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AT 1001
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C15H21BrN2
- MW: 309.24
Description
AT 1001 is a high-affinity and selective α3β4 nicotinic acetylcholine receptor ligand with a Ki value of 2.6 nM. It displays partial agonist and antagonist effects, shows greater than 90-fold selectivity over α4β2 and α7 nAChR subtypes and blocks nicotine self-administration in rats.
α3β4 nAChRs are implicated in nicotine reinforcement, autonomic signaling and addiction-related circuitry. AT 1001 is useful for studying subtype-selective nicotinic receptor modulation and mechanisms distinct from varenicline-like pharmacology.
Key Features
- Selective α3β4 nAChR ligand
- Ki: 2.6 nM at α3β4 nAChR
- Partial agonist and antagonist pharmacology
- >90-fold selectivity over α4β2 and α7 nAChR subtypes
Applications
- Nicotinic receptor pharmacology
- Nicotine self-administration studies
- Smoking-cessation mechanism research
- Subtype-selective nAChR profiling
More Information
| Parent CAS No. | 1314801-63-2 |
|---|---|
| Chemical Name | N-(2-bromophenyl)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine |
| SMILES | N(C1CC2N(C)C(C1)CCC2)C1=CC=CC=C1Br |
| MFCD | N.A. |
| 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 |
| InChiKey | UZJWAFOJOSGEKL-UHFFFAOYSA-N |
| CID | 53302872 |
| Short Description | α3β4 ligand |
References
- 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]
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