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.
2015-10
Patents

Sample Use Guides

12 mg
Route of Administration: Oral
Substance Class Protein
Created
by admin
on Mon Mar 31 20:35:27 GMT 2025
Edited
by admin
on Mon Mar 31 20:35:27 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
FO8S2IW40N
Record Status FAILED
Record Version
  • Download
Name Type Language
LARAZOTIDE ACETATE
USAN  
USAN  
Official Name English
GLYCINE, GLYCYLGLYCYL-L-VALYL-L-LEUCYL-L-VALYL-L-GLUTAMINYL-L-PROLYL-, MONOACETATE
Preferred 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
Classification Tree Code System Code
NCI_THESAURUS C308
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
Code System Code Type Description
SMS_ID
100000175004
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
FDA UNII
FO8S2IW40N
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
NCI_THESAURUS
C81670
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
DRUG BANK
DBSALT002605
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
EPA CompTox
DTXSID401007986
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
CAS
881851-50-9
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
PUBCHEM
44146842
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
USAN
TT-07
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
ChEMBL
CHEMBL2105646
Created by admin on Mon Mar 31 20:35:27 GMT 2025 , Edited by admin on Mon Mar 31 20:35:27 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
STARTING MATERIAL -> INGREDIENT
Related Record Type Details
ACTIVE MOIETY

Agent Modifications

Modification Process Modification Role Modification Type Amount Fragment Name Fragment ID
SALT FORMATION CHEMICAL Acetic acid Q40Q9N063P
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL