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KI1106Pizotifen malate50 mg$154

Chemical Characteristic

Product NamePizotifen malate
CAS No.5189-11-7
Molecular Weight 429.53
FormulaC23H27NO5S
Chemical Name4-(4,5-dihydrobenzo[1,2]cyclohepta[3,4-b]thiophen-10-ylidene)-1-methylpiperidine;2-hydroxybutanedioic acid
SmilesN1(CCC(=C2c3ccsc3CCc3c2cccc3)CC1)C C(=O)(C(CC(=O)O)O)O
Chemical Structure

Biological activities

Pizotifen malate is an antihistamine and serotonin inhibitor. Pizotifenmalate is a potent antagonist of 5-HT2 and histamine H1 receptors used prophylaxis for migraine headaches.[1] The bioavailability of oral pizotifen malate is 78%, with a plasma protein binding of 91% and an elimination half-life of 23 hour.[2] In striatal HdhQ111/Q111 cells, pizotifen malate treatment causes transient ERK activation and significantly blocks caspase activation in a dose-depend manner. In the R6/2 HD mouse model, treatment with pizotifen malate (7.5 and 10 mg/kg) activates ERK in the striatum, reduces neurodegeneration and significantly enhances motor performance.[3]

Protocols

In vitro: 2.4 mg/mL pizotifen malate stock solution is prepared in isotonic buffer [NaCl (150mM)-Hepes (20mM), pH 4.6].[2]

References

[1] Solomon GD, et al. Therapeutic advances in migraine. J Clin Pharmacol. 1993, 33(3): 200-209.
[2] Serna-Jim?nez CE, et al. HPLC-UV analytical method for determination of pizotifen after in vitro transdermal diffusion studies. Biomed Chromatogr. 2012, 26(6): 769-774.
[3] Sarantos MR, et al. Pizotifen activates ERK and provides neuroprotection in vitro and in vivo in models of Huntington's disease. Journal of Huntington?? Disease. 2012, 195??10.

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