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Bopindolol (malonate)

(Synonyms: (±)-Bopindolol (malonate)) 目录号 : GC42966

A β-adrenergic receptor antagonist

Bopindolol (malonate) Chemical Structure

Cas No.:82857-38-3

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100mg
¥1,062.00
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500mg
¥4,249.00
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产品描述

Bopindolol is a non-selective β-adrenergic receptor antagonist. In vivo, bopindolol decreases heart rate and blood pressure and attenuates ischemia-induced myocardial acidosis in dogs. Formulations containing bopindolol have been used to treat essential and renovascular hypertension.

Chemical Properties

Cas No. 82857-38-3 SDF
别名 (±)-Bopindolol (malonate)
Canonical SMILES O=C(O)CC(O)=O.O=C(OC(COC1=CC=CC2=C1C=C(C)N2)CNC(C)(C)C)C3=CC=CC=C3
分子式 C23H28N2O3•C3H4O4 分子量 484.5
溶解度 Water: 5mM 储存条件 Store at -20°C, protect from light
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1 mM 2.064 mL 10.3199 mL 20.6398 mL
5 mM 0.4128 mL 2.064 mL 4.128 mL
10 mM 0.2064 mL 1.032 mL 2.064 mL
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Research Update

Beta-blocking potency and selectivity of Bopindolol and its two metabolites for beta 1- and beta 2-adrenergic receptors as assessed by radioligand binding assay

J Pharmacobiodyn 1991 May;14(5):250-5.PMID:1685186DOI:10.1248/bpb1978.14.250.

Using a radioligand binding assay, we assessed the affinity and selectivity of the antagonistic effects of Bopindolol (4-(benzoyloxy-3-tert-butylaminopropyl)-2-methylindole hydrogen-malonate) and its two metabolites, (18-502, (4-(3-tert-butylamino-2-hydroxypropoxy)-2-methyl indole) and 20-785, (4-(3-tert-butylaminopropoxy)-2-carboxyl indole], for beta 1- and beta 2-adrenoceptors and on 5HT1B-receptors in rat brain and heart. In addition, we also determined the pA2 values of these agents for their antagonistic effects toward positive chronotropic and inotropic actions (beta 1-adrenoceptors) and for their antagonistic effects toward isolated tracheal relaxation (beta 2-adrenoceptors), using isoproterenol as an agonist. The data showed that Bopindolol was more selective for beta 2-adrenoceptors than for beta 1-adrenoceptors and 5HT1B-receptors, but its two metabolites (18-502 and 20-785) did not have significant selectivity for beta 1- and beta 2-adrenoceptors, using both [3H]CGP12177 and [125I]ICYP ([125I]iodocyanopindolol) bindings. In contrast, the results from pharmacological assessment for antagonistic potencies, using atria and trachea, showed that Bopindolol and its two metabolites did not have significant selectivity on beta 1- and beta 2-adrenoceptors. A major metabolite of Bopindolol, 18-502, had higher pKi and pA2 values for beta-adrenoceptors and 5HT1B-receptors than those of Bopindolol and 20-785. These results indicate, first, that a radioligand binding assay for the assessment of the selectivity of Bopindolol and its two metabolites for beta 1- and beta 2-adrenoceptors is more effective than pharmacological experiments, and that there is a possibility that its two metabolites also contribute to the strong beta-blocking action of Bopindolol.

Fluorometric determination of Bopindolol and celiprolol in pharmaceutical preparations and biological fluids

J Fluoresc 2012 Jul;22(4):1141-50.PMID:22477063DOI:10.1007/s10895-012-1053-1.

Two sensitive fluorometric methods were developed for the determination of both Bopindolol malonate (BOP) and celiprolol HCl (CLP) based on measuring their native fluorescence in methanol and acetonitrile, respectively. For BOP, the fluorescence was measured at 316 nm after excitation at 278 nm. The proposed method was successfully applied to the assay of commercial tablets as well as content uniformity testing. For CLP, the fluorescence was enhanced by the addition of carboxymethylcellulose solution and measured at 455 nm after excitation at 339 nm. The method was successfully applied to the analysis of CLP in tablets and biological fluids. In both methods, interference likely to be introduced from co-formulated, co-administered, or chemically related drugs was studied. The results were statistically compared with those obtained by reference methods and were found to be in good agreement.