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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
5 mg USD 108 In-stock
10 mg USD 150 In-stock
25 mg USD 324 In-stock
50 mg USD 564 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


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].

Preparing Stock Solutions
Concentration Volume 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.
Cell Assay

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

Naltrindole is dissolved in distilled water or saline.

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].

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.

Molecular Weight







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

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥188 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name



Applicant name *


Email address *

Phone number *


Organization name *

Country *


Requested quantity *


Bulk Inquiry

Inquiry Information

Product Name:
Naltrindole hydrochloride
Cat. No.: