AP-202

Names

[ CAS No. ]:
2196197-89-2

[ Name ]:
AP-202

Biological Activity

[Description]:

AP-202 (AP202) is a highly potent and selective α4β2 nAChR antagonist with binding Ki of 18 nM, 57-fold selectivity over α3β4 receptor.AP-202 is agonist activity, also dispalys 40-fold, 10-fold and 90-fold selectivity over α4β4, α3β2, α3β4α5 receptors, does not activate α7 nAChR or block acetylcholine induced changes in membrane potential.AP-202 showed significant activity in blocking nicotine priming-induced as well as cue-induced reinstatement of nicotine seeking in vivo.

[References]

1. Jinhua Wu, et al. J Med Chem. 2017 Dec 28;60(24):10092-10104.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₁H₁₆N₄

[ Molecular Weight ]:
204.277

Related Compounds

AP-5 LITHIUM SALT
ap-1-(9-fluorenyl)-2-(1-methylethenyl)naphthalene
AP-768
AP 20187
ap 698
AP 24149
methyl (E)-3-methoxy-2-(4-methylphenyl)prop-2-enoate
1-(1-Benzyl-piperidin-4-yl)-imidazolidin-2-one
4-Methyl-7-phenylindene
(S)-2-(((Benzyloxy)carbonyl)amino)-3-(1-methyl-1H-imidazol-4-yl)propanoic acid
4-[1-(Pyridin-2-yl)piperidin-4-yloxy]benzaldehyde
5-iodo-1-(propan-2-yl)-1H-1,2,3-benzotriazole
Didodecyl diselenide
(2-Methoxy-benzyl)-[3-(2H-pyrazol-3-yl)-benzyl]-amine
1,1-Difluorobut-3-enylbenzene
rel-(1R,2R)-Methyl 2-acetylcyclobutanecarboxylate