CB1R agonist 1
CB1R agonist 1 is a potent, CNS-penetrant, and selective Cannabinoid-1 receptor (CB1R) agonist with a Ki of 0.95 nM, modulating Gi/o signaling. CB1R agonist 1 exhibits high selectivity over CB2R and other off-target GPCRs, including GPR55, GPR18, and GPR119. CB1R agonist 1 induces analgesia and hypothermia, and potentiates opioid analgesia in mice. CB1R agonist 1 can be used for the research of pain.
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- Fòrmula: C20H18F3N3O3S
- Peso molecular:437.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CB1R 0.95 nM (Ki) |
In Vitro
CB1R agonist 1 (compound '1350) (0.001-10000 nM; 30 min) acts as a full agonist in Gi/o-mediated cAMP inhibition in hCB1R-expressing cells (pEC50 = 8.8, pKi = 9.0)[1].
CB1R agonist 1 (3 μM) exhibits no appreciable off-target activity against a broad panel of 320 non-olfactory GPCRs, including the putative cannabinoid receptors GPR55, GPR18, and GPR119[1].
CB1R agonist 1 exhibits partial agonism toward the β-arrestin-2 pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male adult C57BL/6 mice (8-10 weeks old)[1]
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Dosage:0.05, 0.1, 0.2, 0.5, 1 mg/kg
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Administration:i.p.; single dose; 30 min pretreatment
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Result:Dose-dependently increased tailflick and paw withrawal latencies.
Exhibited significantly longer tail-flick latencies at 0.05 and 0.1 mg/kg, when combined with the opioid (3 mg/kg).
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Animal Model:Male adult C57BL/6 mice (8-10 weeks old) injected with CFA[1]
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Dosage:0.2 mg/kg
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Administration:i.p.; single dose; 30 min pretreatment
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Result:Increased paw withdrawal latencies to well-above pre-CFA baseline thresholds.
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Animal Model:Male adult C57BL/6 mice (8-10 weeks old) induced by Acetone[1]
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Dosage:0.05, 0.1, 0.2 mg/kg
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Administration:i.p.; single dose; 30 minutes pre-test
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Result:Strongly reduced spared nerve injury-induced cold allodynia.
Significantly decreased the combined total number of typical Acetone-induced nocifensive behaviors, including paw withdrawals, shakes, and licks.
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Animal Model:Male adult C57BL/6 mice (8-10 weeks old) induced by Formalin[1]
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Dosage:0.2 mg/kg
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Administration:i.p.; single dose; 30 minutes pre-test
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Result:Profoundly decreased the duration of both phase 1 and phase 2 nocifensive behaviors throughout the 60 minute observation period at 0.2 mg/kg.
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Animal Model:Male adult C57BL/6 mice (8-10 weeks old)[1]
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Dosage:0.2, 0.5, 1.0 mg/kg
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Administration:i.p.; single dose; 30 min pretreatment
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Result:Induced locomotor deficits at 0.2 mg/kg in the openfield test and impaired motor coordination at 0.5 mg/kg in the rotarod test.
Did not induce cataleptic behavior post-injection at analgesic doses (0.2 or 0.5 mg/kg).
Induced hypothermia at 0.2 mg/kg.
Chemical Information
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Peso molecular 437.44
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Fòrmula C20H18F3N3O3S
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SMILES
COC([C@@](NC(C1=NN(C(C)=C1)C2=CC(C(F)(F)F)=CC=C2)=O)(C3=CC=CS3)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CB1R agonist 1 Related Classifications
HY-168997 Related Classifications
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