product name Dronedarone HCl
Description: Dronedarone (slao known as SR33589) HCl is an amiodarone analogue which has been used as an effective and promising treatment for Atrial fibrillation (AF). Dronedarone works as a multichannel blocker targeting potassium channel, sodium channel and calcium channel. In vitro, dronedarone has been demonstrated to inhibit muscarinic acetylcholine receptor-operated K+ current IK(ACh) induced by carbachol or GTP-gamma-S with IC50 values of 10nm and <100nm, respectively, in cells isolated from guinea pig atria.
References: J Cardiovasc Pharmacol. 2000;36(6):802-5; Br J Pharmacol. 2001;133(5):625-34.
593.22
Formula
C31H44N2O5S.HCl
CAS No.
141625-93-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (134.9 mM)
Water: <1 mg/mL
Ethanol: 40 mg/mL (67.4 mM)
Solubility (In vivo)
Synonyms
SR33589
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403921
| In Vitro |
In vitro activity: Dronedarone reduces the incidence of early and delayed after depolarizations evoked by 1 mM Dofetilide and 0.2 mM Strophantidine in Purkinje fibres. Dronedarone (10 mM) markedly reduces the L-type calcium current (76.5%) and the rapid component of the delayed rectifier potassium current (97%) in ventricular myocytes. Dronedarone inhibits the activity of I(K(ACh)) channels recorded from cell-attached patches by reducing the channel open probability (from 0.56 to 0.11) without modification of the single-channel conductance in single cells isolated from sinoatrial node (SAN) tissue of rabbit hearts. Dronedarone exhibits a state-dependent inhibition of the fast Na(+) channel current with an IC50 of 0.7 μM in guinea pig ventricular myocytes, when the holding potential (V (hold)) is -80 mV. Dronedarone blocks Ca(2+) currents elicited by rectangular pulses at V (hold) = -40 mV with IC50 value of 0.4 μM, whereas at V (hold) = -80 mV, Dronedarone (10 μM) blocks only 20 % of the current. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Dronedarone increases action potential duration in normal hearts of rats. Dronedarone reduces the late sustained K(+) current, I(K) (or Isus) by 69%. Dronedarone induces only a tonic block of I(K). Dronedarone induces a weak increase in the fast transient outward current, I(to), in rats after myocardial infarction. |
| Animal model | |
| Formulation & Dosage | |
| References | Br J Pharmacol. 2001 Jul;133(5):625-34; Br J Pharmacol. 2001 Jul;133(5):625-34; J Pharmacol Exp Ther. 2000 Jan;292(1):415-24. |
Related Posts
product name Dronedarone HCl
Description: Dronedarone (slao known as SR33589) HCl is an amiodarone analogue which has been used as an effective and promising treatment for Atrial fibrillation (AF). Dronedarone works as a multichannel blocker targeting potassium channel, sodium channel and calcium channel. In vitro, dronedarone has been demonstrated to inhibit muscarinic acetylcholine receptor-operated K+ current IK(ACh) induced by carbachol or GTP-gamma-S with IC50 values of 10nm and <100nm, respectively, in cells isolated from guinea pig atria.
References: J Cardiovasc Pharmacol. 2000;36(6):802-5; Br J Pharmacol. 2001;133(5):625-34.
593.22
Formula
C31H44N2O5S.HCl
CAS No.
141625-93-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (134.9 mM)
Water: <1 mg/mL
Ethanol: 40 mg/mL (67.4 mM)
Solubility (In vivo)
Synonyms
SR33589
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403921
| In Vitro |
In vitro activity: Dronedarone reduces the incidence of early and delayed after depolarizations evoked by 1 mM Dofetilide and 0.2 mM Strophantidine in Purkinje fibres. Dronedarone (10 mM) markedly reduces the L-type calcium current (76.5%) and the rapid component of the delayed rectifier potassium current (97%) in ventricular myocytes. Dronedarone inhibits the activity of I(K(ACh)) channels recorded from cell-attached patches by reducing the channel open probability (from 0.56 to 0.11) without modification of the single-channel conductance in single cells isolated from sinoatrial node (SAN) tissue of rabbit hearts. Dronedarone exhibits a state-dependent inhibition of the fast Na(+) channel current with an IC50 of 0.7 μM in guinea pig ventricular myocytes, when the holding potential (V (hold)) is -80 mV. Dronedarone blocks Ca(2+) currents elicited by rectangular pulses at V (hold) = -40 mV with IC50 value of 0.4 μM, whereas at V (hold) = -80 mV, Dronedarone (10 μM) blocks only 20 % of the current. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Dronedarone increases action potential duration in normal hearts of rats. Dronedarone reduces the late sustained K(+) current, I(K) (or Isus) by 69%. Dronedarone induces only a tonic block of I(K). Dronedarone induces a weak increase in the fast transient outward current, I(to), in rats after myocardial infarction. |
| Animal model | |
| Formulation & Dosage | |
| References | Br J Pharmacol. 2001 Jul;133(5):625-34; Br J Pharmacol. 2001 Jul;133(5):625-34; J Pharmacol Exp Ther. 2000 Jan;292(1):415-24. |