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209326-19-2

中文名稱 化合物 TEBANICLINE DIHYDROCHLORIDE
英文名稱 ABT594 2HCL
CAS 209326-19-2
分子式 C9H12Cl2N2O
分子量 235.11
MOL 文件 209326-19-2.mol
209326-19-2 結(jié)構(gòu)式 209326-19-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 TEBANICLINE DIHYDROCHLORIDE
英文別名
ABT594 2HCL
Tebanicline dihydrochloride

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: ≥ 34 mg/mL (125.20 mM)
形態(tài)Solid
顏色White to off-white

常見(jiàn)問(wèn)題列表

生物活性
Tebanicline dihydrochloride (Ebanicline dihydrochloride) 是 nAChR 的調(diào)節(jié)物,具有有效的口服止痛活性。抑制 cytisine 與神經(jīng)元 nAChR 的結(jié)合的 Ki 值為 37 pM。
靶點(diǎn)

Ki: 37 pM (nAChR)

體外研究

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 K i of 37 pM. Functionally, tebanicline is an agonist. At the transfected human α4β2 neuronal nAChR in K177 cells, with increased 86 Rb + efflux as a measure of cation efflux, ABT-594 has an EC 50 value of 140 nM with an intrinsic activitycompared with (?)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells, an EC 50 of 340 nM; at the F11 dorsal root ganglion cell line, an EC 50 of 1220 nM; and via direct measurement of ion currents, an EC 50 value of 56,000 nM at the human α7 homo-oligimeric nAChR produced in oocytes

體內(nèi)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.

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