2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor Arrestin
  4. TRV0109101

TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist (KD = 70 nM) with blood-brain barrier permeability. TRV0109101 selectively promotes G protein signaling pathway coupling while reducing the recruitment of β-arrestin. TRV0109101 inhibits opioid-induced mechanical hyperalgesia and induces antinociceptive tolerance. TRV0109101 is applicable for pain-related research.

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TRV0109101

TRV0109101 Chemical Structure

CAS No. : 1401027-29-9

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TRV0109101 Related Antibodies

Top Publications Citing Use of Products

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

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Description

TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist (KD = 70 nM) with blood-brain barrier permeability. TRV0109101 selectively promotes G protein signaling pathway coupling while reducing the recruitment of β-arrestin. TRV0109101 inhibits opioid-induced mechanical hyperalgesia and induces antinociceptive tolerance. TRV0109101 is applicable for pain-related research[1].

IC50 & Target[1]

human μ-opioid receptor

70 nM (Kd)

Arrestin-2/β-Arrestin 1

 

In Vitro

TRV0109101 acts as a potent, G protein-biased, MOPR-selective agonist in HEK-293 cells, with an EC50 of 10 nM for cAMP inhibition[1].
TRV0109101 (41 nM-10 μM; 5 min) interacts with the orthosteric ligand binding site of human MOPR in HEK-293 cells, with an apparent KD of 70 nM in competition with DAMGO for β-arrestin2 recruitment[1].

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

TRV0109101 Related Antibodies
In Vivo

TRV0109101 (20 mg/kg/day; s.c.; continuous infusion; 7 days) does not promote opioid-induced mechanical allodynia in male C57BL/6 mice but does induce antinociceptive tolerance[1].
TRV0109101 (20-40 mg/kg; s.c.; twice daily (days 1-3), single double dose (day 4); 5 days) does not induce opioid-induced mechanical allodynia in male C57BL/6 mice but does induce antinociceptive tolerance[1].
TRV0109101 (20 mg/kg; s.c.; twice daily; 7 days) rapidly reverses mechanical allodynia in male C57BL/6 mice, though antinociceptive tolerance still develops[1].
TRV0109101 (1-3 mg/kg; s.c.; twice daily) rapidly and fully reverses induced mechanical allodynia in male C57BL/6 mice, though antinociceptive tolerance still develops[1].
TRV0109101 (0.1-10 mg/kg; s.c.; single dose) produces dose-dependent antinociception in the mouse 56°C hot plate assay, with an ED50 of 1.1 mg/kg[1].
TRV0109101 (1-20 mg/kg; s.c.; single dose) produces dose-dependent inhibition of fecal boli accumulation in male C57BL/6 mice, with an ED50 of 6.3 mg/kg[1].
TRV0109101 (1-20 mg/kg; s.c.; single dose) produces dose-dependent inhibition of colonic motility in male C57BL/6 mice, with an ED50 of 9.4 mg/kg[1].

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

Animal Model: C57BL/6 (8 to 10-week-old male, opioid-induced mechanical allodynia model via chronic minipump infusion of μ-opioid agonists over 7 days)[1]
Dosage: 20 mg/kg/day
Administration: s.c.; continuous infusion; 7 days
Result: Did not induce significant mechanical allodynia over the 7-day period.
Developed antinociceptive tolerance to thermal stimuli comparable to that seen with conventional opioids.
Animal Model: C57BL/6 (8 to 10-week-old male, opioid-induced mechanical allodynia model via twice-daily subcutaneous dosing on days 1-3, with a double dose on day 4)[1]
Dosage: 20 mg/kg (days 1-3); 40 mg/kg (day 4)
Administration: s.c.; twice daily (days 1-3); single double dose (day 4); 5 days
Result: Did not develop opioid-induced mechanical allodynia over the 5-day treatment period.
Developed antinociceptive tolerance comparable to that seen with conventional opioids.
Animal Model: C57BL/6 (8 to 10-week-old male, morphine-induced mechanical allodynia reversal model)[1]
Dosage: 20 mg/kg
Administration: s.c.; twice daily; 7 days
Result: Attenuated morphine-induced mechanical allodynia within 24 hours of treatment initiation, with levels indistinguishable from vehicle-treated animals.
Developed antinociceptive tolerance.
Animal Model: C57BL/6 (8 to 10-week-old male, fentanyl-induced mechanical allodynia reversal model)[1]
Dosage: 1 mg/kg; 3 mg/kg
Administration: s.c.; twice daily
Result: Fully reversed fentanyl-induced mechanical allodynia within 1 day of treatment initiation at both doses, with levels indistinguishable from vehicle-treated animals by days 7-8.
Developed antinociceptive tolerance.
Animal Model: C57BL/6 (8 to 10-week-old male, acute pain model via 56°C hot plate assay)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: s.c.; single dose
Result: Produced dose-dependent antinociception, with an ED50 of 1.1 mg/kg.
Resulted in significant increases in percent maximum possible effect (%MPE) compared to vehicle at doses of 1 mg/kg, 3 mg/kg, and 10 mg/kg.
Animal Model: C57BL/6 (8 to 10-week-old male, gastrointestinal function impairment model via fecal boli accumulation assay)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 20 mg/kg
Administration: s.c.; single dose
Result: Produced dose-dependent reduction in fecal boli weight, with an ED50 of 6.3 mg/kg.
Resulted in significant decreases in fecal boli weight compared to vehicle at doses of 10 mg/kg and 20 mg/kg.
Animal Model: C57BL/6 (8 to 10-week-old male, gastrointestinal function impairment model via glass bead colonic motility assay)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 20 mg/kg
Administration: s.c.; single dose
Result: Produced dose-dependent increases in colonic transit time, with an ED50 of 9.4 mg/kg.
Resulted in significant increases in transit time compared to vehicle at doses of 1 mg/kg, 3 mg/kg, 10 mg/kg, and 20 mg/kg.
Molecular Weight

356.53

Formula

C21H28N2OS
CAS No.
SMILES

C(CNCC1=CC=CS1)[C@@]2(CC3(OCC2)CCCC3)C4=CC=CC=N4
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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TRV0109101 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:

TRV01091011401027-29-9TRV 0109101TRV-0109101Opioid ReceptorArrestinHEK293 cellsantinociceptive toleranceμ-opioid peptide receptormale C57BL/6 miceopioid-induced mechanical allodyniaβ-arrestinHEK-293 cellsG protein signaling pathwayopioid-induced hyperalgesiaMOPRInhibitorinhibitorinhibit

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