Pharmacodynamic and pharmacological effects of MPC-1304, a new calcium channel blocker, in healthy subjects. Results of multiple oral administration.

Key Words: Aranidipine-Antihypertensive agentxalcium channel antagonist.Calcium antagonists play an important role in the treatment of patients with cardiovascular diseases such as ischemic heart disease, heart failure, and hypertension. The dihydropyridine-type calcium antagonists are widely used to treat hypertension, because of their potent vasodilating activity and weak cardiodepressant action (9,38,11). Aranidipine (MPC-1304) is a novel dihydropyridine-type calcium antagonist, which is characterized by its active metabolites, once daily administration to facilitate patient compliance, and the prospect of good efficacy and safety. In experimental animal models aranidipine had more potent antihypertensive effects than did other dihydropyridines. Administration of aranidipine once daily had a highly potent antihypertensive effect and clinical utility in all of the clinical trials conducted in Japan. Aranidipine is now under registration. In this article, the pharmacological, toxicological, pharmacokinetic profiles, and clinical findings of aranidipine are reviewed. CHEMISTRY Aranidipine was first synthesized by Ohno et al. (24,25). The chemical structures of aranidipine [(+)-methyl 2-oxopropyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate] and its active metabolite, M-1 [2-hydroxypropyl methyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate] , are shown in Fig. 1. Aranidipine has an asymmetric carbon at the C-4 position of the dihydropyridine ring. M-1 has two asymmetric carbons in its structure, and there exist four enantiomers: (S,S)-and (R,R)-M-1 (their mixture is M-l(a)), and (S,R)-and (R,S)-M-1 (their mixture is M-l(P)). The molecular weight of aranidipine (C19Hz,Nz0,) is 388.38, and its melting point is 149-150°C. Aranidipine is freely soluble in acetone and insoluble in water.

show abstract

Aranidipine (MPC‐1304), a New Dihydropyridine Calcium Antagonist: A Review of Its Antihypertensive Action

Ohashi

Ebihara

1996

Cardiovascular Drug Reviews

Self Cite

View full text Add to dashboard Cite

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Pharmacodynamic and pharmacological effects of MPC-1304, a new calcium channel blocker, in healthy subjects. Results of multiple oral administration.

Cited by 1 publication

References 0 publications

Aranidipine (MPC‐1304), a New Dihydropyridine Calcium Antagonist: A Review of Its Antihypertensive Action

Aranidipine (MPC‐1304), a New Dihydropyridine Calcium Antagonist: A Review of Its Antihypertensive Action

Contact Info

Product

Resources

About