For research use only. Not for therapeutic Use.
High affinity and selective α3β4 nAChR ligand (Ki value 2.6 nM at α3β4 nAChR) with both partial agonistic and antagonistic effects, and >90-fold selective over the other major subtypes, the α4β2 and α7 nAChR. AT-1001 potently and dose-dependently blocks nicotine self-administration in rats, without affecting food responding, and shows a mechanism of action very different from varenicline (Axon 1384 (HCl salt) and Axon 2074 (tartrate salt)).
Catalog Number | I022574 |
CAS Number | 1314801-63-2 |
Molecular Formula | C15H21BrN2 |
Purity | ≥95% |
IUPAC Name | N-(2-bromophenyl)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine |
InChI | InChI=1S/C15H21BrN2/c1-18-12-5-4-6-13(18)10-11(9-12)17-15-8-3-2-7-14(15)16/h2-3,7-8,11-13,17H,4-6,9-10H2,1H3 |
SMILES | CN1C2CCCC1CC(C2)NC3=CC=CC=C3Br |
Reference | A. Cippitelli et al. AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol. 2015 Apr;172(7):1834-45.
L. Toll et al. AT-1001: a high affinity and selective α3β4 nicotinic acetylcholine receptor antagonist blocks nicotine self-administration in rats. Neuropsychopharmacology. 2012 May;37(6):1367-76.
E.W. Tuan et al. AT-1001 is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors. Mol Pharmacol. 2015 Jul 10. pii: mol.115.099978. [Epub ahead of print] |