2 nicotinic acetylcholine receptor ligand (Ki
values are 0.26 and 54 nM at α
2 and α
4 receptors respectively). May act as a silent desensitizer or as an agonist, depending on subunit stoichiometry (EC50
= 1.1 nM for nAChR-stimulated dopamine release). Exhibits analgesic activity in vivo
and significantly reduces nicotine self-administration in an experimental rat model.
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.
Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them.
Xiao et al.
Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug.
Cucchiaro et al.
Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats.
Levin et al.
Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors.
Zwart et al.
The citations listed below are publications that use Tocris products. Selected citations for Sazetidine A dihydrochloride include:
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