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Catharanthine ((+)-3,4-Didehydrocoronaridine) Sulfate, a constituent of anticancer vinca alkaloids, inhibits voltage-operated L-type Ca2+ channel (VOCC). Catharanthine Sulfate has IC50s of 220 μM and 8 μM for VOCC currents in cardiomyocytes and vascular smooth muscle cells (VSMCs), respectively. Catharanthine Sulfate lowers blood pressure (BP), heart rate (HR). Catharanthine Sulfate has anti-cancer activity[1][2]. | [in vivo]
Catharanthine ((+)-3,4-Didehydrocoronaridine; 0.5-20 mg/kg; IV; single dose) Sulfate evokes dose-dependent reductions in both BP and HR[1].
Catharanthine (40 mg/kg; ip; single dose) Sulfate with acute administration induces similar antidepressant-like activity in male and female mice at 1 h and 24 h[1].
Catharanthine (20 mg/kg; ip; for 14 consecutive days) Sulfate increases swimming time and decreases immobility time at D7 or D14 in mice[1].
| Animal Model: | 13-week-old male SpragueDawley rats (300-350 g)[1] | | Dosage: | 0.5-20 mg/kg | | Administration: | IV; single dose | | Result: | Evoked rapid, transient reductions in BP and HR (lasting ,2 minutes) at low doses (0.5–5 mg/kg), whereas at higher doses (10 and 20 mg/kg), the BP and HR reductions were sustained.
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L-type calcium channel | [References]
[1] Jadhav A, et al. Catharanthine dilates small mesenteric arteries and decreases heart rate and cardiac contractility by inhibition of voltage-operated calcium channels on vascular smooth muscle cells and cardiomyocytes. J Pharmacol Exp Ther. 2013 Jun;345(3):383-92. DOI:10.1124/jpet.112.199661
[2] Hugo R Arias, et al. (+)-Catharanthine and (-)-18-methoxycoronaridine induce antidepressant-like activity in mice by differently recruiting serotonergic and norepinephrinergic neurotransmission. Eur J Pharmacol. 2023 Jan 15:939:175454. DOI:10.1016/j.ejphar.2022.175454 |
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