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Chemical Structure : ABT-594 dihydrochloride
CAS No.: 209326-19-2
Catalog No.: PC-21602Not For Human Use, Lab Use Only.
Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).
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Tebanicline dihydrochloride (ABT-594) is a potent, orally active neuronal nicotinic acetylcholine receptor (alpha 4 beta 2 nAChR) agonist with Ki of 37 pM (rat brain) and 55 pM (transfected human receptor).
Tebanicline dihydrochloride (ABT-594) is 180,000-fold selectivity for the neuronal alpha 4 beta 2 nAChR over alpha 1 beta 1 delta gamma neuromuscular nAChR.
Tebanicline dihydrochloride (ABT-594) has weak affinity in binding assays for adrenoreceptor subtypes alpha-1B (Ki = 890 nM), alpha-2B (Ki=597 nM) and alpha-2C (Ki=342 nM), and it has negligible affinity (Ki > 1000 nM) for approximately 70 other receptors, enzyme and transporter binding sites.
Tebanicline dihydrochloride (ABT-594) has an EC50 value of 140 nM with an intrinsic activity in human alpha 4 beta 2 neuronal nAChR (K177 cells).
Tebanicline dihydrochloride (ABT-594) (30 uM) inhibits the release of calcitonin gene-related peptide from C-fibers terminating in the dorsal horn of the spinal cord, an effect mediated via nAChRs.
| M.Wt | 271.57 | |
| Formula | C9H13Cl3N2O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Pyridine, 5-[(2R)-2-azetidinylmethoxy]-2-chloro-, hydrochloride (1:2) |
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1. Bannon AW, et al. J Pharmacol Exp Ther. 1998 May;285(2):787-94.
2. Holladay MW, et al. J Med Chem. 1998 Feb 12;41(4):407-12.
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