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Tebanicline dihydrochloride  ≥98%

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包装规格：5mg in glass bottle
溶解性：溶于(DMS:≥34mg/ml）
产品描述：基本信息 产品编号： T11024 产品名称： Tebanicline dihydrochloride CAS: 209326-19-2   储存条件 粉末 -20℃ 四年     分子式： C9H13Cl3N2O 溶于液体 -80℃ 6个月 分子量： 271.57 -20℃ 1个月 化学名：  5-[[(2R)-azetidin-2-yl]methoxy]-2-chloropyridine;dihydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.6823mL 18.4115mL 36.8229mL 5mM 0.7365mL 3.6823mL 7.3646mL 10mM 0.3682mL 1.8411mL 3.6823mL   生物活性 产品描述 一种nAChR的调节物，具有有效的口服止痛活性。抑制cytisine与神经元nAChR的结合的Ki值为37pM。 靶点 Ki:37pM (nAChR)   体外研究 Tebanicline is a novel,potent cholinergic nAChR ligand with analgesic properties that shows preferential selectivity for neuronal nAChRs.It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37pM.Functionally,tebanicline is an agonist.At the transfected human α4β2 neuronal nAChR in K177 cells,with increased 86Rb+efflux as a measure of cation efflux,ABT-594 has an EC50 value of 140nM with an intrinsic activitycompared with (−)-nicotine of 130%;at the nAChR subtype expressed in IMR-32 cells,an EC50 of 340nM;at the F11 dorsal root ganglion cell line,an EC50 of 1220nM;and via direct measurement of ion currents,an EC50 value of 56,000nM at the human α7 homo-oligimeric nAChR produced in oocytes. 体内研究 Tebanicline is a potent antinociceptive agent with full efficacy in models of acute and persistent pain and that these effects are mediated predominately by an action at central neuronal nAChRs.Tebanicline produces significant antinociceptive effects in mice against both acute noxious thermal stimulation.ABT-594 is orally active,but 10-fold less potent by this route than after i.p.administration.The antinociceptive effect of ABT-594 is prevented,but not reversed,by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist.Tebanicline has antinociceptive effects in rat models of acute thermal,persistent chemical,and neuropathic pain.Direct injection of tebanicline into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and destruction of serotonergic neurons in the NRM attenuates the effect of systemic tebanicline.   推荐实验方法(仅供参考) 动物实验:   Rats:Rats are dosed with either saline or ABT-594 (0.3μM/kg i.p.) b.i.d.for 5 days.Treatments are separated by approximately 6h (i.e.,morning and afternoon).In the hot box experiment,animals are tested in the morning and afternoon on days 1,2 and 5.For each test,a base-line measure is recorded,and then animals are tested 15,30 and 45 min after treatment.For the afternoon treatment on day 5,all animals received a challenge dose of ABT-594 (0.3μM/kg i.p.) before being tested.For the motor coordination experiment,animals are tested only in the afternoon on day 5. Mice: Tebanicline is dissolved and diluted in sterile 0.9% saline.The effects of tebanicline are tested for anxiolytic-like activity using the elevated plus-maze procedure.Mice are injected with ABT-594 (0.019,0.062,or 0.19μM/kg) or saline,the mouse is placed in the center of the maze and allowed to explore the maze for 5 min.During this period, an auto-mated video tracking system is used to record the time spent on the open arms and the total distance traveled.Diazepam (10.5μM/kg,i.p). is used as a positive control compound.
保存条件：-20℃

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