1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor

Naltrindole hydrochloride 

Cat. No.: HY-101177 Purity: 99.68%
Handling Instructions

Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.

For research use only. We do not sell to patients.

Naltrindole hydrochloride Chemical Structure

Naltrindole hydrochloride Chemical Structure

CAS No. : 111469-81-9

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10 mM * 1 mL in DMSO USD 119 In-stock
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Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
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Estimated Time of Arrival: December 31
25 mg USD 324 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 564 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.

IC50 & Target

Ki: 0.02 nM (δ opioid), 64 nM (μ opioid), 66 nM (κ opioid)[1]

In Vitro

Opioid drugs exert a wide spectrum of physiological and behavioral effects. These effects are mediated via membrane-bound receptors, of which the best characterized are the kappa, delta, and mu receptors[1]. Naltrindole inhibits the proliferation of cultured human U266 MM cells in a time- and dose-dependent manner with an EC50 of 16 μM. Treatment of U266 cells with naltrindole significantly decreases the level of the active, phosphorylated form of the kinases, extracellular signal-regulated kinase and Akt, which may be related to its antiproliferative activity[2]. Naltrindole inhibits growth and induces apoptosis in the three characteristic SCLC cell lines, NCI-H69, NCI-H345, and NCI-H510. Naltrindole treatment reduces constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells and also its downstream effectors glycogen synthase kinase-3β and the Forkhead transcription factors AFX and FKHR[3].

In Vivo

Naltrindole significantly decreases tumor cell volumes in human MM cell xenografts in severe combined immunodeficient mice[2]. In mice, naltrindole at 20 mg/kg s.c. antagonizes the δ-selective agonist effect of [D- Ser, Leu, Thr]enkephalin (DSLET) without blocking the antinociceptive effect of morphine or U50488H. Naltrindole is the only highly selective δ antagonist that is active upon peripheral administration[4]. Acute naltrindole induces significant decreases in external and total ambulation (horizontal activity) and rearing behaviour (vertical activity), as well as a significant increase in grooming frequency. In animals chronically treated with naltrindole there is an increase in total ambulation one day after the discontinuation of the treatment[5].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 188 mg/mL (416.89 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2175 mL 11.0875 mL 22.1749 mL
5 mM 0.4435 mL 2.2175 mL 4.4350 mL
10 mM 0.2217 mL 1.1087 mL 2.2175 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

U266 cells are plated in 96-well plates at 2000 cells per well in 100 μL of RPMI 1640 medium, supplemented with 10% fetal bovine serum, 100 U/mL penicillin, and 100 μg/mL streptomycin sulfate. Cells are incubated in quadruplicate in the presence of the various antineoplastic agents to construct dose-response curves, alone or in combination with various doses of naltrindole. At the end of the incubation 10 μL of WST-1 cell proliferation reagent is added to each well, and the plates are returned to the incubator for 1 h. Absorbance is then measured[2].

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

Animal Administration
[2][5]

Rats:
Effects of neonatal naltrindole treatments on open field activity is tested in 20-day old rats. The animals are injected chronically with saline or naltrindole (1 mg/kg, s.c.) (from birth to day 19), and 1 day after the discontinuation of this treatment are studied for the acute effects of naltrindole (1 mg/kg, i.p.)[5].

Mice:
Naltrindole is dissolved in distilled water to make a 3 mg/mL solution, and mice are injected with 10 mL/kg daily. Human RPMI 8226 multiple myeloma cells are inoculated subcutaneously into both flanks of SCID mice (10 million cells per flank). After 8 days, 12 mice are divided into two groups of six mice each: vehicle-injected and naltrindole-injected (30 mg/kg). Animals are dosed daily for 36 days, and body weights and xenograft tumors are measured twice a week with a digital caliper[2].

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

References
Molecular Weight

450.96

Formula

C₂₆H₂₇ClN₂O₃

CAS No.

111469-81-9

SMILES

O[[email protected]@]1(CC(C(C=CC=C2)=C2N3)=C3[[email protected]]4([H])OC5=C6O)[[email protected]]74C5=C(C=C6)C[[email protected]@]1([H])N(CC8CC8)CC7.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Naltrindole hydrochloride
Cat. No.:
HY-101177
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Naltrindole hydrochloride

Cat. No.: HY-101177