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Biological Data Biological description Na+ , Ca+ channel blocker (IC50 = 10 µM for R type Ca2+ channel currents). Also acts as TREK-1 antagonist and inhibits glutamate release. Analog of lamotrigine. Displays neuroprotective and antidepressant properties.
Solubility & Handling Storage instructions Room temperature
Solubility overview Soluble in DMSO (100mM) or ethanol (25mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use
Chemical Data Chemical name 2-(4-Methyl-1-piperazinyl)-5-(2,3,5-trichlorophenyl)-4-pyrimidinamine
Chemical structure
Molecular Formula C15 H16 Cl3 N5
SMILES ClC1=CC(Cl)=C(Cl)C(C2=C(N)N=C(N3CCN(C)CC3)N=C2)=C1
InChi InChI=1S/C15H16Cl3N5/c1-22-2-4-23(5-3-22)15-20-8-11(14(19)21-15)10-6-9(16)7-12(17)13(10)18/h6-8H,2-5H2,1H3,(H2,19,20,21)
InChiKey PDOCBJADCWMDGL-UHFFFAOYSA-N
References for Sipatrigine References are publications that support the biological activity of the product
Sipatrigine could have therapeutic potential for major depression and bipolar depression through antagonism of the two-pore-domain K+ channel TREK-1. Tsai SJ (2008) Med Hypotheses 70(3) : 548-50. The neuroprotective agent sipatrigine blocks multiple cardiac ion channels and causes triangulation of the ventricular action potential. Gao Z et al (2005) Clin Exp Pharmacol Physiol 32(12) : 1088-96. Actions of sipatrigine, 202W92 and lamotrigine on R-type and T-type Ca2+ channel currents. Hainsworth AH et al (2003) Eur J Pharmacol 467(1-3) : 77-80. BW619C89, a glutamate release inhibitor, protects against focal cerebral ischemic damage. Leach MJ et al (1993) Stroke 24(7) : 1063-7.
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Na+ / Ca+ channel blocker