Bioactivity | 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]. | ||||||||||||
Invitro | 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]. | ||||||||||||
In Vivo | Bradanicline (0.1-1 mg/kg) shows efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia[2]. | ||||||||||||
Name | Bradanicline | ||||||||||||
CAS | 639489-84-2 | ||||||||||||
Formula | C22H23N3O2 | ||||||||||||
Molar Mass | 361.44 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
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. |