Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 12:09:21 GMT 2023
by
admin
on
Sat Dec 16 12:09:21 GMT 2023
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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
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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 | ||
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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 Sat Dec 16 12:09:33 GMT 2023 , Edited by admin on Sat Dec 16 12:09:33 GMT 2023
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PRIMARY | |||
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1PE72K8X46
Created by
admin on Sat Dec 16 12:09:33 GMT 2023 , Edited by admin on Sat Dec 16 12:09:33 GMT 2023
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PRIMARY |
From | To |
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1_142 | 1_219 |
Glycosylation Type | HUMAN |
Glycosylation Link Type | Site |
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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 |
POTENCY
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
Emax = 81% of Fentanyl
EC50
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET | |||
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WEAK AGONIST->TARGET |
Inhibition of forskolin-induced cAMP accumulation
IC50
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INHIBITOR -> 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
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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AGONIST -> TARGET |
POTENCY
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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 |
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
In contrast to naloxone, diprenorphine (0.03 mgkg−1i.p.)reversed equipotent doses of morphine and fentanyl to the same degree. Assay done on SH-SY5Y cells displacing [3H]DIPRENORPHINE.
Ki
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LIGAND->TARGET |
BINDING
IC50
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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ANTAGONIST->TARGET | |||
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RADIOLIGAND->TARGET |
Kd
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AGONIST -> TARGET |
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AGONIST -> TARGET |
Mini Gi assay. Emax=129 (123-136) relative to Fentanyl. EC50 for Fentanyl=34.6
EC50
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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 |
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AGONIST -> TARGET |
Ki
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
IC50
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
Inhibition of cAMP accumulation
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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 | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Blood furanylfentanyl concentrations are expected to be in a range of 1-45 μg/L in victims of fatal overdosage.[
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AGONIST -> TARGET |
Assumed an agonist
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PARTIAL AGONIST->TARGET |
Emax = 23% of DAMGO
EC50
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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AGONIST -> TARGET |
HUMAN RECEPTOR
AGONIST
Ki
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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 | |||
|
AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
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AGONIST -> TARGET |
Potency higher than fentanyl (IC50=1.23 NM) fast onset and short duration of action.
IC50
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AGONIST -> TARGET | |||
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INHIBITOR -> 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 | |||
|
AGONIST -> TARGET |
POTENCY
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|
AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
POTENCY
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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 |
Ki
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AGONIST -> TARGET | |||
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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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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 |
POTENCY
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
Mouse hot plate test. 117 times more potent than morphine.
ED50
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
In mouse hot plate test, the antinociceptive ED50 of C8813 was 11.5 μg/kg, being 591 times and 3.4 times more potent than morphine and fentanyl respectively.
Ki
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AGONIST -> TARGET | |||
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RADIOLIGAND->TARGET |
Kd
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AGONIST -> TARGET |
Assumed active
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INHIBITOR -> TARGET |
Ki
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
POTENCY
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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 |
Herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A.
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INHIBITOR -> TARGET |
Mu Receptor [3H]DAMGO BINDING INHIBITION
BINDING
Ki
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PARTIAL AGONIST->TARGET |
MOR partial agonists with reduced β-arrestin-2 recruitment in-vitro. 20-fold more potent than morphine at inhibiting contractions and 100-fold more potent than mitragynine.
EC50
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
EC50
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PARTIAL AGONIST->TARGET |
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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 μ-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in μ-opioid binding.
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PARTIAL AGONIST->TARGET |
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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 |
The fluorinated MT‐45 derivatives have higher apparent potencies (2F‐MT‐45: 42 nM) than MT‐45 (1.3 μM) for inhibition of cAMP accumulation and β‐arrestin2 recruitment (2F‐MT‐45: 196 nM; MT‐45: 23.1 μM).
EC50
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WEAK AGONIST->TARGET |
Emax=91.2% of Fentanyl
EC50
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
Emax=94.9 relative to Fentanyl
EC50
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
Has around 7.5-fold the potency of morphine in animal models.
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AGONIST -> TARGET |
Atypical. G-protein activation
EC50
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
ANTAGONIST
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|
AGONIST -> TARGET |
EC50
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INHIBITOR -> TARGET | |||
|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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INHIBITOR -> 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 |
POTENCY
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INHIBITOR -> TARGET |
IC50
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET | |||
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RADIOLIGAND->OFF TARGET |
Ki
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AGONIST -> TARGET |
The antinociceptive ED50 in mouse hot plate of the two compounds were 11.5 μg/kg and 13.4 μg/kg respectively.
Ki
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Lance Ultra cAMP Assay
EC50
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AGONIST -> TARGET |
Lance Ultra cAMP Assay
EC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
IC50 of Fentanyl= 1.23 NM
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Lance Ultra cAMP Assay
EC50
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AGONIST -> TARGET |
In vitro data suggest that flunitazene is much less potent than fentanyl. Emax=118% of Fentanyl
EC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Emax=134% of Fentanyl
EC50
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AGONIST -> TARGET |
POTENCY
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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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INHIBITOR->OFF-TARGET |
Ki
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AGONIST -> TARGET |
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WEAK AGONIST->TARGET |
POTENCY
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NON-INHIBITOR->OFF TARGET |
ED50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
Emax=106 of Fentanyl
EC50
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AGONIST -> TARGET |
Ki
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
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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 | |||
|
AGONIST -> TARGET |
POTENCY
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
Emax =140% of Fentanyl. In vitro data shows that N-desethyl isotonitazene is similar in potency to etonitazene, and approximately 20 times more potent than fentanyl.
EC50
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AGONIST -> TARGET |
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|
AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Inhibition of forskolin-induced cAMP accumulation.
IC50
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AGONIST -> TARGET |
Rat tail withdrawal test. Morphine ED50 3.15. Fentanyl ED50 0.1 mg/mL
ED50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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|
AGONIST -> TARGET |
Assumed active
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
An active opioid with potency approximately two times greater than that of fentanyl [unpublished data from L. De Vrieze and C. Stove].
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
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|
AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
An active opioid with potency approximately 25 times greater than that of fentanyl [unpublished data from L. De Vrieze and C. Stove].
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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 | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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PARTIAL AGONIST->TARGET |
PARTIAL AGONIST
BINDING
Ki
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AGONIST -> TARGET |
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
POTENCY
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AGONIST -> TARGET |
Butonitazene is tens of times superior to morphine when administered intravenously, as was found in chemical studies in rodents. Emax=103% of Fentanyl. beta-Arrestin assay
EC50
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AGONIST -> TARGET |
Mouse hot plate test. 1516 times more potent than morphine.
ED50
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AGONIST -> TARGET |
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AGONIST -> TARGET |
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WEAK AGONIST->TARGET |
Presumed to be weak agonist.
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AGONIST -> TARGET |
10 times more potent than Fentanyl.
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AGONIST -> TARGET |
Emax 180 of hydromorphone
BIOASSAY (CELLULAR)
EC50
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AGONIST -> TARGET |
IC50 of Fentanyl= 1.23 NM
IC50
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AGONIST -> TARGET |
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AGONIST -> TARGET |
POTENCY
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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 |
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|
AGONIST -> TARGET |
EC50
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|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET | |||
|
AGONIST -> TARGET |
POTENCY
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
BINDING
Ki
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AGONIST -> TARGET |
IC50 of Fentanyl= 1.23 NM
IC50
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
|
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|
AGONIST -> TARGET |
Emax=113% relative to Fentanyl
EC50
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AGONIST -> TARGET |
Mouse hot plate test. 2600 times more potent than morphine.
ED50
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AGONIST -> TARGET |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Molecular Formula | CHEMICAL |
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MOL_WEIGHT | CHEMICAL |
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