Diltiazem

Manufactured by Merck Group

Sourced in United States, Germany, Belgium, France

Diltiazem is a laboratory equipment product manufactured by Merck Group. It is a calcium channel blocker used in scientific research and analysis.

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Lab products found in correlation

43 protocols using diltiazem

Immunoprofiling of Oligodendrocyte Lineage

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The following antibodies and chemicals were used for this study: rabbit anti-α-tubulin (Abcam catalog #ab15246, RRID: AB_301787; 1:500), Rabbit anti-β3-tubulin (TUBB3; Covance catalog #MMS-435P, RRID: AB_2313773, 1:2000), mouse anti-MBP (BioLegend catalog #836504, RRID: AB_2616694; 1:1000), goat anti-Olig2 (R&D Systems catalog #AF2418, RRID: AB_2157554; 1:20), and mouse anti-O4 IgM (R&D Systems catalog #MAB 1326, RRID: AB_357617; 1:200). Alexa Fluor-conjugated secondary antibodies were all purchased from Thermo Fisher Scientific with a dilution of 1:500. nifedipine, verapamil, diltiazem, NNC 55-0396, ω-conotoxin GVIA (ω-CTX), ω-agatoxin IVA, SKF96365, cyclopiazonic acid (CPA), thapsigargin (Tg), and ryanodine (Ry) were all purchased from Sigma.

Rui Y., Pollitt S.L., Myers K.R., Feng Y, & Zheng J.Q. (2020). Spontaneous Local Calcium Transients Regulate Oligodendrocyte Development in Culture through Store-Operated Ca2+ Entry and Release. eNeuro, 7(4), ENEURO.0347-19.2020.

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Calcium Signaling Modulation During Neural Development

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Neural tissue was dissected and dissociated in the same manner as calcium-imaged cultures, at the neural plate (st. 14), neural fold (st. 18), and neural tube (st. 22) stages. Cells were plated in MR containing 10 μM or 100 μM diltiazem (Sigma, St. Louis, MO), 1 μM or 10 μM (−)BayK-8644 (Sigma), MR alone, or MR with 0.05% dimethylsulfoxide (DMSO; BayK-8644 experiments only). The concentrations of diltiazem used in these experiments have previously been demonstrated to decrease calcium currents for VGCC α1 subunits in cell culture (Cai et al., 1997 (link); De Paoli et al., 2002 (link)), and the concentrations of (−)BayK 8644 used were shown to increase calcium activity in amphibian explants and cell culture (Moreau et al., 1994 (link); Takano et al., 2011 (link)). Cultures were fixed in 1X MEMFA when intact sibling embryos reached the swimming tadpole stage (35–36), and then stored in ethanol at −20°C.

Lewis B.B., Miller L.E., Herbst W.A, & Saha M.S. (2014). The role of voltage-gated calcium channels in neurotransmitter phenotype specification: Coexpression and functional analysis in Xenopus laevis. The Journal of Comparative Neurology, 522(11), 2518-2531.

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Pharmacological Modulators of Vascular Function

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The following drugs were used: bradykinin, diltiazem, 5-hydroxytryptamine (5-HT), indomethacin, and nitro-l-arginine (NLA) (Sigma Chemical, St. Louis, MO); iberiotoxin, and 1H-[1,2,4] oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) (Tocris, Ellisville, MO); apelin-13, and F13A (H-Gln-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Ala-OH trifluoroacetate salt) (Bachem, Torrance, CA), A23187 (Abcam, Cambridge, MA) and N-(methylsulfonyl)-2-(2-propynyloxy)-benzenehexanamide (MS-PPOH), 11,12-EET, 14,15-EET and 14,15-EE(Z)E (Cayman Chemicals, Ann Arbor, MI). All solutions were freshly prepared, stored on ice, and protected from light until used. All drugs were dissolved initially in double-distilled water with the exception of MS-PPOH, ODQ, and A23187, which were dissolved initially in DMSO, and indomethacin, which was dissolved initially in 1 mM sodium carbonate solution. Drugs were added to the myograph chambers in volumes not greater than 0.02 ml except 14,15-EE(Z)E, with a volume of 0.16 ml. Final molar concentrations in the myograph chamber are reported for each drug, unless otherwise stated.

Mughal A., Anto S., Sun C, & O’Rourke S.T. (2020). Apelin Inhibits an Endothelium-Derived Hyperpolarizing Factor-Like Pathway in Rat Cerebral Arteries. Peptides, 132, 170350.

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Pharmaceutical Compound Sourcing Protocol

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All chemicals and reagents including nifedipine and diltiazem were purchased from Sigma-Aldrich (St. Louis, MO) with the exception of papain, which was purchased from Worthington Biochemical Corp. (Lakewood, NJ).

Wang F., Koide M, & Wellman G.C. (2017). Nifedipine Inhibition of High-Voltage Activated Calcium Channel Currents in Cerebral Artery Myocytes Is Influenced by Extracellular Divalent Cations. Frontiers in Physiology, 8, 210.

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Calcium Channel Modulation in Neural Development

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Neural tissue was dissected and dissociated in the same manner as calcium-imaged cultures, at the neural plate (st. 14), neural fold (st. 18), and neural tube (st. 22) stages. Cells were plated in MR containing 10 μM or 100 μM diltiazem (Sigma), 1 μM or 10 μM (−)BayK-8644 (Sigma), MR alone, or MR with 0.05% DMSO (BayK-8644 experiments only). The concentrations of diltiazem used in these experiments have previously been demonstrated to decrease calcium currents for VGCC α1 subunits in cell culture (Cai et al., 1997 (link); De Paoli et al., 2002 (link)) and concentrations of (−)BayK 8644 used were shown to increase calcium activity in amphibian explants and cell culture (Moreau et al., 1994 (link); Takano et al., 2011 (link)). Cultures were fixed in 1X MEMFA when intact sibling embryos reached the swimming tadpole stage (35–36), and then stored in ethanol at −20°C.

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Comprehensive CYP Inhibition Profiling

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BBR, phenacetin, coumarin, bupropion, tolbutamide, dextromethorphan, chlorzoxazone, testosterone (TST), ketoconazole, verapamil, diltiazem, mifepristone, carbamazepine (CBZ), potassium ferricyanide (K₃Fe(CN)₆), glucose 6-phosphate (G6P), glucose 6-phosphate dehydrogenase (G6PDH), β-nicotinamide adenine dinucleotide phosphate hydrate (NADP⁺; oxidized form), nebivolol hydrochloride, formic acid were purchased from Sigma-Aldrich (St. Louis, MO, USA). Midazolam (MDZ) was bought from Bukwang Pharmaceutical Co. (Seoul, Korea). S-Mephenytoin was purchased from BD Gentest Co. (Woburn, MA, USA). BRB chloride, JTZ, tetrahydroberberine (THB; canadine), and β-nicotinamide adenine dinucleotide phosphate (NADPH; reduced form) were supplied by Toronto Research Chemicals Inc. (Toronto, ON, Canada). DMB and TFD chloride were purchased from Inter Pharm (Goyang, Korea) and WuXi AppTec Co. (Shanhai, China), respectively. Tetrahydroberberrubine·acetate (TRB; purity > 95%) was isolated from the fruits of Nandina domestica (see Supplementary Materials). Pooled HLM and recombinant human CYP2D6 (rhCYP2D6; product number: 456217) were obtained from Corning Gentest (Corning, NY, USA) and stored at −80 °C before use. All the other chemicals and reagents used were of analytical grade.

Kim H.G., Lee H.S., Jeon J.S., Choi Y.J., Choi Y.J., Yoo S.Y., Kim E.Y., Lee K., Park I., Na M., Park H.J., Cho S.W., Kim J.H., Lee J.Y, & Kim S.K. (2020). Quasi-Irreversible Inhibition of CYP2D6 by Berberine. Pharmaceutics, 12(10), 916.

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Pharmacological Evaluation of Novel Compounds

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The following drugs were used: acetylcholine, diethyl amine (DEA) NONOate, diltiazem, and 5-HT (Sigma Chemical, St. Louis, MO); apelin-13 and F13A trifluoro-acetate salt (Bachem, Torrance, CA); CMPD 101 (Tocris, Ellisville, MO); and CMF 019 (Aobious, Gloucester, MA). Drug solutions were freshly prepared in double-distilled water with the exception of CMF-019 and CMPD 101, which were dissolved initially in DMSO and followed by further dilutions in double-distilled water.

Anto S., Sathish V., Sun C, & O’Rourke S.T. (2022). Apelin-Induced Relaxation of Coronary Arteries is Impaired in a Model of Second-Hand Cigarette Smoke Exposure. Journal of cardiovascular pharmacology, 80(6), 842-851.

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Physiological Salt Solution Preparation

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The physiological salt solution (PSS) contained: 119 mM NaCl, 4.7 mM KCl, 24.0 mM NaHCO₃, 1.2 mM KH₂PO₄, 1.6 mM CaCl₂, 1.2 mM MgSO₄, 0.023 mM EDTA, and 11.0 mM glucose, pH = 7.4. High K⁺ solutions were prepared by equimolar substitution of NaCl with KCl. All chemicals were purchased from Thermo Fisher Scientific (Agawam, MA, United States). ACh, PE, diltiazem and papaverine were obtained from Sigma Chemical Co. (St. Louis, MO, United States). diltiazem was prepared as a 10 mM stock solution in deionized water and kept refrigerated until use (1–2 weeks). papaverine was dissolved in deionized water on the day of the experiment. Stock solution of N^G-nitro-L-arginine, L-NNA in PSS, and ACh and PE in deionized water were prepared on each experimental day.

Gokina N.I., Fairchild R.I., Prakash K., DeLance N.M, & Bonney E.A. (2021). Deficiency in CD4 T Cells Leads to Enhanced Postpartum Internal Carotid Artery Vasoconstriction in Mice: The Role of Nitric Oxide. Frontiers in Physiology, 12, 686429.

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Metabolic Drug Interaction Profiling

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Crizotinib, diltiazem, erythromycin, imatinib, nilotinib, pazopanib, roxithromycin, and verapamil were obtained from Sigma-Aldrich (St. Louis, MO). Nefazodone and azithromycin were purchased from Toronto Research Chemicals (Toronto, ON) and telithromycin from Cayman Chemical Company (Ann Arbor, MI). Midazolam was obtained from Cerilliant Corporation (Round Rock, TX), 1′-hydroxyMidazolam from Ultrafine Chemical Co. (Manchester, England) and nicotinamide adenine dinucleotide phosphate (NADPH) from AppliChem (Darmstadt, Germany). HLM from 50 individual mixed-sex donors were purchased from Xenotech (Lenexa, KS). Human hepatocytes were isolated in house from liver tissue obtained from a female donor undergoing surgical resection at the Department of Surgery, Uppsala University Hospital (Sweden) and cryopreserved as described previously^{34 (link),35 (link)}. Ethical approval was granted by the Uppsala Regional Ethics Committee (ethical Approvals Nos 2009/028 and 2011/037). Donors gave informed consent and all studies were performed in accordance with the current national regulations and ethical guidelines.

Filppula A.M., Parvizi R., Mateus A., Baranczewski P, & Artursson P. (2019). Improved predictions of time-dependent drug-drug interactions by determination of cytosolic drug concentrations. Scientific Reports, 9, 5850.

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Manganese-Enhanced MRI of NSCs in TBI

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As mentioned above, approximately 1 month after transplantation of NSCs into the TBI rat brains, SPIOs-labeled NSCs could migrate to the injured brain areas. Then, manganese-enhanced MRI (ME-MRI) scan was performed to detect the function of these NSCs^{16 (link)}.
In brief, 1% MnCl₂ (Sigma-Aldrich) was first intravenously infused into group A TBI rats within 1 h. At approximately the halfway stage of MnCl₂ infusion, blood–brain barrier (BBB) of the right-side cerebral hemisphere (the injury site) was opened by 20% mannitol. Then, left (contralateral) forepaw electrical stimulation was conducted for 30 min, and the ME-MRI scan was then performed. In group B TBI rats, the same procedures were performed, but the Ca²⁺ channel inhibitor diltiazem (Sigma-Aldrich) was infused 10 min before electrical stimulation and was continued during the entire stimulus period.
Next, ME-MRI scan was performed using a clinical 3 T MRI scanner (Siemens) with an animal coil and the three-dimensional spoiled gradient recalled acquisition in a steady state (3D-SPGR) pulse sequence was used. The scan was performed using the following parameters: TE = 2.4 ms; TR = 8.8 ms; FOV = 5 cm × 4 cm; flip angle = 45°; repetition = 6 NEX.

Jiang L., Li R., Tang H., Zhong J., Sun H., Tang W., Wang H, & Zhu J. (2018). MRI Tracking of iPS Cells-Induced Neural Stem Cells in Traumatic Brain Injury Rats. Cell Transplantation, 28(6), 747-755.

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