CAS NO: | 209326-19-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Tebanicline dihydrochloride (Ebanicline dihydrochloride) is anAChRmodulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with aKiof 37 pM[1]. | ||||||||||||||||
IC50& Target | Ki: 37 pM (nAChR)[1] | ||||||||||||||||
体外研究 (In Vitro) | 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 Kiof 37 pM. Functionally, tebanicline is an agonist. At the transfected human α4β2 neuronal nAChR in K177 cells, with increased86Rb+efflux as a measure of cation efflux, ABT-594 has an EC50value of 140 nM with an intrinsic activitycompared with (–)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells, an EC50of 340 nM; at the F11 dorsal root ganglion cell line, an EC50of 1220 nM; and via direct measurement of ion currents, an EC50value of 56,000 nM at the human α7 homo-oligimeric nAChR produced in oocytes[1] | ||||||||||||||||
体内研究 (In Vivo) | 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[2]. 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[3]. 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[4]. | ||||||||||||||||
分子量 | 271.57 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C9H13Cl3N2O | ||||||||||||||||
CAS 号 | 209326-19-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 100 mg/mL(368.23 mM;Need ultrasonic) DMSO : ≥ 34 mg/mL(125.20 mM) *"≥" means soluble, but saturation unknown. 配制储备液
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