Ethaverine hydrobromide
Ethaverine hydrobromide is a Papaverine derivative and vasodilator. Ethaverine hydrobromide inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrobromide blocks L-type Ca2+ channels, reduces intracellular Ca2+ levels, inhibits platelet adhesion and aggregation, regulates cardiac conduction and heart rate, and increases peripheral and cerebral blood flow. Ethaverine hydrobromide alters cochlear microcirculation, intracochlear Po2, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrobromide is used in the research of peripheral vascular diseases.
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- CAS No.: 855701-63-2
- Formule: C24H30BrNO4
- Masse moléculaire:476.40
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Stockage:
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
L-type calcium channel |
MAO-B |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PC-12 | IC50 |
2 μM
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Inhibition of 70 mM K+-induced catecholamine secretion in undifferentiated rat pheochromocytoma PC12 cells measured via scintillation counting of [3H]norepinephrine release, with preincubation and co-incubation with ethaverine during stimulation periods.
Inhibition of 70 mM K+-induced catecholamine secretion in undifferentiated rat pheochromocytoma PC12 cells measured via scintillation counting of [3H]norepinephrine release, with preincubation and co-incubation with ethaverine during stimulation periods.
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8161356 |
In Vitro
Ethaverine (0.3-30 μM) hydrobromide reduces open probability (EC50 ≈ 1 μM) and unitary current amplitude by ~20% in dihydropyridine-sensitive L-type calcium channels from porcine cardiac muscle incorporated into planar lipid bilayers, with near-complete inhibition at 30 μM[4].
Ethaverine hydrobromide inhibits binding of [3H]nitrendipine (Ki ≈ 8.5 μM), [3H]diltiazem (Ki = 1-2 μM), and [3H]verapamil (Ki = 1-2 μM) to porcine cardiac sarcolemma membranes[4].
Ethaverine (1-10 μM) hydrobromide concentration-dependently inhibits K+-induced catecholamine secretion in PC12 cells with an IC50 of ~2 μM, has maximal inhibitory activity at 10 μM, and does not affect bradykinin-induced secretion[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:anesthetized[6]
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Dosage:1 mg/kg
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Administration:i.v.
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Result:Inhibited atrioventricular conduction and heart rate.
Showed partial persistence of inhibitory action, especially at the atrioventricular level, after total cardiac denervation.
Chemical Information
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CAS No. 855701-63-2
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Masse moléculaire 476.40
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Formule C24H30BrNO4
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SMILES
CCOC1=CC(C=CN=C2CC3=CC=C(C(OCC)=C3)OCC)=C2C=C1OCC.Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureté et documentation
Références
[1]. Lee SS, et al. Inhibitory effects of ethaverine, a homologue of papaverine, on monoamine oxidase activity in mouse brain. Biological & pharmaceutical bulletin. 2001 Jul;24(7):838-40. [Content Brief]
[2]. Shin JS, et al. Inhibitory effects of ethaverine, a homologue of papaverine, on dopamine content in PC12 cells. Biological & pharmaceutical bulletin. 2001 Jan;24(1):103-5. [Content Brief]
[3]. Prazma J, et al. Effect of ethaverine hydrochloride on cochlear microcirculation. Archives of otolaryngology (Chicago, Ill. : 1960). 1981 Apr;107(4):227-9. [Content Brief]
[4]. Wang Y, et al. Ethaverine, a derivative of papaverine, inhibits cardiac L-type calcium channels. Molecular pharmacology. 1991 Nov;40(5):750-5. [Content Brief]
[5]. Suh BC, et al. Inhibition by ethaverine of catecholamine secretion through blocking L-type Ca2+ channels in PC12 cells. Biochemical pharmacology. 1994 Mar 29;47(7):1262-6. [Content Brief]
[6]. Lacroix P, et al. Activit comparée de l'ethavérine et de la papavérine sur les fonctions cardiaques chronotrope et dromotrope chez le chien anesthésié [Comparative activity of ethaverine and papaverine on chronotropic and dromotropic cardiac functions in the anesthetized dog]. Arch Int Pharmacodyn Ther. 1976 May;221(1):163-76. French. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ethaverine hydrobromide Related Classifications
HY-B1440A Related Classifications
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Keywords
- Ethaverine
- 855701-63-2
- Drug Derivative
- Phosphodiesterase (PDE)
- Calcium Channel
- Tyrosine Hydroxylase
- Monoamine Oxidase
- porcine cardiac sarcolemma membranes
- guinea pigs
- porcine cardiac L-type Ca++ channel
- MAO
- tyrosine hydroxylase
- phosphodiesterase
- MAO-B
- PC12 cells
- anesthetized dogs
- neural cells
- Inhibitor
- inhibitor
- inhibit