Sb366791

Manufactured by Merck Group

Sourced in United States

SB366791 is a selective antagonist of the transient receptor potential vanilloid 4 (TRPV4) ion channel. It is used in research applications as a tool compound to investigate the role of TRPV4 in various biological processes.

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14 protocols using sb366791

Investigating Leech Nociception Modulation

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Drugs used for each experiment were kept as frozen aliquot solutions and then diluted to their final concentration in normal Hirudo saline (110 mM NaCl, 5 mM NaOH, 4 mM KCl, 1.8 mM CaCl₂, 1 mM MgCl₂, and 10 mM HEPES, pH = 7.4) just before the start of the experiment. Allyl isothiocyanate (AITC), 2-arachidonylglycerol (2-AG), and anandamide stocks were made in dimethyl sulfoxide (DMSO). 2-AG, anandamide DMSO, and SB366791 (TRPV1 antagonist) were obtained from Tocris (Ellisville, MO), while AITC was obtained from Sigma-Aldrich (St. Louis, MO).
Prior to drug injections, animals were lightly anesthetized with ice-cold saline in an ice-lined dissecting dish and injected with 100 μL of either 100 μM anandamide, 100 μM of anandamide +25 μM of SB366791, 75 μM 2-AG, or 75 μM 2-AG +25 μM SB366791. Pilot studies examining the effects of SB366791 injections found that concentrations greater than 25 μM reduced responses to nociceptive stimuli. For vehicle control experiments, 100 μL of 0.01% DMSO were injected. As previously reported^{36 (link)}, injections were made just anterior of the posterior sucker, a region where the dorsal and ventral sinuses that are part of the leech vascular system converge¹⁹. The leech CNS is contained within the ventral sinus so this method of injection is likely to be effective in delivering drugs to the CNS.

Summers T., Hanten B., Peterson W, & Burrell B. (2017). Endocannabinoids Have Opposing Effects On Behavioral Responses To Nociceptive And Non-nociceptive Stimuli. Scientific Reports, 7, 5793.

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Intrathecal Catheter Implantation and Drug Administration in Rats

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The rats were anesthetized by sodium pentobarbital (40 mg/kg, i.p.) in order to implant intrathecal catheter for administration of drugs 3 days prior to each experiment. Briefly, one end of polyethylene-10 tubing was inserted intrathecally through an incision in the cisternal membrane and advanced 7-9 cm caudal until the tip of the catheter was positioned at the lumbar spinal level (L5 to L6). The other end of the intrathecal tubing was sutured to the musculature and skin at the incision site and externalized to the back of the rat. In each experiment, a Hamilton microsyringe (250 µl) was connected to the intrathecal tubing and used to deliver 100 μl of dimethyl sulfoxide (DMSO) as control, FSLLRY-NH2 (PAR2 antagonist, 10 μg), SB366791 (TRPV1 antagonist, 100 μM) and HC030031 (TRPA1 antagonist, 10 μg) (Kanai et al. 2006 ) (obtained from Sigma-Aldrich).
In a subset of studies, in order to examine the effects of PAR2 on expression of TRPV1 and TRPA1 and engagement of substance P and CGRP FSLLRY-NH2 (10 μg), SB366791 (100 μM) and HC030031 (10 μg) were intrathecally given using an infusion pump in control rats and rats 4 weeks following SCI, respectively. The pump was set to constantly deliver vehicle or the drugs over a period of 3 h. At the end of infusion, the superficial dorsal horn tissues were obtained under an anatomical microscope for Western Blot and ELISA experiments.

Wei H., Wei Y., Tian F., Niu T, & Yi G. (2016). Blocking proteinase-activated receptor 2 alleviated neuropathic pain evoked by spinal cord injury. Physiological research, 65(1).

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CBD Effects on Neuronal Activity

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Cannabidiol (2-[(1R,6R)-3-methyl-6-(1-methylethenyl)-2-cyclohexen-1-yl]-5-pentyl-1,3-benzenediol) was obtained from Tocris Bioscience (Bio-Techne, Abingdon, United Kingdom). AM281 (CB₁ receptor antagonist; 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-4-morpholinyl-1H-pyrazole-3-carboxamide) and AM630 (CB₂ receptor antagonist; 6-iodo-2-methyl-1-(2-morpholin-4-ylethyl)indol-3-yl]-(4-methoxyphenyl)methanone) were obtained from Cayman Chemicals (Ann Arbor, MI). SB-366791 (N-(3-methoxyphenyl)-4-chlorocinnamide), rhodamine 6G, cremophor, dimethyl sulphoxide (DMSO), urethane, and MIA were obtained from Sigma-Aldrich (St. Louis, MO). Solutions of CBD, AM281, AM630, and SB-366791 were prepared in vehicle (1:1:18; DMSO:cremophor:saline) on the day of use. rhodamine 6G (0.05%) and MIA were dissolved in saline. Physiological buffer (135 mM NaCl, 20 mM NaHCO3, 5 mM KCl, 1 mM MgSO4*7H2O, pH = 7.4) was prepared in the laboratory.

Philpott H.T., O'Brien M, & McDougall J.J. (2017). Attenuation of early phase inflammation by cannabidiol prevents pain and nerve damage in rat osteoarthritis. Pain, 158(12), 2442-2451.

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Quantifying TRPV1 Receptor Binding

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Receptor binding characteristics were studied by displacement assays using TRPV1 selective agonists (capsaicin, anandamide, and RTX; Sigma Aldrich) and antagonists (capsazepine, 5-I-RTX, and SB-366791; Sigma Aldrich). Aliquots of 100 µL of membrane suspension (1 mg protein/mL) were incubated with increasing concentrations (10^-10-10^-3 M) of the TRPV1 unlabelled agonists and antagonists in presence of 1.2 nM ³[H]RTX. The concentration of unlabelled ligand that it took to inhibit 50% (IC₅₀) of ³[H]RTX specific binding was determined from the competition curves obtained by nonlinear regression analysis of the data (GraphPad Prism; GraphPad Software). The fit of the one-site model was tested by R² by nonlinear regression and by the runs test. The affinity constant (Ki) for the competitors were calculated using the Cheng-Prussoff equation [17 (link)].

Vercelli C., Barbero R., Cuniberti B., Racca S., Abbadessa G., Piccione F, & Re G. (2014). Transient Receptor Potential Vanilloid 1 Expression and Functionality in MCF-7 Cells: A Preliminary Investigation. Journal of Breast Cancer, 17(4), 332-338.

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Immunofluorescent Labeling of Neuronal Markers

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Primary antibodies used were: chick and rabbit EGFP (1:4,000 dilution; Abcam), mouse GAD65 (1:1,000), guinea pig (1:800 for uptake) and mouse syt1 (1:150 for uptake), rabbit alpha tubulin (1:5,000), mouse syb2 (1:1,000 dilution; Synaptic Systems), chick and mouse MAP2 (1:4,000 dilution; Millipore), sheep NGF, mouse reelin, guinea pig TRPV1 C-T (1:1,000, Millipore), mouse TRPV1 N-T (1:500; Neuromab), rabbit TRPV2, TRPV3, TRPV4 (1:500; Alomone), rabbit mGluR7 (1:500; Upstate), mouse PV25 (1:2,000 dilution; Swant), rabbit Somatostatin-14 (1:2,000 dilution; Bachem), rat Somatostatin-14 (1:1,000 dilution; Thermo Fisher), rabbit VIP (1:500 dilution; Abcam), mouse BDNF (1:500; Developmental Studies Hybridoma Bank; Yves Barde monoclonal #9). Secondary antibodies used were: guinea pig, mouse and rabbit HRP (1:5,000 dilution; BioRad) and chick, rabbit, guinea pig, mouse, rat and sheep Alexa 405, 488, 546 and 647 (1:2,000 dilution; Abcam/Invitrogen). Neurotrace was from Thermo Fisher.
Capsaicin and SB-366791 were purchased from Sigma-Aldrich. Methyllycaconitine (MLA) was from Abcam and dihydro-beta-erythroidine (DHBE), mecamylamine (MEC) picrotoxin, TTX, APV and CNQX were from Tocris. Recombinant Human TrkA Fc and TrkB Fc Chimera Proteins were from R & D Systems. All other reagents were from Carl Roth.

Hurtado-Zavala J.I., Ramachandran B., Ahmed S., Halder R., Bolleyer C., Awasthi A., Stahlberg M.A., Wagener R.J., Anderson K., Drenan R.M., Lester H.A., Miwa J.M., Staiger J.F., Fischer A, & Dean C. (2017). TRPV1 regulates excitatory innervation of OLM neurons in the hippocampus. Nature Communications, 8, 15878.

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Calcium Signaling in Cell Lines

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14,15-EET and 14,15-EE5ZE were from Cayman (Ann Arbor, MI). Quest Fluo-8 NW Calcium Assay Kit was from AAT Bioquest (AAT Bioquest Inc., Sunnyvale, CA, USA). Ca²⁺ free medium, capsaicin, capsazepine (CPZ), SB366791, HC030031 (HC), 1,2-Bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid/acetoxymethyl ester (BAPTA/AM), ethylene glycol tetraacetic acid (EGTA), Griess's reagent, and Drabkin's reagent kit 525 were from Sigma-Aldrich (St. Louis, MO, USA). TurboFect was from Fermentas (Glen Burnie, MD, USA). Matrigel was from BD Biosciences (San Jose, CA, USA).

Su K.H., Lee K.I., Shyue S.K., Chen H.Y., Wei J, & Lee T.S. (2014). Implication of Transient Receptor Potential Vanilloid Type 1 in 14,15-Epoxyeicosatrienoic Acid-induced Angiogenesis. International Journal of Biological Sciences, 10(9), 990-996.

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Cannabinoid Receptor Agonist Delivery

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CBD was obtained from THC-pharm (Frankfurt am Main, Germany). GW9662, HC-067047, AP-18, SB-366791, MIA and Kolliphor EL were obtained from Sigma-Aldrich (Darmstadt, Germany). Drugs were dissolved in a vehicle solution containing 5% Kolliphor^® EL and 5% ethanol in 0.9% saline. MIA was dissolved in 0.9% saline.

Mlost J., Kędziora M, & Starowicz K. (2021). Computational Approach Reveals Pronociceptive Potential of Cannabidiol in Osteoarthritis: Role of Transient Receptor Potential Channels. Pharmaceuticals, 14(10), 964.

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Vascular Responses to Oxidative Stress and Capsaicin

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Following each surgery, mice were given a bolus injection of the ganglionic blocker hexamethonium (HEX, 5 mg/kg, Sigma) to eliminate reflex adjustments and focus on the primary vascular actions of capsaicin. Initial studies were performed to determine the effects of continuous infusion of H₂O₂ and/or capsaicin administered in an escalating fashion at the rate of 20 μl/min for 4 min Hemodynamic response curves were performed in WT, db/db and V1KO mice, before and after inhibition of TRPV1 channels (SB366791—100 μg/kg iv, Sigma). 10 min elapsed following each inhibitor before H₂O₂ and/or capsaicin infusion began to allow for MAP to stabilize. Pressures and/or heart rate were continuously recorded throughout the experiment. A subset of db/db mice were injected (via tail vein administration) with PEG-Catalase (three times per week 7000 Units/injection) for 1 week and subjected to capsaicin to examine blood flow responses.

DelloStritto D.J., Connell P.J., Dick G.M., Fancher I.S., Klarich B., Fahmy J.N., Kang P.T., Chen Y.R., Damron D.S., Thodeti C.K, & Bratz I.N. (2016). Differential regulation of TRPV1 channels by H2O2: implications for diabetic microvascular dysfunction. Basic research in cardiology, 111(2), 21.

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Investigating Oxidative Stress Pathways

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The following chemicals and antibodies were obtained from Sigma-Aldrich (St. Louis, MO, USA): Complete Freund's adjuvant (CFA), rat serum albumin (RSA), hypochlorous acid (HOCl), amebocyte lysate assay kit, chloramine-T, acetic acid, 4% paraformaldehyde, bovine serum albumin (BSA), trypsin, collagenase type IA, DNase type IV, cytosine arabinoside, thiazolyl blue tetrazolium blue (MTT), dimethyl sulfoxide (DMSO), 2′,7′-dichlorofluorescein diacetate (DCFH-DA), phenylmethylsulfonyl fluoride (PMSF), protease and phosphatase inhibitors, Fura-2/AM, apocynin, N-acetyl-l-cysteine (NAC), and SB366791. Dulbecco’s modified Eagle’s medium (DMEM; 4.5 g/L glucose), fetal bovine serum (FBS), penicillin, streptomycin and glutamine were purchased from Gibco (CA, USA). Detoxi-Gel column and BCA Protein Assay Kit were purchased from Thermo Fisher Scientific (MA, USA).
The primary antibodies used in this study were rabbit anti-NADPH oxidase 1, anti-NADPH oxidase 2, anti-NADPH oxidase 4, rabbit anti-TRPV1, rabbit anti-calcitonin gene-related peptide (CGRP) and chicken anti-beta III Tubulin antibody and rabbit anti-β-actin from Abcam (MA, USA). Secondary antibodies conjugated with FITC or Cy3 were purchased from Abcam (MA, USA).

Ding R., Jiang H., Sun B., Wu X., Li W., Zhu S., Liao C., Zhong Z, & Chen J. (2016). Advanced oxidation protein products sensitized the transient receptor potential vanilloid 1 via NADPH oxidase 1 and 4 to cause mechanical hyperalgesia. Redox Biology, 10, 1-11.

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Preparation of Neurotransmitter Receptor Ligands

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A concentrated stock solution of NGF-7S at 10 μg/ml was made by dissolution in DMEM and stored at –30 °C until use. Concentrated stock solutions of 4-(3-chloro-2-pyridinyl)-N-[4-(1,1-dimethylethyl) phenyl]-1- piperazinecarboxamide (BCTC, 10 mM, Sigma), 5’-iodoresiniferatoxin (5’-IRTX; 200 μM; Alomone Labs, Jerusalem, Israel), capsaicin (10 mM, Sigma), capsazepine (10 mM, Sigma), icilin (50 mM, Sigma) and SB366791 (30 mM, Sigma) were made by dissolution in DMSO and stored at –30 °C until use. All other chemicals used were of analytical grade.

Kitamura N., Nagami E., Matsushita Y., Kayano T, & Shibuya I. (2018). Constitutive activity of transient receptor potential vanilloid type 1 triggers spontaneous firing in nerve growth factor-treated dorsal root ganglion neurons of rats. IBRO Reports, 5, 33-42.

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