Biochem/physiol Actions
PD-85639 (PD85,639) is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 µM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 µM/60% at pH 9.0, 5 nM/28% & 3 µM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 µM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, ﹤0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 µM against 5 nM [3H]-BTX for binding rat neocrotical membranes).
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| Colour | white to beige |
|---|---|
| InChI key | QNZVKSNHNMBPSR-UHFFFAOYSA-N |
| InChI | 1S/C23H31N3O/c1-4-13-23(22(24)27,19-9-6-5-7-10-19)20-11-8-12-21(14-20)26-17(2)15-25-16-18(26)3/h5-12,14,17-18,25H,4,13,15-16H2,1-3H3,(H2,24,27) |
| Manufacturer | SIGMA-ALDRICH |
| Form | powder |
| Assay | ≥98% (HPLC) |
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