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 |
---|---|---|---|
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
Created
by
admin
on
Edited
Sat Dec 16 00:25:58 GMT 2023
by
admin
on
Sat Dec 16 00:25:58 GMT 2023
|
Protein Sub Type | |
Sequence Type | COMPLETE |
Record UNII |
FO8S2IW40N
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
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 | ||
---|---|---|---|---|---|
|
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 | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY | |||
|
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
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
PARENT -> SALT/SOLVATE | |||
|
STARTING MATERIAL -> INGREDIENT |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
|
||||
Molecular Formula | CHEMICAL |
|