| Name | Tebanicline hydrochloride |
| Description | Tebanicline hydrochloride (Ebanicline hydrochloride) , 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[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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (212.67 mM), Sonication is recommended.
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| Keywords | nAChR | ABT594 Hydrochloride | ABT 594 Hydrochloride |
| Inhibitors Related | Adiphenine hydrochloride | Levamisole hydrochloride | Ethyl (triphenylphosphoranylidene) acetate | Urethane | Hexamethonium Bromide | Ribavirin | Adenine | Mitotane | Choline chloride | Propoxur | N,N-Dicyclohexylcarbodiimide | Arecoline |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Anti-Alzheimer's Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Ion Channel Targeted Library |
United States
