Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Wed Apr 02 15:20:45 GMT 2025
by
admin
on
Wed Apr 02 15:20:45 GMT 2025
|
| Protein Type | ION CHANNEL |
| Protein Sub Type | GABA RECEPTOR |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
RU3465V8V1
|
| Record Status |
FAILED
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| Record Version |
|
-
Download
| Name | Type | Language | ||
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Common Name | English | ||
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Preferred 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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RU3465V8V1
Created by
admin on Wed Apr 02 15:20:45 GMT 2025 , Edited by admin on Wed Apr 02 15:20:45 GMT 2025
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
OFF-TARGET ACTIVITY: INHIBITING LIGAND BINDING TO THE AGBAA CHLORIDE ION CHANNEL
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INHIBITOR -> TARGET |
OFF-TARGET ACTIVITY: INHIBITING LIGAND BINDING TO GABAA CHLORIDE ION CHANNEL
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AGONIST -> TARGET |
Etizolam acts as a full agonist at the benzodiazepine/GABAa receptor to produce its range of therapeutic and adverse effects.
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AGONIST -> TARGET |
SL651498 is a subtype-selective GABAA agonist, which acts as a full agonist at ?2 and ?3 subtypes, and as a partial agonist at ?1 and ?5 (although its action at ?5 subtypes is much weaker than at the others).
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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AGONIST -> TARGET |
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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INHIBITOR->OFF-TARGET |
OFF-TARGET ACTIVITY: INHIBITING LIGAND BINDING TO THE GABAA CHLORIDE ION CHANNEL
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
Has been used as an antidote in the treatment of benzodiazepine and Z-drug overdoses.[
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MODULATOR->TARGET |
ALLOSTERIC ACTIVATOR
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PARTIAL AGONIST->TARGET |
Its affinity and efficacy profile were comparable to pagoclone with the exception that efficacy at the ?1 subtype was considerably greater for 5?-hydroxy pagoclone compared with the parent.
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PARTIAL AGONIST->TARGET | |||
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INVERSE AGONIST->TARGET |
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MODULATOR->TARGET |
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ACTIVATOR -> TARGET |
ALLOSTERIC ACTIVATOR
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AGONIST -> TARGET |
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
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MODULATOR->TARGET |
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INVERSE AGONIST->TARGET |
Non selective GABAA inverse agonist. Therapeutic potential is limited by severe side effects (anxiogenic, convulsant, and proconvulsant).
ALLOSTERIC
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NEGATIVE ALLOSTERIC MODULATOR (NAM)->TARGET |
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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AGONIST -> TARGET |
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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ACTIVATOR -> TARGET |
MODULATOR
ALLOSTERIC
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PARTIAL AGONIST->TARGET |
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AGONIST -> TARGET | |||
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MODULATOR->TARGET |
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PARTIAL AGONIST->TARGET |
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PARTIAL AGONIST->TARGET | |||
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AGONIST -> TARGET |
Positive allosteric modulator on GABAA receptors and, at high concentrations, as a direct agonist of the GABAA receptor.
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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POSITIVE ALLOSTERIC MODULATOR (PAM)->TARGET |
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| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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