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Bradanicline

Names

[ CAS No. ]:
639489-84-2

[ Name ]:
Bradanicline

[Synonym ]:
tc-5619
tc-5619-238

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR
Signaling Pathways >> Neuronal Signaling >> nAChR
Research Areas >> Neurological Disease

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H23N3O2

[ Molecular Weight ]:
361.44

[ Exact Mass ]:
361.17900

[ PSA ]:
61.86000

[ LogP ]:
3.77580

Related Compounds