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Diproteverine HCl

Catalog No. T68853   CAS 69373-88-2

Diproteverine HCl is a novel calcium antagonist with antianginal properties, antispasmodic and vasoactive.

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Diproteverine HCl Chemical Structure
Diproteverine HCl, CAS 69373-88-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 195.00
5 mg In stock $ 430.00
10 mg In stock $ 636.00
25 mg In stock $ 987.00
50 mg In stock $ 1,360.00
100 mg In stock $ 1,830.00
500 mg In stock $ 3,680.00
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Purity: 99.44%
Purity: 99.38%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Diproteverine HCl is a novel calcium antagonist with antianginal properties, antispasmodic and vasoactive.
In vitro Diproteverine (1 μM; sheep Purkinje fibers) to reduce the amplitude of the slow action potential (IC30 = 2 μM) and to shorten the duration of the fast action potential at 50% repolarisation (IC30 = 2.5 μM). Papaverine was found to possess marginal membrane channel-blocking activity and to be much more potent than diproteverine as a cAMP-phosphodiesterase inhibitor (IC50 = 8 μM).[2]
In vivo Diproteverine (0.25-0.75 mg/kg; i.e.; dog; at plasma levels within the assumed therapeutic range) dose-relatedly decreases heart rate, increases corrected sinus node recovery time, and decreases Wenckebach point. These effects are observed at plasma levels ranging between 16.2 +/- 4.1 and 144.7 +/- 12.5 ng/ml. After cholinergic blockade with N-methylscopolammonium, diproteverine lowers heart rate (greater than or equal to 0.25 mg/kg), increases corrected sinus node recovery time, and decreases Wenckebach point (greater than or equal to 0.5 mg/kg). After propranolol, diproteverine only significantly reduces corrected sinus node recovery time 5 min after the third administration (0.75 mg/kg). After pharmacologic autonomic blockade by N-methylscopolammonium propranolol combination, diproteverine lowers the intrinsic heart rate (greater than or equal to 0.25 mg/kg) and Wenckebach point (greater than or equal to 0.5 mg/kg). Diproteverine does not modify mean blood pressure. These results show that diproteverine administered with and without pharmacologic autonomic blockade in the conscious dog causes dose-related depressant effects on sinus node function and atrioventricular conduction without producing significant vasodilatation.[1]
Molecular Weight 462.02
Formula C26H36ClNO4
CAS No. 69373-88-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (119.04 mM)

TargetMolReferences and Literature

1. Kantelip JP, et al. Effects of diproteverine, a new calcium antagonist on sinoatrial node and atrioventricular conduction in conscious unsedated dogs. J Cardiovasc Pharmacol. 1988;12(4):432-437. 2. Lacroix P, et al. Diproteverine (BRL 40015): a new type of calcium antagonist with potential antianginal properties. Eur J Pharmacol. 1991;192(3):317-327. 3. Ridings JE, et al. Prenatal toxicity studies in rats and rabbits with the calcium channel blocker diproteverine. Reprod Toxicol. 1996;10(1):43-49.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Diproteverine HCl 69373-88-2 Membrane transporter/Ion channel Metabolism Calcium Channel Diproteverine hydrochloride inhibitor inhibit

 

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