Naltrexone

Manufactured by Bio-Techne

Sourced in United Kingdom

Naltrexone is a laboratory reagent used in research applications. It functions as an opioid antagonist, blocking the effects of opioid drugs. Naltrexone is commonly used in studies involving opioid receptors and their interactions with various compounds.

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Lab products found in correlation

8 protocols using naltrexone

DPDPE and Naltrexone Binding Assay

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[D-Pen²,D-Pen⁵]enkephalin (DPDPE) and naltrexone were purchased from Tocris
Bioscience (Bristol, UK). Concentrated solutions (1 mM) were made
in bidistilled water and kept at −20 °C until use. The
medium and reagents for cell culture were from Euroclone (Milan, Italy).
Fluo-4 AM and pluronic acid were from Invitrogen/ThermoFisher Scientific
(Waltham, USA). N-(2-Hydroxyethyl)piperazine-N′-ethanesulfonic acid (HEPES), probenecid, brilliant
black, and bovine serum albumin (BSA) fraction V were from Sigma-Aldrich
(St. Louis, USA).

Pacifico S., Albanese V., Illuminati D., Marzola E., Fabbri M., Ferrari F., Holanda V.A., Sturaro C., Malfacini D., Ruzza C., Trapella C., Preti D., Lo Cascio E., Arcovito A., Della Longa S., Marangoni M., Fattori D., Nassini R., Calò G, & Guerrini R. (2021). Novel Mixed NOP/Opioid Receptor Peptide Agonists. Journal of Medicinal Chemistry, 64(10), 6656-6669.

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Chemical Sympathectomy and CB1 Receptor Modulation

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Rimonabant (Tocris) was dissolved in 4% DMSO and 1% Tween-80 in saline and administered i.p at 5 mg/kg (10 mL/kg). Naltrexone (Tocris) was dissolved in saline and administered i.p at 10 mg/kg (10 mL/kg). Naloxone (Sigma-Aldrich) was dissolved in saline and administered i.p at 2 mg/kg (10 mL/kg). CGS15943 was dissolved in 5% DMSO, 0.3% Tween-80 in saline and administered i.p at 10 mg/kg (1 mL/kg). For induction of chemical sympathectomy, 6-OHDA free base (Tocris) was dissolved in 0.1% ascorbic acid in saline and administered i.p at 100 mg/kg (10 mL/kg) one week prior to ET injection. BCI (EMD Millipore) was dissolved in 1% DMSO in saline and administered intrathecally (1.6 μg in 5 μL).

Yang N.J., Isensee J., Neel D., Quadros A.U., Zhang H.X., Lauzadis J., Liu S.M., Shiers S., Belu A., Palan S., Marlin S., Maignel J., Kennedy-Curran A., Tong V.S., Moayeri M., Röderer P., Nitzsche A., Lu M., Pentelute B.L., Brüstle O., Tripathi V., Foster K.A., Price T.J., Collier R.J., Leppla S.H., Puopolo M., Bean B.P., Cunha T.M., Hucho T, & Chiu I.M. (2021). Anthrax toxins regulate pain signaling and can deliver molecular cargoes into Antxr2+ DRG sensory neurons. Nature neuroscience, 25(2), 168-179.

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Evaluation of Linalool-Rich Lavender Oil

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LAV EO and neutral vegetable oil (i.e. avocado oil) were obtained from a commercial source (Quinarí, Ponta Grossa, Brazil) and both were diluted in cereal alcohol (Cloroquímica, Curitiba, Brazil) at a concentration of 5% (v/v) following previous studies.^{8 (link)} The same batch of LAV EO was used in all experiments, which was evaluated by gas chromatography-mass spectrometry (GC/MS, provided by Quinarí) and presented 30% of linalool and 40% of linalyl acetate as main constituents, which is in accordance with the pattern stablished by ISO-3515:2002.²² Ketamine hydrochloride (50 mg/kg; Syntec, São Paulo, Brazil) and Xylasin hydrochloride (7 mg/kg; Syntec, São Paulo, Brazil) were used as anesthetics. Some experiments were carried out with formalin administration (Alphatec, Brazil) diluted to 2,5% in 0,9% sterile saline solution (Equiplex Pharmaceutical Industry, Goiania, Brazil). Naltrexone (from Tocris Bioscience, Bristol, UK) was diluted in saline sterile solution and the dose used was based on previous studies.^{23 (link)} All drugs were freshly prepared just before the experiments.

LEJEUNE V.B., LOPES R.V., BAGGIO D.F., KOREN L.D., ZANOVELI J.M, & CHICHORRO J.G. (2023). Antinociceptive and anxiolytic-like effects of Lavandula angustifolia essential oil on rat models of orofacial pain. Journal of Applied Oral Science, 30, e20220304.

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Investigating CRF and Naltrexone Interactions

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Human/rat CRF and naltrexone (NTX) were purchased from Tocris Bioscience (Minneapolis, MN). CFA and lidocaine were obtained from Sigma-Aldrich (St. Louis, MO). Other reagents were from Sigma-Aldrich. All compounds were dissolved in saline.

Chen W., Taché Y, & Marvizón J.C. (2018). Corticotropin Releasing Factor in the brain and blocking spinal descending signals induce hyperalgesia in the latent sensitization model of chronic pain. Neuroscience, 381, 149-158.

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Pharmacological Modulation of Addiction

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The ethanol solution (10% v/v) was prepared using 95% ethyl alcohol and tap water.
Morphine sulfate (Sigma Aldrich, St. Louis, MO) was dissolved in isotonic saline. In the dose-response study, morphine (0, 0.5, 1 and 2 mg/kg, 1 ml/kg, subcutaneous (s.c.)) was acutely administered according to a within-subject design. When co-administered with DTG, morphine (0, 0.75 mg/kg/inj., total dose 1.5 mg/kg/day, s.c.) was given 20 min before each injection of DTG, hence twice daily.
naltrexone (Sigma Aldrich, St. Louis, MO) was dissolved in isotonic saline. In the dose-response study, naltrexone (0, 0.0083, 0.025, 0.075 mg/kg, 1 ml/kg, s.c.) was acutely administered according to a within-subject design. When co-administered with DTG, naltrexone (0, 0.0125 mg/kg/inj.) was given 10 min before each injection of DTG, hence twice daily (total dose 0.025 mg/kg/day).
The SigR agonist 1, 3-di-(2-tolyl) guanidine (DTG, Tocris Bioscience, Ellisville, MO) was suspended in isotonic saline with a few drops of Tween-20 and administered subchronically (0, 7.5 mg/kg, 2 ml/kg, s.c.) twice a day for 7 days (total dose 15 mg/kg/day). Dose and schedule of DTG administration was based on our previous report showing its effects on ethanol intake in Scr:sP rats (Sabino et al., 2011 (link)).

Valenza M., Blasio A., DiLeo A., Cottone P, & Sabino V. (2020). Sigma receptor-induced heavy drinking in rats: Modulation by the opioid receptor system. Pharmacology, biochemistry, and behavior, 192, 172914.

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Synthesis and Pharmacological Evaluation of Opioid-NT Hybrid Peptide

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The opioid–NT hybrid peptide—PK23 (Tyr-d-Ala-Phe-Phe-Lys-Lys-Pro-Phe-Ile-Leu-OH) was designed and prepared at the Department of Neuropeptides of the Mossakowski Medical Research Centre PAS (Warsaw, Poland) by manual solid-phase peptide synthesis using N-fluorenylmethoxycarbonyl (Fmoc) chemistry. Morphine was obtained from Polfa (Warsaw, Poland) and similarly to the chimera tested, was dissolved in saline. NT as well as naltrexone, an opioid receptor antagonist together with SR 48692 and NTRC 824, NTS1 and NTS2 receptor selective antagonists, respectively, were purchased from Tocris Bioscience (Germany). The anaesthetic drugs ketamine and xylazine were purchased from Biowet (Pulawy, Poland) while isoflurane was obtained from Baxter (Cracow, Poland).
Guanosine-5-[γ-³⁵S]-triphosphate (1000 Ci/mmol, [³⁵S]GTPγS) was purchased from Hartmann Analytic (Braunschweig, Germany), whereas [³H]DAMGO was purchased from PerkinElmer (Waltham, MA, USA). EDTA, bovine serum albumin (BSA), polyethylenimine (PEI), tris(hydroxymethyl)amino-methane (Tris), guanosine 5′-diphosphate (GDP), unlabeled GTPγS, and peptidase inhibitors—bestatin, bacitracin and phosphoramidon were purchased from Sigma–Aldrich (St. Louis, MO, USA).

Frączek K., Ferraiolo M., Hermans E., Bujalska-Zadrozny M., Kasarello K., Erdei A., Kulik K., Kowalczyk A., Wojciechowski P., Sulejczak D., Sosnowski P., Granica S., Benyhe S., Kaczynska K., Nagraba L., Stolarczyk A., Cudnoch-Jedrzejewska A, & Kleczkowska P. (2020). Novel opioid-neurotensin-based hybrid peptide with spinal long-lasting antinociceptive activity and a propensity to delay tolerance development. Acta Pharmaceutica Sinica. B, 10(8), 1440-1452.

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Pharmacological Modulation of Opioid Signaling

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Ketamine (10–30 mg/kg, MWI Veterinary Supply Co.), Naltrexone (5 mg/kg, Tocris, 0677), beta-funaltrexamine (β-FNA, 15 mg/kg, Sigma Aldrich, O003), norbinaltorphimine (norBNI, 10 mg/kg, Tocris, 0347), and cocaine (10 mg/kg, Sigma Aldrich, C5776) were all dissolved in 0.9% normal saline. 4-hydroxytamoxifen (4OHT, 50 mg/kg, Sigma Aldrich, T176) was dissolved in warm ethanol (50 μl / mg 4OHT) and mixed into sunflower oil (80 μl / mg 4OHT) and castor oil (20 μl / mg 4OHT), followed by vacuum centrifugation to evaporate out the ethanol. Drugs were administered intraperitoneally (i.p.) at a volume of 10 mL/kg. For all experiments involving drug injection, matched control groups always received the same total number of drug or SAL injections.
For local inhibition of MORs in the CeA, mice were bilaterally microinjected with CTAP (300 ng in 500 nL in saline, Sigma Aldrich, C6352) 5 min before behavioral testing. CTAP was infused through an injector cannula coupled to a 5 μL Hamilton syringe using a microinfusion pump (Harvard Apparatus) at a continuous rate of 150 nL min⁻¹ to a total volume of 0.5 μL per hemisphere. Injector cannulas were removed 1 min after infusions were complete.

Pomrenze M.B., Vaillancourt S., Llorach P., Rijsketic D.R., Casey A.B., Gregory N., Salgado J.S., Malenka R.C, & Heifets B.D. (2024). Opioid receptor expressing neurons of the central amygdala gate behavioral effects of ketamine in mice. bioRxiv.

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Injections of Opioid Receptor Ligands

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U50,488 ((trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclo-hexyl] benzeneacetamide; Tocris Biosciences, Ellisville, MO) and norbinaltorphimine (nor-BNI; Tocris Biosciences, Ellisville, MO) were dissolved in 0.9% saline solution for intraperitoneal (i.p.) injections. Naltrexone (Tocris Biosciences, Ellisville, MO) was dissolved in 0.9% saline solution for subcutaneous (s.c.) injections.

Harshberger E., Gilson E.A., Gillett K., Stone J.H., El Amrani L, & Valdez G.R. (2016). nor-BNI Antagonism of Kappa Opioid Agonist-Induced Reinstatement of Ethanol-Seeking Behavior. Journal of Addiction, 2016, 1084235.

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