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アッセイ
≥98% (HPLC)
フォーム
powder
色
white to beige
溶解性
DMSO: 2 mg/mL, clear (warmed)
保管温度
room temp
SMILES記法
CC1CCCC(C)N1CCCNC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O
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)
InChI Key
QNZVKSNHNMBPSR-UHFFFAOYSA-N
生物化学的／生理学的作用
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).
シグナルワード
Warning
危険有害性情報
危険有害性の分類
Acute Tox. 4 Oral
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
PZ0370-VAR:
PZ0370-25MG:
PZ0370-BULK:
PZ0370-5MG:
最新バージョンのいずれかを選択してください：
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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