Ligand id: 2524

Name: nisoldipine

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View more information in the IUPHAR Pharmacology Education Project: nisoldipine

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 8
Topological polar surface area 107.77
Molecular weight 388.16
XLogP 4.99
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used in the treatment of hypertension, either alone or in combination with other antihypertensive drugs.
Mechanism Of Action and Pharmacodynamic Effects
Nisoldipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes, by means of three mechanisms: deforming calcium channels, inhibiting ion-control gating mechanisms and and interfering with the release of calcium from the sarcoplasmic reticulum. This results in a decrease in intracellular calcium which inhibits the contractile processes of the myocardial smooth muscle, which leads to dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure and decreased afterload.
Due to the complex nature of this drug's MMOA, and the paucity of (human) affinity data, we do not tag a primary drug target.
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