Potent positive allosteric modulator of α4β2 nAChRs (EC50
values are 20 and 18 nM for rat and human, respectively). Selective for hα4β2 over hα3β2, hα3β4 and hα7. Inhibits (α4)2
, muscle-type and Torpedo
values are 0.5, 0.7 and 0.2 μM, respectively), but not (α4)3
receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant α4β2 nicotinic acetylcholine receptor potentiators.
Albrecht et al.
Photolabeling a nicotinic acetylcholine receptor (nAChR) with an (α4)3(β2)2 nAChR-selective positive allosteric modulator.