N-(2-Bromophenyl)-9-Methyl-9-Azabicyclo[3.3.1]Nonan-3-Amine (also known as AT-1001) is a high-affinity and highly selective ligand at α3β4 nicotinic cholinergic receptors (nAChRs) that was reported to decrease nicotine self-administration in rats. AT-1001 has a single-digit nanomolar binding affinity for the α3β4 nAChR and over 100-fold selectivity over the α4β2 nAChR and α7 nAChR in competition binding experiments. In electrophysiological experiments, AT-1001 had partial agonist activity at the α3β4 nAChR, evoking 35% of maximum ACh response, and at the same doses, produced desensitization of the ACh response, effectively acting as a functional antagonist at the α3β4 nAChR. Interestingly, AT-1001 also selectively decreased self-administration of cigarette smoke extract (CSE), an aqueous extract of cigarette smoke components, without altering natural food intake, when administered systemically to rats trained to self-administer CSE
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1907594 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22278092 |
2.64 nM [Ki] |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17697209
12 mg
Route of Administration:
Oral
Substance Class |
Protein
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ZN3R5560ZV
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C308
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Molecular Formula | CHEMICAL |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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