Tebanicline hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tebanicline（ABT-594，Ebanicline）是一种有效的合成烟碱（非阿片类）镇痛药。

Tebanicline (ABT-594, Ebanicline), is an effective synthetic nicotinic (non-opioid) analgesic drug.(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 Ki of 37 pM. 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 140 nM with an intrinsic activitycompared with (?)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells, an EC50 of 340 nM; at the F11 dorsal root ganglion cell line, an EC50 of 1220 nM; and via direct measurement of ion currents, an EC50 value of 56,000 nM at the human α7 homo-oligimeric nAChR produced in oocytes (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. 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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Ebanicline hydrochloride | ABT-594 hydrochloride

Neuroscience

GluR

nAChR

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203564-54-9

235.11

C9H12Cl2N2O

>98% (HPLC)

DMSO : ≥ 34 mg/mL; 144.61 mM

Clc1ncc(OC[C@H]2CCN2)cc1.Cl

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(-20℃)

With Ice Pack

≥ 2 years