Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 12:10:47 UTC 2023
by
admin
on
Sat Dec 16 12:10:47 UTC 2023
|
| Protein Type | RECEPTOR |
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
G9XQ9S7T2F
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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G9XQ9S7T2F
Created by
admin on Sat Dec 16 12:10:50 UTC 2023 , Edited by admin on Sat Dec 16 12:10:50 UTC 2023
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PRIMARY |
| From | To |
|---|---|
| 1_103 | 1_181 |
| 1_355 | 1_358 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_12 |
| N | 1_19 |
| N | 1_97 |
| N | 1_173 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
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PARTIAL AGONIST->TARGET |
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INHIBITOR -> TARGET |
INHIBITOR
Ki
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PARTIAL AGONIST->TARGET |
Most of the clinically used antipsychotics display fairly high affinity for D3 receptors in vitro, they lack significant D3 receptor binding in vivo. They also do not occupy D3 receptors in schizophrenic patients at clinically-relevant doses, despite having significant and expected D2 receptor occupancy. The lack of in vivo D3 receptor occupancy of currently used antipsychotics may be due to their inability to displace endogenous DA from these sites; especially since DA has approximately 20- fold higher affinity for D3 vs D2 receptors and D3 (but not D2) receptors exist predominantly in a high affinity state for DA”
Ki
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INHIBITOR -> TARGET |
Ki
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
Ki
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WEAK INHIBITOR->TARGET |
INHIBITOR
Ki
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
MAJOR
Ki
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
PARTIAL AGONIST
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LIGAND->OFF TARGET |
BINDING
Ki
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RADIOLIGAND->TARGET |
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PARTIAL AGONIST->TARGET |
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AGONIST -> TARGET |
A potent and highly selective agonist for the dopamine D3 receptor.
EC50
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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RADIOLIGAND->TARGET |
D3-selective radiotracer.
Ki
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RADIOLIGAND->TARGET | |||
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AGONIST -> TARGET | |||
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PARTIAL AGONIST->TARGET |
Ki
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ANTAGONIST->TARGET |
ANTAGONIST
Ki
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AGONIST -> TARGET |
Emax 82% Transfected CHO cells
EC50
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AGONIST -> TARGET | |||
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RADIOLIGAND->TARGET |
Did not image D3 receptors.
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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PARTIAL AGONIST->TARGET | |||
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INHIBITOR -> TARGET |
Ki
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
ANTAGONIST
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
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![Structure of 3-(2-oxo-3-{2-[4-(trifluoromethyl)piperidin-1-yl]ethyl}imidazolidin-1-yl)benzonitrile](/img/6ee93f49-30dd-4dc0-8a7f-3fa244561391.svg "Structure of 3-(2-oxo-3-{2-[4-(trifluoromethyl)piperidin-1-yl]ethyl}imidazolidin-1-yl)benzonitrile")
![Structure of 3-[2-Oxo-3-[2-[4-(trifluoromethyl)-1-piperidinyl]ethyl]-1-imidazolidinyl]benzonitrile-cyano-11C](/img/7efd2ba1-a762-47c9-9035-94a18beaa119.svg "Structure of 3-[2-Oxo-3-[2-[4-(trifluoromethyl)-1-piperidinyl]ethyl]-1-imidazolidinyl]benzonitrile-cyano-11C")
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT | CHEMICAL |
|