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Active ingredient: Nicardipine - Chemisty and Biological Activity

Chemisty and Biological Activity

Chemical Formula

C26H29N3O6

Chemical Name

methyl2-(benzyl-methyl-amino)ethyl2,6-dimethyl-4-(3-nitrophenyl)-1,4- dihydropyridine-3,5-dicarboxylate

Chemical Structure

Molecular Weight

479.525 g/mol

Physical State

Solid

Melting Point

136-138 oC

Water Solubility

2.2 mg/L

Isoelectric Point

Not Available

Organisms Affected

Humans and other mammals

Phase 1 Metabolising Enzyme (1-st Step of Metabolism)

CYP3A4

Primary Drug Target
NameVoltage-dependent L-type calcium channel alpha-1C subunit
Gene NameCACNA1C
SynonymsVoltage-dependent L-type calcium channel alpha-1C subunit; Voltage-gated calcium channel alpha subunit Cav1.2; Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle
General FunctionTransport activities
Specific FunctionVoltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1C gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belong to the "high-voltage activated" (HVA) group. They are blocked by dihydropyridines (DHP), phenylalkylamines, benzothiazepines, and by omega-agatoxin-IIIA (omega-Aga-IIIA). They are however insensitive to omega-conotoxin-GVIA (omega-CTx-GVIA) and omega-agatoxin-IVA (omega-Aga-IVA). Calcium channels containing the alpha-1C subunit play an important role in excitation-contraction coupling in the heart. The various isoforms display marked differences in the sensitivity to DHP compounds

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