Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 19:21:44 GMT 2023
by
admin
on
Sat Dec 16 19:21:44 GMT 2023
|
| Protein Type | ION CHANNEL |
| Protein Sub Type | GABA RECEPTOR |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
RU3465V8V1
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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| Code System | Code | Type | Description | ||
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RU3465V8V1
Created by
admin on Sat Dec 16 19:21:49 GMT 2023 , Edited by admin on Sat Dec 16 19:21:49 GMT 2023
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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 α2 and α3 subtypes, and as a partial agonist at α1 and α5 (although its action at α5 subtypes is much weaker than at the others).
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POSITIVE ALLOSTERIC MODULATOR (PAM)->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 α1 subtype was considerably greater for 5′-hydroxy pagoclone compared with the parent.
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PARTIAL 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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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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