Oxodipine

Oxodipine, a dihydropyridine-type calcium antagonist, inhibits KCl-induced aortic contraction in rabbits and reduces cardiac force in less potent rat ventricular test-paper contractions. In rat cultured neonatal ventricular myocytes, Oxodipine reduces L-type Ca currents (I) with an IC50 of 0.24 μM, and against T-type Ca currents (I) with an IC50 of 0.41 μM. Oxodipine causes constipation in mice and gingival hyperplasia in dogs[1][2][3][4][5][6].

This dihydropyridine-class calcium ion blocker (FW = 359.37 g/mol; CAS 90729-41-2), also known as 4-(1,3-benzodioxol-4-yl)-2,6-dimethyl-1,4- dihydropyridine-3,5-dicarboxylic acid O3 -ethyl,O5 -methyl ester, greatly depresses KCl-induced contraction of rabbit aorta and also decreases the contractile force of rat ventricular strips, the latter with lower potency. Oxodipine markedly shortens cardiac action potentials, and, in rat cultured neonatal ventricular myocytes, oxodipine decreases the L-type Ca2+ current (ICaL) with IC50 of 0.24 μM and is also an effective blocker of T-type Ca2+ current (ICaT) than elgodipine (IC50 = 0.41 μM).

[1] Nyska A, et al. Gingival hyperplasia in rats induced by oxodipine‐a calcium channel blocker[J]. Journal of Periodontal Research, 1990, 25(2): 65-68. DOI:10.1111/j.1600-0765.1990.tb00893.x
[2] Tamargo J, et al. Effects of oxodipine on 45Ca movements and contractile responses in vascular smooth muscle[J]. British journal of pharmacology, 1989, 97(2): 339. DOI:10.1111/j.1476-5381.1989.tb11959.x
[3] Galán L, et al. Characteristics of Ca2+ channel blockade by oxodipine and elgodipine in rat cardiomyocytes[J]. European journal of pharmacology, 1998, 357(1): 93-105. DOI:10.1016/s0014-2999(98)00543-3
[4] Egros F, et al. An original intragastric delivery system for oral administration of solid formulations to fully conscious rats: its application to oxodipine studies[J]. European Journal of Drug Metabolism and Pharmacokinetics, 1991: 71-76. PMID:1820939
[5] Montastruc P, et al. Effect of oxodipine, a novel dihydropyridine calcium channel blocker, in neurogenic hypertensive dogs[J]. Archives internationales de pharmacodynamie et de thérapie, 1993, 321: 57-62. PMID:8323416
[6] Tejerina T, et al. Effects of oxodipine on isolated rabbit aorta and mesenteric resistance vessels[J]. European journal of pharmacology, 1992, 219(2): 279-284. DOI:10.1016/0014-2999(92)90306-o