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Tebanicline dihydrochloride

产品编号 T60474 CAS 209326-19-2

Tebanicline dihydrochloride (Ebanicline dihydrochloride) 是一种nAChR 的调节剂，具有有效的口服镇痛活性。Tebanicline dihydrochloride 可抑制金雀花碱与神经元 nAChR 的结合，Ki 值为 37 pM。

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Tebanicline dihydrochloride Chemical Structure

Tebanicline dihydrochloride, CAS 209326-19-2

规格	价格/CNY	货期
2 mg	￥ 491	5日内发货
5 mg	￥ 822	5日内发货
1 mL * 10 mM (in DMSO)	￥ 885	5日内发货

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Tebanicline dihydrochloride 的其他形式现货产品:

Tebanicline hydrochloride

其他形式的 Tebanicline dihydrochloride:

Tebanicline hydrochloride
现货
Tebanicline tosylate
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生物活性

化学信息

存储 & 溶解度

产品描述	Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with effective orally analgesic activity. Tebanicline dihydrochloride inhibits the cytisine binding to α4β2 neuronal nAChRs with a Ki of 37 pM [1].
体外活性	Tebanicline is a novel and effective cholinergic nAChR ligand with analgesic properties and preferential selectivity for neuronal nAChRs. Tebanicline inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM. Tebanicline is functionally an agonist. At the transfected human alpha 4 beta 2 neuronal nAChR (K177 cells), with increased 86Rb+ efflux as a measure of cation efflux, Tebanicline had an EC50 value of 140 nM with an intrinsic activity (IA) compared with (-)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells (sympathetic ganglion-like), an EC50 of 340 nM (IA = 126%); at the F11 dorsal root ganglion cell line (sensory ganglion-like), an EC50 of 1220 nM (IA = 71%); and via direct measurement of ion currents, an EC50 value of 56,000 nM (IA = 83%) at the human alpha 7 homooligimeric nAChR produced in oocytes.
体内活性	Tebanicline is a potent analgesic with full efficacy in models of acute and persistent pain and these effects are primarily mediated by an action at central neuronal nAChRs [2]. Tebanicline produces significant analgesic effects in mice in response to acute noxious thermal stimulation. ABT-594 is orally active, but 10-fold less potent by this route than after intraperitoneal injection. The analgesic effect of ABT-594 is blocked, but not reversed, by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist [3]. Tebanicline has analgesic effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Injection of tebanicline directly into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and disruption of serotonergic neurons in the NRM attenuates the effect of systemic tebanicline [4].

分子量	271.57
分子式	C9H13Cl3N2O
CAS No.	209326-19-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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