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Tebanicline hydrochloride

Catalog No. T3720 CAS 203564-54-9

Synonyms: ABT-594 hydrochloride, Ebanicline hydrochloride

Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug.

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Tebanicline hydrochloride Chemical Structure

Tebanicline hydrochloride, CAS 203564-54-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 91.00
10 mg	In stock	$ 141.00
25 mg	In stock	$ 277.00
50 mg	In stock	$ 498.00
100 mg	In stock	$ 725.00
500 mg	In stock	$ 1,520.00

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Purity: 98.71%

Purity: 95%

Biological Description

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Description	Tebanicline hydrochloride (Ebanicline hydrochloride) , is an effective synthetic nicotinic (non-opioid) analgesic drug.
Targets&IC50	nAChR:37 pM(ki)
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[1]
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].

Synonyms	ABT-594 hydrochloride, Ebanicline hydrochloride
Molecular Weight	235.11
Formula	C9H12Cl2N2O
CAS No.	203564-54-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 34 mg/mL (144.61 mM)

References and Literature

1. Donnelly-Roberts DL, et al. ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization.J Pharmacol Exp Ther. 1998 May;285(2):777-86. 2. Bannon AW, et al. ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization. J Pharmacol Exp Ther. 1998 May;285(2):787-94. 3. Decker MW, et al. Antinociceptive effects of the novel neuronal nicotinic acetylcholine receptor agonist, ABT-594, in mice. Eur J Pharmacol. 1998 Apr 3;346(1):23-33. 4. Decker MW, et al. The role of neuronal nicotinic acetylcholine receptors in antinociception: effects of ABT-594. J Physiol Paris. 1998 Jun-Aug;92(3-4):221-4.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Anti-Alzheimer's Disease Compound Library Covalent Inhibitor Library Clinical Compound Library NO PAINS Compound Library Bioactive Compound Library

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Keywords

Tebanicline hydrochloride 203564-54-9 Neuroscience AChR ABT 594 Hydrochloride ABT594 Hydrochloride ABT-594 hydrochloride Ebanicline hydrochloride ABT-594 Hydrochloride Tebanicline Hydrochloride Ebanicline Hydrochloride inhibitor inhibit

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