Naltrindole

Manufactured by Merck Group

Sourced in United States, Sao Tome and Principe

Naltrindole is a laboratory reagent used in scientific research. It functions as a selective delta-opioid receptor antagonist, which is a class of compounds that block the activity of delta-opioid receptors. Naltrindole is commonly utilized in experiments and studies involving the endogenous opioid system and its role in various physiological and behavioral processes.

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Lab products found in correlation

23 protocols using naltrindole

Microinjections into PAG Subregions in Rats

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For intra-vlPAG injections, isoflurane-anesthetized rats were mounted in a stereotaxic frame and lidocaine (2%; 0.1 μl, 0.2 μl or 1.0 μl), naltrindole (2.0 nmol; 0.2 μl) (Sigma Chemical Co., St. Louis, MO) or an equivalent volume of saline was injected bilaterally into the vlPAG with a Hamilton syringe connected to cannulae lowered vertically 0.8 mm lateral and 8.3 mm caudal from bregma and 6.2 mm below the dural surface.²⁹ For dorsolateral PAG (dlPAG) injections, 2% lidocaine, 0.2 nmol naltrindole or 0.2 μl saline was injected bilaterally 0.8 mm lateral and 8.3 mm caudal to bregma and 4.6 mm below the dural surface.^{14 (link),16 (link)}Lidocaine and naltrindole were dissolved in saline containing 0.2% Chicago Sky Blue dye to mark the injection sites. Drug doses were selected from dose-response studies published previously.^{13 (link),16 (link)} Stereotaxic injections were delivered at a constant rate over a 1 min period and, two minutes later, LPS (1.0 mg/kg) or saline (1 ml/kg) was administered i.v. At the end of each experiment, rats were sacrificed with an overdose of isoflurane, brains were removed, sectioned (50 μm) and stained with eosin to confirm the location of cannulae. Only data from confirmed cannula placements were included in this report.

Millington W.R., Yilmaz M.S, & Feleder C. (2016). The initial fall in arterial pressure evoked by endotoxin is mediated by the ventrolateral periaqueductal gray. Clinical and experimental pharmacology & physiology, 43(6), 612-615.

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Pharmacological Agents Used in Neuroscience

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6’-Guanidinonaltrindole (6’-GNTI), U50488, naltrindole, U0126, and λ-Carrageenan were purchased from Sigma-Aldrich (St. Louis, MO). [D-Pen2,D-Pen5]Enkephalin (DPDPE), and bradykinin (BK) were purchased from Bachem Americas, Inc. (Torrance, CA). ICI-199441 was purchased from Tocris (Minneapolis, MN). Prostaglandin E2 (PGE₂), 12-HETE, 15-HETE, baicalein and luteolin were purchased from Cayman Chemicals (Ann Arbor, MI). SCH772984 was purchased from Selleckchem (Houston, TX). ¹²⁵I-cAMP was purchased from PerkinElmer Life and Analytical Sciences (Waltham, MA). Nerve growth factor was from Harlan (Houston, TX). Collagenase was from Worthington (Lakewood, NJ). Hank’s balanced salt solution, feta l bovine serum, Dulbecco’s modified Eagles Medium (DMEM) were purchased from Invitrogen Corp. (Carlsbad, CA). All other drugs and chemical (reagent grade) were purchased from Sigma-Aldrich.

Jacobs B.A., Pando M.M., Jennings E.M., Jamshidi R.J., Zamora J.C., Chavera T.S., Clarke W.P, & Berg K.A. (2019). Signaling characteristics and functional regulation of delta opioid-kappa opioid receptor (DOP-KOP) heteromers in peripheral sensory neurons. Neuropharmacology, 151, 208-218.

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Delta Opioid Receptor Agonist Protocol

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UFP-512 was synthetized by Balboni et al. (2002) (link), SFN was acquired from Merck Chemicals and Life Science S.A.U (Madrid, Spain), and naltrindole and naloxone were purchased in Sigma–Aldrich (St. Louis, MO, United States). UFP-512 was dissolved in saline solution (0.9%) and intraperitoneally administered at 1, 3, 10, 20, and 30 mg/kg. SFN was dissolved in dimethylsulfoxide (1% in saline solution 0.9%) and intraperitoneally administered at 10 mg/kg. naltrindole and naloxone were also diluted in saline solution (0.9%) and subcutaneously administered at 4 and 1 mg/kg, respectively. All drugs were prepared daily just before use and administered in a final volume of 10 ml/kg, at 1 h (UFP-512), 3 h (SFN), and 30 min (naltrindole and naloxone) before testing in accordance to our previous pilot studies and other works (Aguila et al., 2007 (link); Hervera et al., 2013 (link); Carcolé et al., 2014 (link); Redondo et al., 2017 (link); Ferreira-Chamorro et al., 2018 (link)). For each group treated with a drug, the respective control group received the same volume of corresponding vehicle.

Polo S., Díaz A.F., Gallardo N., Leánez S., Balboni G, & Pol O. (2019). Treatment With the Delta Opioid Agonist UFP-512 Alleviates Chronic Inflammatory and Neuropathic Pain: Mechanisms Implicated. Frontiers in Pharmacology, 10, 283.

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Pharmacological Investigation of Pain Relief

Cited 3 times

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DADS and GYY4137, purchased from Sigma–Aldrich (St. Louis, MO, USA), were dissolved in SS, and intraperitoneally injected in a final volume of 10 mL/kg at 1 h, before testing in compliance with other works [23 (link),33 (link)].
Morphine hydrochloride purchased from Alcaiber S.A. (Madrid, Spain), UFP-512 synthesized by [34 (link)], and naloxone and naltrindole obtained from Sigma–Aldrich (St. Louis, MO, USA), were dissolved in SS and intraperitoneally or subplantarly injected in a final volume of 10 mL/kg or 30 µL, in agreement with previous studies [18 (link),23 (link),29 (link),32 (link)].
All drugs were prepared just before use. For each group injected with a drug, the corresponding control group received the identical volume of SS.

Bai X., Batallé G., Balboni G, & Pol O. (2022). Hydrogen Sulfide Increases the Analgesic Effects of µ- and δ-Opioid Receptors during Neuropathic Pain: Pathways Implicated. Antioxidants, 11(7), 1321.

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Opioid Receptor Pharmacology Protocol

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The compounds used were: loperamide HCl (Sigma, St. Louis, MO), oxymorphindole HCl^{14 (link)}, β-funaltrexamine^{18 (link)}, naltrindole^{19 (link)}, and naloxone methiodide (Sigma, St. Louis, MO). Stock solutions were prepared with 5% Cremophor EL and 5% DMSO in H2O. All drugs were diluted to testing concentrations with 0.9% sterile saline (or aCSF for electrophysiology) such that final Cremophor and DMSO concentrations were <1%; the topical vehicle was further diluted 1:1 with 95% ethanol. The routes and volumes of administration were: intrathecal (i.t.), 5 μL; intraplantar (i.pl.), 30 μL; subcutaneous (s.c.), 10 μL per gram; and topical, 20 μL. Intrathecal injections were performed as previously described^{20 (link)}. For i.pl. injections and topical administration, animals were lightly anesthetized with 2.5% isoflurane and the drugs were administered to the left hindpaw.

Bruce D.J., Peterson C.D., Kitto K.F., Akgün E., Lazzaroni S., Portoghese P.S., Fairbanks C.A, & Wilcox G.L. (2019). The combination of a delta-opioid receptor agonist and loperamide produces peripherally-mediated analgesic synergy in mice. Anesthesiology, 131(3), 649-663.

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Antinociceptive Effects of CBHE and Cnicin

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The agonist and antagonist drugs and the dosage were selected according to the previous studies and on pilot experiments in our laboratory (21 (link)22 (link)23 ). For all tests, the CBHE (50, 150, and 300 mg/kg, i.p.) and cnicin (8, 20, and 30 mg/kg, i.p.) were dissolved in dimethyl sulfoxide (DMSO). Morphine sulfate (Morph; 1 mg/kg, i.p.), naloxone (NLX; 1 mg/kg, i.p.), diclofenac (Diclo; 10 mg/kg, i.p.), and xylazine were purchased from Daroopakhsh (Iran). Acetic acid and formalin were purchased from Merck (Germany). Cnicin isolated from Cnicus benedictus L., L-arg hydrochloride (L-arg HCL; 25, 50, 100 μg/paw), Nω-nitro-L-arg methyl ester hydrochloride (L-NAME; 25, 50, 100 μg/paw), sodium nitroprusside (SNP; 125, 250, 500 μg/paw), methylene blue (MB; 100, 200, 400 μg/paw), glibenclamide (Gli; 25, 50, 100 μg/paw), naltrindole (NAL; 0.99 mg/kg, i.p.), nor-binaltorphimine (NBT; 1.03 mg/kg, i.p.), naloxonazine (NAX; 3.5 mg/kg, i.p.), and glutamate all were purchased from Sigma Aldrich Company; USA.

Ahmadimoghaddam D., Sadeghian R., Ranjbar A., Izadidastenaei Z, & Mohammadi S. (2020). Antinociceptive activity of Cnicus benedictus L. leaf extract: a mechanistic evaluation. Research in Pharmaceutical Sciences, 15(5), 463-472.

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Hypoxia-Induced Cellular Responses

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For drug treatments, UFP-512, a specific and effective DOR agonist, was synthesized by our research teams (Balboni et al., 2002 (link); Chao et al., 2007 (link)), naltrindole, a particular DOR antagonist (Zhang et al., 2006 (link); Granier et al., 2012 (link)), was purchased from Sigma (St. Louis, MO, United States), tumor necrosis factor-α (TNF-α) was purchased from R&D Systems (Minneapolis, MN, United States), they were added into the culture medium in demanded concentrations and exposed to normoxic or hypoxic conditions starting immediately before the onset of hypoxia (or at the same time-point in normoxia).

Luo F., Xu R., Song G., Lu H., He X, & Xia Y. (2020). The δ-Opioid Receptor Differentially Regulates MAPKs and Anti-inflammatory Cytokines in Rat Kidney Epithelial Cells Under Hypoxia. Frontiers in Physiology, 10, 1572.

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Opioid Receptor Agonists and Antagonist Effects

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SFN was acquired from Merck Chemicals and Life Science S.A.U. (Madrid, Spain), dissolved in dimethyl sulfoxide (DMSO; 1% solution in saline) and administered intraperitoneally 2–3 hours before behavioral testing. DPDPE, SNC-80 and naltrindole were purchased from Sigma-Aldrich (St. Louis, MO). DPDPE was dissolved in saline solution (0.9% NaCl) and SNC-80 and naltrindole were dissolved in DMSO (1% solution in saline). DPDPE and SNC-80 were administered subcutaneously and naltrindole intraperitoneally, 30 min before behavioral testing. All compounds were freshly prepared before use and administered in a final volume of 10 ml/kg. Control animals received the same volume of vehicle.

McDonnell C., Leánez S, & Pol O. (2017). The induction of the transcription factor Nrf2 enhances the antinociceptive effects of delta-opioid receptors in diabetic mice. PLoS ONE, 12(7), e0180998.

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Solvent Effects on TPI Compound Assays

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In all assays, TPI compounds were dissolved
in 10% dimethyl sulfoxide, a concentration that did not produce any
detectable behavioral effect. Morphine sulfate, naloxone, nor-binaltorphimine
(nor-BNI), and naltrindole were purchased from Sigma-Aldrich (St.
Louis, MO) and dissolved in 0.9% sterile saline.

Houghten R.A., Ganno M.L., McLaughlin J.P., Dooley C.T., Eans S.O., Santos R.G., LaVoi T., Nefzi A., Welmaker G., Giulianotti M.A, & Toll L. (2015). Direct Phenotypic Screening in Mice: Identification of Individual, Novel Antinociceptive Compounds from a Library of 734 821 Pyrrolidine Bis-piperazines. ACS Combinatorial Science, 18(1), 51-64.

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Solid-Phase Synthesis of EM-1 and EM-2 Peptides

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EM-1 and EM-2 were prepared by manual solid-phase synthesis using standard N-fluorenylmethoxycarbonyl (Fmoc) chemistry as reported in our previous study [32 (link)]. Fmoc-protected amino acids (GL Biochem Ltd., China) were coupled with Rink amide 4-methybenzhydrylamine (MBHA) resin (Tianjin Nankai Hecheng Science & Technology Co., Ltd., China). The crude peptides were purified by preparative reversed-phase HPLC (RP-HPLC) and determined by electrospray ionization mass spectrometer (ESI-Q-TOF maXis-4G, Bruker Daltonics).
Naloxone, β-FNA, nor-binaltorphimine (nor-BNI), and naltrindole (NTI) were obtained from Sigma-Aldrich. The selective p38 MAPK inhibitor SB203580 was purchased from Beyotime Institute of Biotechnology and dissolved in 1% DMSO in saline. All other drugs were dissolved in sterilized saline and stored at − 20 °C.

Zhang T., Zhang N., Zhang R., Zhao W., Chen Y., Wang Z., Xu B., Zhang M., Shi X., Zhang Q., Guo Y., Xiao J., Chen D, & Fang Q. (2018). Preemptive intrathecal administration of endomorphins relieves inflammatory pain in male mice via inhibition of p38 MAPK signaling and regulation of inflammatory cytokines. Journal of Neuroinflammation, 15, 320.

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