PZ0370
PD-85639
别名:
N-[3-(2,6-Dimethyl-1-piperidinyl)propyl]-α-phenylbenzeneacetamide, PD 85639, PD85,639, PD85639
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关于此项目
经验公式（希尔记法）:
C24H32N2O
化学文摘社编号:
分子量:
364.52
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
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)
SMILES string
CC1CCCC(C)N1CCCNC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O
InChI key
QNZVKSNHNMBPSR-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
room temp
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).
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
I Roufos et al.
Journal of medicinal chemistry, 37(2), 268-274 (1994-01-21)
The synthesis and structure-activity relationships of a series of phenylacetamides related to N-[3-(2,6-dimethyl-1-piperidinyl)propyl]-alpha-phenylbenzeneacetamide (1) (PD85639) acting at the voltage-dependent Na+ channel are described. All structural variations for this study were made in the phenylacetic acid portion of these molecules, and
W Thomsen et al.
Molecular pharmacology, 43(6), 955-964 (1993-06-01)
The local anesthetic-like Na+ channel-blocking drug [3H]PD85639 [alpha-([4-3H]phenyl)-N-[3-(2,6-dimethyl-1-piperizinyl)-alpha-prop yl] [4-3H]benzeneacetamide] binds specifically to receptor sites on Na+ channels in intact synaptosomes and synaptosomal membranes, purified and reconstituted Na+ channels, and type IIA Na+ channel alpha subunits expressed in the transfected
D S Ragsdale et al.
Molecular pharmacology, 43(6), 949-954 (1993-06-01)
This study examined the actions of the novel Na+ channel blocker PD85,639. In whole-cell voltage-clamp recordings from Chinese hamster ovary cells transfected with a cDNA encoding the rat brain type IIA Na+ channel and from dissociated rat brain neurons, PD85,639
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