Repositioning Candidate Details

Candidate ID: R1253
Source ID: DB09229
Source Type: experimental
Compound Type: small molecule
Compound Name: Aranidipine
Synonyms: Aranidipine
Molecular Formula: C19H20N2O7
SMILES: COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC=C1[N+]([O-])=O)C(=O)OCC(C)=O
Structure:
DrugBank Description: Aranidipine is a novel dihydropyridine derivative that gives rise to two active metabolites (M-1α and M-1β) that exhibit hypotensive activity. It is a calcium antagonist with the formula methyl 2-oxopropyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate. It was developed by Maruko Seiyaku, introduced by Taiho and launched in Japan in 1997.
CAS Number: 86780-90-7
Molecular Weight: 388.376
DrugBank Indication: Aranidipine has been used for many years to treat angina pectoris and hypertension.
DrugBank Pharmacology: Pre-clinical studies with aranidipine and its two metabolites have shown production of increases in femoral blood flow. It has been shown to present potent and long-lasting vasodilating actions. Aranidipine and its metabolites are shown to inhibit calcium-induced contraction in isolated rabbit arteries. Studies have shown that aranidipine is more potent to reduce blood pressure than other dihydropyridines. Aranidipine produce changes in renal blood flow, this effect may be explained by its effect on alpha-2-adrenoreceptor-mediated vasoconstriction.
DrugBank MoA: The high potential of aranidipine is thought to be related to the additional calcium antagonistic activity of its metabolite. The mechanism is thought to be related to the capacity of aranidipine and its metabolites to vasodilate afferent and efferent arterioles. this action is performed through the inhibition of voltage-dependent calcium channels. The typical mechanism of action of aranidipine, as all dihydropyridines, is based on the inhibition of L-type calcium channels, decreasing calcium concentration and inducing smooth muscle relaxation. It is a selective alpha2-adrenoreceptor antagonist which inhibits vasoconstrictive responses.
Targets: Voltage-dependent L-type calcium channel subunit alpha-1C antagonist; Voltage-dependent L-type calcium channel subunit alpha-1D antagonist; Voltage-dependent L-type calcium channel subunit alpha-1F antagonist; Voltage-dependent L-type calcium channel subunit alpha-1S antagonist; Alpha adrenergic receptor agonist
Inclusion Criteria: Indication associated