2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. 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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CB1R agonist 1

CB1R agonist 1 Chemical Structure

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CB1R agonist 1 Related Antibodies

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Description

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[1].

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.

CB1R agonist 1 Related Antibodies
Parmacokinetics
Species Dose Route Note AUC0-last AUC0-inf Cmax Tmax T1/2 AUC0-t
Mice[1] 0.2 mg/kg i.p. blood sample 1440 min·ng/mL 1510 min·ng/mL 10.8 ng/mL 15 min 102 min /
Mice[1] 0.2 mg/kg i.p. brain sample / 8180 min·ng/mL 44.1 ng/mL 60 min 112 min 7720 min·ng/mL
In Vivo

CB1R agonist 1 (0.05-1 mg/kg; i.p.; single dose; 30 min pretreatment) exerts strong analgesic effects across acute and chronic pain models in mice, and potentiates opioid analgesia[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male adult C57BL/6 mice (8-10 weeks old)[1]
Dosage: 0.05, 0.1, 0.2, 0.5, 1 mg/kg
Administration: i.p.; single dose; 30 min pretreatment
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).
Animal Model: Male adult C57BL/6 mice (8-10 weeks old) injected with CFA[1]
Dosage: 0.2 mg/kg
Administration: i.p.; single dose; 30 min pretreatment
Result: Increased paw withdrawal latencies to well-above pre-CFA baseline thresholds.
Animal Model: Male adult C57BL/6 mice (8-10 weeks old) induced by Acetone[1]
Dosage: 0.05, 0.1, 0.2 mg/kg
Administration: i.p.; single dose; 30 minutes pre-test
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.
Animal Model: Male adult C57BL/6 mice (8-10 weeks old) induced by Formalin[1]
Dosage: 0.2 mg/kg
Administration: i.p.; single dose; 30 minutes pre-test
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.
Animal Model: Male adult C57BL/6 mice (8-10 weeks old)[1]
Dosage: 0.2, 0.5, 1.0 mg/kg
Administration: i.p.; single dose; 30 min pretreatment
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.
Molecular Weight

437.44

Formula

C20H18F3N3O3S
SMILES

COC([C@@](NC(C1=NN(C(C)=C1)C2=CC(C(F)(F)F)=CC=C2)=O)(C3=CC=CS3)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CB1R agonist 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CB1R agonist 1Cannabinoid ReceptorGi/o/G13Cannabinoid-1 receptorGi/o signalingblood-brain barrieranalgesiaCB2RhypothermiaCB1RInhibitorinhibitorinhibit

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