U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
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

Targets

Primary TargetPharmacologyConditionPotency
2.64 nM [Ki]
PubMed

PubMed

TitleDatePubMed
AT-1001 Is a Partial Agonist with High Affinity and Selectivity at Human and Rat α3β4 Nicotinic Cholinergic Receptors.
2015 Oct
Patents

Sample Use Guides

12 mg
Route of Administration: Oral
Name Type Language
LARAZOTIDE ACETATE
USAN  
USAN  
Official Name English
GLYCYLGLYCYL-L-VALYL-L-LEUCYL-L-VALYL-L-GLUTAMINYL-L-PROLYLGLYCINE ACETATE
Common Name English
LARAZOTIDE ACETATE [USAN]
Common Name English
Larazotide acetate [WHO-DD]
Common Name English
AT-1001 (LARAZOTIDE ACETATE)
Code English
AT-1001
Code English
GLYCINE, GLYCYLGLYCYL-L-VALYL-L-LEUCYL-L-VALYL-L-GLUTAMINYL-L-PROLYL-, MONOACETATE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C308
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
Code System Code Type Description
FDA UNII
FO8S2IW40N
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
PRIMARY
NCI_THESAURUS
C81670
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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DRUG BANK
DBSALT002605
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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EPA CompTox
DTXSID401007986
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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CAS
881851-50-9
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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PUBCHEM
44146842
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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USAN
TT-07
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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ChEMBL
CHEMBL2105646
Created by admin on Sat Dec 16 00:25:58 GMT 2023 , Edited by admin on Sat Dec 16 00:25:58 GMT 2023
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