For research use only. Not for therapeutic Use.
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].
| Catalog Number | I045059 |
| CAS Number | 639489-84-2 |
| Synonyms | N-[(2S,3R)-2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]octan-3-yl]-1-benzofuran-2-carboxamide |
| Molecular Formula | C22H23N3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H23N3O2/c26-22(20-13-17-5-1-2-6-19(17)27-20)24-21-16-7-10-25(11-8-16)18(21)12-15-4-3-9-23-14-15/h1-6,9,13-14,16,18,21H,7-8,10-12H2,(H,24,26)/t18-,21+/m0/s1 |
| InChIKey | OXKRFEWMSWPKKV-GHTZIAJQSA-N |
| SMILES | C1CN2CCC1C(C2CC3=CN=CC=C3)NC(=O)C4=CC5=CC=CC=C5O4 |
| Reference | [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) [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. |
