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3-Bromocytisine

Names

[ CAS No. ]:
207390-14-5

[ Name ]:
3-Bromocytisine

Biological Activity

[Description]:

3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC50s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC50s are 8 and 50 nM, respectively[1][2].

[Related Catalog]:

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

[Target]

IC50: 0.28 nM (hα4β4), 0.30 nM (hα4β2), 31.6 nM (hα7)[1]


[References]

[1]. Houlihan LM, et al. Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors. J Neurochem. 2001 Sep;78(5):1029-43.

[2]. Moroni M, et al. alpha4beta2 nicotinic receptors with high and low acetylcholine sensitivity: pharmacology, stoichiometry, and sensitivity to long-term exposure to nicotine. Mol Pharmacol. 2006 Aug;70(2):755-68.

Chemical & Physical Properties

[ Density]:
1.61±0.1 g/cm3(Predicted)

[ Boiling Point ]:
463.3±45.0 °C(Predicted)

[ Molecular Formula ]:
C11H13BrN2O

[ Molecular Weight ]:
269.13800

[ Exact Mass ]:
268.02100

[ PSA ]:
34.03000

[ LogP ]:
1.64630

[ Storage condition ]:
2-8°C

Related Compounds