Zolertine is an alpha-adrenergic receptor antagonist that acts as an antihypertensive agent. Its effect was studied in animals in vivo and in vitro. Zolertine considerably decreased systemic blood pressure in mecamylamine hypertensive dogs in a dose-related fashion. Competition binding experiments using the alpha1-adrenoceptor antagonist [3H] prazosin showed a zolertine pKi of 6.81 +/- 0.02 in rat liver (alpha1B-adrenoceptors) and 6.35 +/- 0.04 in rabbit liver (alpha1A-adrenoceptors) membranes. Zolertine showed higher affinity for alpha1D-adrenoceptors compared to alpha1A-adrenoceptors, while it had an intermediate affinity for alpha1B-adrenoceptors. The ability of the alpha1-adrenoceptor antagonist zolertine to block alpha1D-adrenoceptor-mediated constriction in different vessels of Wistar Kyoto (WKY) and spontaneously hypertensive (SHR) rats may explain its antihypertensive efficacy despite its low order of potency.
MedKoo Cat#: 559304
Name: Zolertine HCl
CAS#: 7241-94-3
Chemical Formula: C13H19ClN6
Exact Mass:
Molecular Weight: 294.79
Elemental Analysis: C, 52.97; H, 6.50; Cl, 12.03; N, 28.51
The following data is based on the product molecular weight 294.79 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 |
