Bradanicline (Synonyms: TC-5619) |
| Catalog No.GC64064 |
La bradaniclina es un agonista del receptor nicotÍnico de acetilcolina (nAChR) α7 altamente selectivo (nAChR α7 humano: CE50 = 17 nM; Ki = 1,4 nM).
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Cas No.: 639489-84-2
Sample solution is provided at 25 µL, 10mM.
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Bradanicline is a highly selective α7 nicotinic acetylcholine receptor (nAChR) agonist (humanα7 nAChR: EC50=17 nM; Ki= 1.4 nM). Bradanicline is used for the research of cognitive disorders[1][2].
Bradanicline is more than a thousand-fold separation between the affinities for the α7 and α4β2 receptor subtypes and has no detectable effects on muscle or ganglionic nicotinic receptor subtypes, indicating a marked selectivity for the central nervous system over the peripheral nervous system[1].
Bradanicline (0.1-1 mg/kg) shows efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia[2].
[1]. Mazurov AA, et al. Discovery of (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders. J Med Chem. 2012;55(22):9793-9809. [2]. Hauser TA, et al. TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia. Biochem Pharmacol. 2009;78(7):803-812.
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