2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Mu opioid receptor antagonist 9

Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD).

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Mu opioid receptor antagonist 9

Mu opioid receptor antagonist 9 Chemical Structure

CAS No. : 3058600-77-1

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Mu opioid receptor antagonist 9 Related Antibodies

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

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Description

Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD)[1].

IC50 & Target[1]

μ Opioid Receptor/MOR

77.3 nM (Ki)

κ Opioid Receptor/KOR

681 nM (Ki)

δ Opioid Receptor/DOR

4182 nM (Ki)

In Vitro

Mu opioid receptor antagonist 9 (compound 53) (15 min) inhibits calcium flux induced by DAMGO (HY-P0210) and psychoactive substances in mMOR-CHO cells with IC50 values of 33.6 and 4.51 μM, respectively[1].

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

Mu opioid receptor antagonist 9 Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration Brain-to-Plasma Ratio
Mice[1] 10 mg/kg s.c. 0.97 μg/mL 720 ng/g 0.74
Mice[1] 10 mg/kg s.c. 0.80 μg/mL 640 ng/g 0.80
Mice[1] 10 mg/kg s.c. 0.66 μg/mL 820 ng/g 1.24
Mice[1] 10 mg/kg s.c. 0.58 μg/mL 480 ng/g 0.82
In Vivo

Mu opioid receptor antagonist 9 (1-10 mg/kg; s.c.; single dose) blocks the antinociceptive effects of Morphine and fentanyl in the warm water tail immersion pain model in mice[1].
Mu opioid receptor antagonist 9 (1-32 mg/kg; s.c.; single dose at 20min post-fentanyl) demonstrates a potent reversal effect on fentanyl-induced respiratory depression in the whole-body plethysmography study in mice[1].

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

Animal Model: Male Swiss Webster mice(6-8-week-old) subcutaneous injected with psychoactive substances[1]
Dosage: 1, 2, 4, 5, 10 mg/kg
Administration: s.c.; single dose
Result: Blocked the antinociception of morphine at a dose of 10 mg/kg. showed AD50s of 2.02 mg/kg (95% CL) against 10 mg/kg morphine, and 4.02 mg/kg (95% CL) against 0.1 mg/kg fentanyl.
Animal Model: Male Swiss Webster mice(6-8-week-old) subcutaneous injected with psychoactive substances[1]
Dosage: 1, 3.2, 10, 32 mg/kg
Administration: s.c.; single dose at 20min post-fentanyl
Result: Demonstrated a potent reversal effect on fentanyl-induced respiratory depression at both 10 and 32 mg/kg doses. Increased both respiratory frequency and tidal volume. Showed beneficial effect within a short time frame, appearing 10 min postadministration for the 32 mg/kg dose and 15 min postadministration for the 10 mg/kg dose.
Molecular Weight

374.90

Formula

C21H27ClN2O2
CAS No.
SMILES

C=CCN(CCC1)CCCC1N(C(C2=COC=C2)=O)C3=CC=CC=C3.Cl
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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Mu opioid receptor antagonist 9 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:

Mu opioid receptor antagonist 93058600-77-1Mu opioid receptor antagonist9Mu opioid receptor antagonist-9Opioid Receptorpotent mu opioid receptor antagonistantagonism studiesInhibitorinhibitorinhibit

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