Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 11:57:42 UTC 2023
by
admin
on
Sat Dec 16 11:57:42 UTC 2023
|
| Protein Sub Type | |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
1EKV1NFY3Y
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
1EKV1NFY3Y
Created by
admin on Sat Dec 16 11:57:43 UTC 2023 , Edited by admin on Sat Dec 16 11:57:43 UTC 2023
|
PRIMARY |
| From | To |
|---|---|
| 1_32 | 1_74 |
| 1_216 | 1_500 |
| 1_337 | 1_344 |
| 1_382 | 1_389 |
| 1_482 | 1_501 |
| 1_486 | 1_504 |
| 1_507 | 1_519 |
| 1_522 | 1_535 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_185 |
| N | 1_268 |
| N | 1_320 |
| N | 1_384 |
| N | 1_529 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
|
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|
AGONIST -> TARGET |
Ki
|
||
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RADIOLIGAND->TARGET |
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||
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INHIBITOR -> TARGET |
ANTAGONIST
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INHIBITOR -> TARGET |
In Rodents
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RADIOLIGAND->TARGET |
ALLOSTERIC
|
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|
MODULATOR->TARGET |
The pharmacokinetics and effects of JNJ-40411813 on cognition and subjective awareness were evaluated. Plasma JNJ-40411813 exposure was dose-dependent, t max ranged from 3-4 h and t 1/2 19.4-34.2 h across the dose levels. JNJ-40411813 significantly (p=0.02) reduced continuity of attention score (150 mg dose) and ameliorated smoking withdrawal-induced changes in power of attention and quality of episodic memory versus placebo. A modest reduction in alertness was observed at 150-225 mg doses, JNJ-40411813 (500 mg) reduced S(+) ketamine-induced negative symptoms by approximately 43% and 30% in cohorts 1 and 3, respectively. JNJ-40411813 was generally well-tolerated.
ALLOSTERIC ACTIVATOR
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RADIOLIGAND->TARGET |
ALLOSTERIC
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NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
Complete selectivity against mGluR1,3,4,5,6,8 (IC50 > 10000 nM). Flipr Assay
IC50
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|
|
INHIBITOR -> TARGET |
MAY BE RESPONSIBLE FOR ANTIDEPRESSANT ACTIVITY OF KETAMINE
|
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NEGATIVE ALLOSTERIC MODULATOR->TARGET |
|
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INHIBITOR -> TARGET |
MAY BE RESPONSIBLE FOR ANTIDEPRESSANT ACTIVITY OF KETAMINE
|
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|
LIGAND->TARGET |
|
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|
INHIBITOR -> TARGET |
Ki
|
||
|
LIGAND->TARGET |
|
||
|
AGONIST -> TARGET |
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
|