Quinidine hydrochloride
Quinidine hydrochloride is an orally active antiarrhythmic agent. Quinidine hydrochloride reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride can be used in studies related to uterine sarcoma and seizures.
For research use only. We do not sell to patients.
- CAS No.: 1668-99-1
- Formula: C20H25ClN2O2
- Molecular Weight:360.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Quinidine (10 μM; 24 h) hydrochloride potentiates Paclitaxel (HY-B0015)-induced cytotoxicity in P-gp-positive MES-SA/DX5 uterine sarcoma cells (reducing paclitaxel IC50 to 80.56 nM) but does not alter paclitaxel cytotoxicity in P-gp-negative MES-SA uterine sarcoma cells[1].
Quinidine (10 μM; 24 h) hydrochloride significantly increases the sub-G1 apoptotic portion in paclitaxel-treated P-gp-positive MES-SA/DX5 uterine sarcoma cells, enhancing paclitaxel-induced apoptosis[1].
Quinidine inhibits the in vitro metabolism of Debrisoquine in rat liver microsomes, with lower potency than observed in human liver microsomes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:P-gp-negative MES-SA uterine sarcoma cells, P-gp-positive MES-SA/DX5 uterine sarcoma cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Did not significantly alter the cytotoxicity of paclitaxel in MES-SA cells, with paclitaxel IC50 remaining comparable to paclitaxel alone (19 nM vs. 18 nM).
Strongly potentiated paclitaxel-induced cytotoxicity in MES-SA/DX5 cells, reducing the IC50 of paclitaxel from 13851 nM to 81 nM.
Showed no significant cytotoxicity up to 100 μM in either cell line.\nShowed concentration-dependent cytotoxicity with docetaxel against MES-SA cells.
Enhanced docetaxel-induced cytotoxicity in MES-SA/DX5 cells more potently than hydrocinchonine, alongside cinchonine.
Showed no significant cytotoxicity up to 100 μM in either cell line.
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Cell Line:P-gp-positive MES-SA/DX5 uterine sarcoma cells (paclitaxel-treated)
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly increased the sub-G1 apoptotic portion (G0 = 27.19) in paclitaxel-treated MES-SA/DX5 cells, whereas paclitaxel alone induced minimal sub-G1 accumulation (G0 = 0.05).
Quinidine (10-30 mg/kg; intraperitoneal injection; single administration) hydrochloride significantly elevates the threshold of pentylenetetrazol-induced tonic convulsions in male NMRI mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis (male, 175-225 g)[3]
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Dosage:80 mg/kg
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Administration:p.o.; single dose
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Result:Reduced urinary excretion of p-hydroxyamphetamine to 7.2% of vehicle-control levels in the 0-24 h collection period.
Reduced urinary excretion of p-hydroxyamphetamine to 24.1% of vehicle-control levels in the 24-48 h collection period.
Increased amphetamine excretion to 542% of control levels in the 24-48 h period.
Excreted an average of 0.40 μmol p-hydroxyamphetamine and 7.80 μmol amphetamine in the 0-24 h period.
Excreted an average of 3.60 μmol amphetamine and a significantly reduced amount of p-hydroxyamphetamine relative to controls in the 24-48 h period.
Achieved total combined excretion of amphetamine and p-hydroxyamphetamine over 48 h equal to 79.7% of the administered dose, which was not significantly different from control groups.
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Animal Model:NMRI (male, 5-6 weeks old, 25-30 g)[4]
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Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg
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Administration:i.p.; single dose
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Result:Did not alter the pentylenetetrazole threshold dose for onset of myoclonic twitch.
Significantly increased the pentylenetetrazole threshold dose for onset of tonic hind limb extension compared to saline-treated controls (p < 0.05).
Chemical Information
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CAS No. 1668-99-1
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Molecular Weight 360.88
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Formula C20H25ClN2O2
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SMILES
O[C@H]([C@]1([H])[N@@]2C[C@@H]([C@](CC2)([H])C1)C=C)C3=CC=NC4=C3C=C(OC)C=C4.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Lee SY, et al. Hydrocinchonine, cinchonine, and quinidine potentiate paclitaxel-induced cytotoxicity and apoptosis via multidrug resistance reversal in MES-SA/DX5 uterine sarcoma cells. Environ Toxicol. 2011 Aug;26(4):424-31. [Content Brief]
[2]. Kehl SJ, et al. Quinidine-induced inhibition of the fast transient outward K+ current in rat melanotrophs. Br J Pharmacol. 1991;103(3):1807-1813. [Content Brief]
[3]. Moody DE, et al. Quinidine inhibits in vivo metabolism of amphetamine in rats: impact upon correlation between GC/MS and immunoassay findings in rat urine. J Anal Toxicol. 1990;14(5):311-317. [Content Brief]
[4]. Jamali H, et al. Effect of dextromethorphan/quinidine on pentylenetetrazole- induced clonic and tonic seizure thresholds in mice. Neurosci Lett. 2020;729:134988. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Quinidine hydrochloride Related Classifications
HY-W115674 Related Classifications
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