PD-85639

Name: PD-85639
CAS#: 149838-21-1 (free base)
Chemical Formula: C24H32N2O
Exact Mass: 364.2515
Molecular Weight: 364.533
Elemental Analysis: C, 79.08; H, 8.85; N, 7.68; O, 4.39

Description: PD-85639 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).

IUPAC/Chemical Name: N-[3-(2,6-Dimethyl-1-piperidinyl)propyl]-α-phenylbenzeneacetamide

InChi Key: BPZBEIHSHWNWTE-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H32N2O/c1-19-11-9-12-20(2)26(19)18-10-17-25-24(27)23(21-13-5-3-6-14-21)22-15-7-4-8-16-22/h3-8,13-16,19-20,23H,9-12,17-18H2,1-2H3,(H,25,27)

SMILES Code: O=C(NCCCN1C(C)CCCC1C)C(C2=CC=CC=C2)C3=CC=CC=C3

Appearance: Solid powder