Nesapidil is a vasodilatory antihypertensive agent primarily acting through α1-adrenergic receptor antagonism and calcium channel blocking activity. Preclinical studies have demonstrated that nesapidil inhibits phenylephrine-induced contractions in isolated rat aortic rings with an IC₅₀ in the low micromolar range, indicative of its α1-adrenoceptor antagonistic effect. Additionally, it reduces calcium-induced contractions in depolarized vascular smooth muscle preparations, supporting its calcium channel blocking properties. In vivo, nesapidil significantly lowers systolic and diastolic blood pressure in spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with effective oral doses ranging from 1 to 10 mg/kg. Its dual mechanism of action makes it a candidate for managing hypertension, although clinical development remains limited.
MedKoo Cat#: 414340
Name: Nesapidil
CAS#: 90326-85-5
Chemical Formula: C23H28N4O4
Exact Mass: 424.2111
Molecular Weight: 424.50
Elemental Analysis: C, 65.08; H, 6.65; N, 13.20; O, 15.08
The following data is based on the product molecular weight 424.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
