product name Amiodarone HCl
Description: Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator that is used to treat various types of cardiac dysrhythmias. Amiodarone HCl has shown a non-competitive inhibition of the chronotropic effect of isoproterenol with a pD’ value of ~4.17. In addition, Amiodarone HCl has been reported to inhibit the norepinephrine-induced contractions in a non-competitive type with a pD’ value of about 4.06.
References: Cardiovasc Res. 1997 Jul;35(1):13-29.
681.77
Formula
C25H29I2NO3.HCl
CAS No.
19774-82-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 23 mg/mL (33.7 mM)
Water: <1 mg/mL
Ethanol: 11 mg/mL (16.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19395498
| In Vitro |
In vitro activity: Amiodarone possesses an inhibitory effect on the fast sodium channel as well as on the slow calcium channel. Amiodarone also has non-competitive antisympathetic effects, and modulates thyroid function and phospholipid metabolism. Amiodarone penetrates deeply into the lipid matrix of the membrane, and is released from cardiac tissues very slowly when washed out. Amiodarone (44–88 μM) depresses Vmax of guinea pig papillary muscle without affecting the resting membrane potential, and that this Vmax inhibition is enhanced in a frequency- or use-dependent manner like Class I antiarrhythmic drugs. Amiodarone (50–88 μM) is also found to suppress the depolarization-induced spontaneous action potentials (abnormal automaticity) in ventricular muscles and in Purkinje fibers. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Amiodarone (1.25–25 mg/kg) results in a decrease in sinus rate, a prolongation of effective and functional refractory periods of the atrioventricular node, and a frequency-dependent conduction delay in the atrioventricular node and in the ventricle of anesthetized dogs. Amiodarone (50 mg/kg/day, i.p. for 3–4 weeks) results in significant decreases in the current density of iK and ito in ventricular cells without affecting iCa and iK1 densities in rabbit. Amiodarone (AM) inhibits intracellular conversion from thyroxine (T4) to triiodothyronine (T3) via 5′-deiodination (5′DI) without affecting intracellular conversion from T4 to reverse T3 (rT3). |
| Animal model | |
| Formulation & Dosage | |
| References | Cardiovasc Res. 1997 Jul;35(1):13-29. |
Related Posts
product name Amiodarone HCl
Description: Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator that is used to treat various types of cardiac dysrhythmias. Amiodarone HCl has shown a non-competitive inhibition of the chronotropic effect of isoproterenol with a pD’ value of ~4.17. In addition, Amiodarone HCl has been reported to inhibit the norepinephrine-induced contractions in a non-competitive type with a pD’ value of about 4.06.
References: Cardiovasc Res. 1997 Jul;35(1):13-29.
681.77
Formula
C25H29I2NO3.HCl
CAS No.
19774-82-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 23 mg/mL (33.7 mM)
Water: <1 mg/mL
Ethanol: 11 mg/mL (16.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19395498
| In Vitro |
In vitro activity: Amiodarone possesses an inhibitory effect on the fast sodium channel as well as on the slow calcium channel. Amiodarone also has non-competitive antisympathetic effects, and modulates thyroid function and phospholipid metabolism. Amiodarone penetrates deeply into the lipid matrix of the membrane, and is released from cardiac tissues very slowly when washed out. Amiodarone (44–88 μM) depresses Vmax of guinea pig papillary muscle without affecting the resting membrane potential, and that this Vmax inhibition is enhanced in a frequency- or use-dependent manner like Class I antiarrhythmic drugs. Amiodarone (50–88 μM) is also found to suppress the depolarization-induced spontaneous action potentials (abnormal automaticity) in ventricular muscles and in Purkinje fibers. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Amiodarone (1.25–25 mg/kg) results in a decrease in sinus rate, a prolongation of effective and functional refractory periods of the atrioventricular node, and a frequency-dependent conduction delay in the atrioventricular node and in the ventricle of anesthetized dogs. Amiodarone (50 mg/kg/day, i.p. for 3–4 weeks) results in significant decreases in the current density of iK and ito in ventricular cells without affecting iCa and iK1 densities in rabbit. Amiodarone (AM) inhibits intracellular conversion from thyroxine (T4) to triiodothyronine (T3) via 5′-deiodination (5′DI) without affecting intracellular conversion from T4 to reverse T3 (rT3). |
| Animal model | |
| Formulation & Dosage | |
| References | Cardiovasc Res. 1997 Jul;35(1):13-29. |