inhibited the 60 mM K+-induced contraction of rabbit aorta and those of coronary, renal, mesenteric and femoral arteries of dog less potently than nifedipine and nicardipine. In dog portal and femoral veins, CV-4093.2HCl inhibited K+-induced contraction as potently as nifedipine and nicardipine did. The inhibitory effect of this drug was fully developed by pretreatment for 60 min, and it lasted long after washout. The drug inhibited both K+-induced 45Ca-influx and K+-induced contraction at a similar concentration range in rabbit aorta and dog portal vein, but had no effect on 45Ca-efflux from either vessel. On the other hand, in the isolated, perfused kidneys and mesenteric vascular beds of SHR, CV-4093.2HCl inhibited K+-induced vasoconstriction more effectively than did nifedipine. Moreover, in pithed rats (i.v.) and ganglion-blocked conscious SHR (p.
2.Effects of a new dihydropyridine derivative, CV-4093.2HCl, on renal hemodynamics in spontaneously hypertensive rats.
Nagaoka A1, Shibota M, Hamajo K. Jpn J Pharmacol. 1989 Sep;51(1):25-35.
The effects of a new calcium antagonist, CV-4093.2HCl, on renal hemodynamics were examined in anesthetized and conscious spontaneously hypertensive rats (SHR). In the anesthetized rats, CV-4093.2HCl (5 and 10 micrograms/ kg, i.v.) showed a long-lasting hypotensive action, dilated renal vasculature, and increased renal blood flow. These renal hemodynamic actions of CV-4093.2HCl were more prominent than those of nicardipine (5 and 10 micrograms/kg). Moreover, CV-4093.2HCl (10 micrograms/kg, i.v.) inhibited renal vascular contractions induced by intravenous norepinephrine and angiotensin II. The inhibitory effect of CV-4093.2HCl was much more marked than that of nicardipine, although the inhibitory effects of both calcium antagonists on systemic pressor responses induced by the vasoactive substances were almost the same. In addition, CV-4093.2HCl (1 and 3 mg/kg, p.o.) increased blood flow in the kidneys but not in the other organs except for the small intestine in conscious SHR.
3.Antihypertensive effect of CV-4093.2HCl, a new calcium antagonist, in three rat models of hypertension.
Kakihana M1, Suno M, Nagaoka A. Jpn J Pharmacol. 1988 Oct;48(2):223-8.
The hypotensive action of CV-4093.2HCl (CV-4093), a new calcium antagonist, was studied in spontaneously hypertensive, renal hypertensive, DOCA-salt hypertensive and normotensive rats. CV-4093 (3 and 10 mg/kg, p.o.) dose-dependently decreased systolic blood pressure in the three types of hypertensive rats. At the dose of 10 mg/kg, the compound decreased the blood pressure to the normotensive level between 1 and 3 hr after it was administered; the antihypertensive effect lasted for at least 8 hr. The systolic blood pressure in normotensive rats was also decreased at 3 and 10 mg/kg, p.o., but less evidently than in the hypertensive rats. When the antihypertensive effect of CV-4093 was compared with that of seven known calcium antagonists in spontaneously hypertensive rats, it was the most potent and the most long-lasting.
4.Pharmacokinetics and tolerability of a new manidipine and delapril fixed oral combination in young and elderly subjects.
Stockis A1, De Bruyn S, Gengler C, Goethals F, Lens S, Poli G, Acerbi D. Arzneimittelforschung. 2003;53(8):554-61.
OBJECTIVES: The aim of the present study was to compare the pharmacokinetic and pharmacodynamic properties of a fixed combination tablet containing 10 mg of manidipine dihydrochloride (CAS 89226-75-5), a calcium channel antagonist, and 30 mg of delapril hydrochloride (CAS 83435-67-0), an angiotensin converting enzyme (ACE) inhibitor, during once daily repeated dosing in young and elderly subjects and to assess the bioequivalence of the fixed combination tablet and the single ingredient tablets taken simultaneously in young healthy subjects after a single dose administration.
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CAS 89226-75-5 Manidipine 2HCl

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