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Tebanicline dihydrochloride

CAS No. : 209326-19-2

MCE 站：Tebanicline dihydrochloride

产品活性：Tebanicline dihydrochloride (Ebanicline dihydrochloride) 是 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 K_i 值为 37 pM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：nAChR

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 K_i 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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