5-(4-クロロフェニル)-N-(3,5-ジメトキシフェニル)-2-フランカルボキサミド 化学特性,用途語,生産方法
説明
Na
v1.8 is a tetrodotoxin-
resistant (TTX-
R) sodium channel with high activation threshold and slow inactivating kinetics that is highly expressed in small-
diameter sensory neurons and has been implicated in signaling various types of pain. A-
803467 is a sodium channel blocker with high-
affinity and selectivity for inhibiting human Na
v1.8 sodium channels (IC
50 = 8 nM when stimulated at half-
maximal inactivation and IC
50 = 79 nM at a resting state). This compound is unusual in that it blocks hNav1.8 at negative resting membrane potentials (many small molecule sodium channel blockers show a reduced affinity for the resting state) and does not demonstrate significant frequency-
dependent block during a 10 Hz pulse train. A-
803467 dose-
dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.
化学的特性
White Solid
一般的な説明
The small molecule A-803467 is a potent and selective Nav1.8 sodium channel blocker. Nav1.8 is a tetrodotoxin-resistant (TTX-R) sodium channel that contributes to pain sensation by transmitting pain stimuli in peripheral sensory neurons; blockage of this channel by A-803467 reduces pain with varying effectiveness in a number of different models. A-803467 has been used to further understand the role of Nav1.8 in transmitting pain stimuli and also can be used as an analgesic.
生物活性
Selective blocker of Na V 1.8 channels (IC 50 values are 8, 2450, 6740, 7340 and 7380 nM for hNa V 1.8, hNa V 1.3, hNa V 1.7, hNa V 1.5 and hNa V 1.2 channels respectively). Shows no significant activity against TRPV1, P2X 2/3 , Ca V 2.2 and KCNQ2/3 channels. Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration.
5-(4-クロロフェニル)-N-(3,5-ジメトキシフェニル)-2-フランカルボキサミド 上流と下流の製品情報
原材料
準備製品