Aranidipine (MPC1304)|Ca2+ channel antagonist

Cas No.:	86780-90-7
Chemical Name:	Aranidipine
Synonyms:	3-Methyl 5-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;MPC-1304;Sapresta;1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-methyl 5-(2-oxopropyl) ester;Asanidipine;3,5-Pyridinedicarboxylicacid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, 3-methyl 5-(2-oxopropyl)ester;3-O-methyl 5-O-(2-oxopropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;Aranidipine;2,6-Dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid methyl 2-oxopropyl ester;MPC1304;DTXCID6028575;Tox21_113003;CAS-86780-90-7;D01562;BS-18193;BCP32584;3,5-DIMETHYL-1-ADAMANTYLZINCBROMIDE;Aranidipine (MPC1304);3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-oxopropyl ester;AC-907;2-oxopropyl 5-(methoxycarbonyl)-2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3-carboxylate;NCGC00182054-03;CCRIS 6724; CCRIS-6724; CCRIS6724; MPC 1304; MPC-1304; MPC1304;HY-U00212;3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(2-NITROPHENYL)-, 3-METHYL 5-(2-OXOPROPYL) ESTER;CS-7341;MPC 1304;CHEMBL2104030;GTPL11744;UNII-4Y7UR6X2PO;Tox21_113003_1;ARANIDIPINE [JAN];DTXSID9048649;(+-)-Acetonyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate;Sapresta (TN);86780-90-7;(+/-)-ACETONYL METHYL 1,4-DIHYDRO-2,6-DIMETHYL-4-(O-NITROPHENYL)-3,5-PYRIDINEDICARBOXYLATE;AKOS015967075;ARANIDIPINE [MART.];ARANIDIPINE [WHO-DD];ARANIDIPINE [MI];Aranidipine [INN];Aranidipine (JAN/INN);CCRIS 6724;CHEBI:31232;FT-0705721;D81791;Q4784109;DB09229;MPC1304;CCRIS-6724;NCGC00182054-02;SCHEMBL49910;4Y7UR6X2PO;Aranidipine (MPC1304)?;DB-090281;GLXC-01783
SMILES:	O=C(C1=C(C)NC(C)=C(C(OCC(C)=O)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
Formula:	C₁₉H₂₀N₂O₇
M.Wt:	388.3713
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	MPC1304 is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
Target:	Ca2+ Channel [1]
In Vivo:	MPC1304 (MPC-1304) is a new Ca2+ channel antagonist in spontaneously hypertensive rats. Following oral administration of MPC1304 at doses of 3 and 10 mg/kg to spontaneously hypertensive rats (SHR), there are significant decreases in Bmax values for specific [3H](+)-PN 200-110 binding to myocardial membranes compared to the control values. The Bmax values at 1 h (3 mg/kg), 1 and 6 h (10 mg/kg) are significantly decreased (47.7, 48.9 and 25.8%, respectively) compared to the control values. The effect is greatest at 1 h and decreases with time. The Bmax values at 6 h (3 mg/kg) and 12 or 24 h (10 mg/kg) after the oral administration of MPC1304 are not significantly different from the control values, suggesting the disappearance of the effect of MPC1304. The Kd values for myocardial [3H](+)-PN 200-110 binding are unaltered by oral administration of MPC1304[1].
Animal Administration:	Rats[1] Male SHR (11-15 weeks) are used. They are fasted for 16 h before the administration of drugs, and given MPC1304 (3, 10 mg/kg) orally through a gastric tube. Control animals are given the vehicle. At 1-24 h after drug administration, the SHR are killed by bleeding from the descending aorta under light anesthesia with ethyl ether, and the myocardium and brain are perfused with 0.9% saline from the aorta. Then, both tissues are removed, and blood vessels are trimmed away. Plasma from rat blood is isolated by centrifugation, and stored at -80°C until the concentration of MPC1304 is determined.
References:	[1]. Nozawa Y, et al. Receptor occupation and pharmacokinetics of MPC-1304, a new Ca2+ channel antagonist, in spontaneously hypertensive rats. Eur J Pharmacol. 1995 Dec 12;287(2):191-6.

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