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
Substance Class Protein
Created
by admin
on Sat Dec 16 00:01:59 GMT 2023
Edited
by admin
on Sat Dec 16 00:01:59 GMT 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
ZN3R5560ZV
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LARAZOTIDE
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
AT-2347
Code English
larazotide [INN]
Common Name English
Larazotide [WHO-DD]
Common Name English
LARAZOTIDE [USAN]
Common Name English
GLYCINE, GLYCYLGLYCYL-L-VALYL-L-LEUCYL-L-VALYL-L-GLUTAMINYL-L-PROLYL-
Common Name English
GLYCYLGLYCYL-L-VALYL-L-LEUCYL-L-VALYL-L-GLUTAMINYL-L-PROLYLGLYCINE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C308
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
Code System Code Type Description
INN
8951
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
NCI_THESAURUS
C81350
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
ChEMBL
CHEMBL2105646
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
WIKIPEDIA
Larazotide
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
EPA CompTox
DTXSID30180526
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
USAN
UU-122
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
CAS
258818-34-7
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
FDA UNII
ZN3R5560ZV
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
PUBCHEM
9810532
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
DRUG BANK
DB05645
Created by admin on Sat Dec 16 00:01:59 GMT 2023 , Edited by admin on Sat Dec 16 00:01:59 GMT 2023
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
INGREDIENT -> STARTING MATERIAL
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Molecular Formula CHEMICAL
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL