Bopindolol malonate (CAS 62658-64-4)
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Bopindolol malonate is the malonate preparation of Bopindolol, a beta1-AR (beta1-adrenoceptor) antagonist. Bopindolol malonate slowly dissociates into the active metabolites 4-(3-tert-butylamino-2-hydroxypropoxy)-2-methyl indole (18-502) and 4-(3-tert-butylaminopropoxy)-2-carboxyl indole (20-785) which both demonstrate potent beta1-adrenoceptor blocking activity in vitro. The relative potencies of these compounds was determined with a radioligand binding assay, demonstrating 18-502 to be more potent than Bopindolol which is more potent than 20-785. Both Bopindolol and its metabolite 18-502 demonstrate inhibition of H2O2-induced lipid peroxdiation (IC50 = 1.8 muM and 10 muM, respectively) and both demonstrate scavenging of the radical species 1,1-diphenyl-2-picrylhydrazyl. Bopindolol malonate is a potent, non-selective beta adrenoceptor antagonist with long-acting properties. It effectively inhibits lipid peroxidation induced by H2O2.
Bopindolol malonate (CAS 62658-64-4) References
- Fluorometric determination of bopindolol and celiprolol in pharmaceutical preparations and biological fluids. | Belal, F., et al. 2012. J Fluoresc. 22: 1141-50. PMID: 22477063
- Antioxidative action of the beta-adrenoceptor antagonist bopindolol and its metabolite 18-502. | Aniya, Y., et al. 1995. Jpn J Pharmacol. 68: 323-9. PMID: 7474556
- Alpha-1 and beta-adrenergic receptor blocking potencies of bopindolol and its two metabolites (18-502 and 20-785) as assessed by radioligand binding assay methods. | Hosohata, Y., et al. 1995. Gen Pharmacol. 26: 743-7. PMID: 7635249
- Bopindolol is a slowly dissociating beta 1-adrenoceptor antagonist when compared to other beta-blockers. | Hosohata, Y., et al. 1995. Biol Pharm Bull. 18: 1066-71. PMID: 8535397
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Bopindolol malonate, 100 mg | sc-200144 | 100 mg | $92.00 | |||
Bopindolol malonate, 500 mg | sc-200144A | 500 mg | $326.00 |