Chemical Name:6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-
ol dihydrochloride
Biological Activity:
Subtype-selective α4β2
nicotinic acetylcholine receptor desensitiser (Ki values are 0.41,
0.61 and 10,000 nM for rat α4β4,
human α4β2 and rat α3β4
receptor subtypes respectively). Causes receptor desensitisation without first
activating it, an inhibitory action termed silent desensitisation.
Xiaoet al
(2006) Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors
without activating them. Mol.Pharmacol. 70 1454.