Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Fri Jun 25 20:51:11 UTC 2021
by
admin
on
Fri Jun 25 20:51:11 UTC 2021
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Protein Sub Type | |
Sequence Type | COMPLETE |
Record UNII |
1PE72K8X46
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Record Status |
Validated (UNII)
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Record Version |
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-
Download
Name | Type | Language | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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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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P35372
Created by
admin on Fri Jun 25 20:51:11 UTC 2021 , Edited by admin on Fri Jun 25 20:51:11 UTC 2021
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PRIMARY | |||
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1PE72K8X46
Created by
admin on Fri Jun 25 20:51:11 UTC 2021 , Edited by admin on Fri Jun 25 20:51:11 UTC 2021
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PRIMARY |
From | To |
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1_142 | 1_219 |
Glycosylation Type | HUMAN |
Glycosylation Link Type | Site |
---|---|
N | 1_9 |
N | 1_12 |
N | 1_33 |
N | 1_40 |
N | 1_48 |
Related Record | Type | Details | ||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
Reported to have 13X the potency of morphine
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
An opioid analgesic drug from the thiambutene family, which has around the same potency as morphine.
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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ANTAGONIST->TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
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AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.5
AGONIST
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
Blood furanylfentanyl concentrations are expected to be in a range of 1-45 ?g/L in victims of fatal overdosage.[
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AGONIST -> TARGET |
HUMAN RECEPTOR
AGONIST
Ki
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AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
(+)-isomer
COMPETITIVE INHIBITOR
Ki
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
Cannot cross blood-brain barrier due to positive charge
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
Herkinorin is a ?-opioid agonist with more than 100x higher ?-opioid affinity and 50x lower ?-opioid affinity compared to Salvinorin A.
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INHIBITOR -> TARGET |
Mu Receptor [3H]DAMGO BINDING INHIBITION
BINDING
Ki
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INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
Opioid activity is due to both low affinity binding of the parent compound and higher affinity binding of the O-demethylated metabolite M1 to ?-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in ?-opioid binding.
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AGONIST -> TARGET | |||
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PARTIAL AGONIST->TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
BINDING
Ki
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET | |||
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PARTIAL AGONIST->TARGET |
PARTIAL AGONIST
BINDING
Ki
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INHIBITOR -> TARGET |
ANTAGONIST
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
ED50(mg/kg) = 0.220, Potency ratio to morphine = 1.5, Potency ratio to fentanyl = 0.03
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
TRV0109662 is a weak (EC50= 5 mcM) partial agonist of the human mu-opioid receptor.
PARTIAL AGONIST
EC50
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
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AGONIST -> TARGET |
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 4.0
AGONIST
IC50
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
|
INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
Emax 180 of hydromorphone
BIOASSAY (CELLULAR)
EC50
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
RAT OPIOD RECEPTOR; POTENCY RELATIVE TO MORPHINE 2.1
AGONIST
IC50
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
MOL_WEIGHT | CHEMICAL |
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Molecular Formula | CHEMICAL |
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