All chemicals were used as received from the supplier. Diphenhydramine hydrochloride (20 mg kg−1 or 50 mg kg−1 Sigma Aldrich, St. Louis, MO, USA), zolantidine dimaleate (10 mg kg−1; Tocris, Minneapolis, MN, USA), immepip dihydrobromide (5 mg kg−1; Sigma Aldrich, St. Louis, MO, USA), thioperamide maleate (20 mg kg−1; Sigma Aldrich and Tocris), tacrine hydrochloride (2 mg kg−1; Tocris), and α-fluoromethylhistidine (20 mg kg−1; Toronto Research Chemicals, North York, ON, CAN) were all dissolved in sterile saline (0.9% NaCl solution, Mountainside Medical Equipment, NY, USA) at 5 mL kg−1. Reserpine (10 mg kg−1; Sigma Aldrich, St. Louis, MO, USA) was dissolved in 0.1% acetic acid (Sigma Aldrich, St. Louis, MO, USA) in sterile saline at 5 mL kg−1. Tetrabenazine (Sigma Aldrich) was dissolved in 10% DMSO (Sigma Aldrich, St. Louis, MO, USA) in sterile saline with 1 M HCl (10 µL mL−1 injection volume). All solutions were made fresh at the time of injection and all injections were given via intraperitoneal (i.p.) injection. Urethane (Sigma Aldrich, St. Louis, MO, USA) was dissolved in sterile saline as a 25% w/v solution and administered at 7 µL g−1.
Thioperamide maleate
Manufactured by Merck Group
Sourced in United States
Thioperamide maleate is a laboratory chemical produced by Merck Group. It is a white, crystalline powder. The chemical formula is C13H17N3OS·C4H4O4. Thioperamide maleate is used in various research and analytical applications.
Automatically generated - may contain errors
Lab products found in correlation
Dimethyl sulfoxide (dmso), by Merck Group (3 mentions)
Urethane, by Merck Group (3 mentions)
Zolantidine dimaleate, by Bio-Techne (3 mentions)
Immepip dihydrobromide, by Merck Group (3 mentions)
Tacrine hydrochloride, by Bio-Techne (3 mentions)
Diphenhydramine hydrochloride, by Merck Group (3 mentions)
Reserpine, by Merck Group (3 mentions)
Tetrabenazine, by Merck Group (3 mentions)
α fluoromethylhistidine, by LGC (3 mentions)
Acetic acid, by Merck Group (1 mentions)
Hepes, by Merck Group (1 mentions)
Ip one tb assay kit, by PerkinElmer (1 mentions)
Histamine hydrochloride, by Merck Group (1 mentions)
Histamine dihydrochloride, by Merck Group (1 mentions)
Indomethacin, by Merck Group (1 mentions)
R α methylhistamine dihydrochloride, by Merck Group (1 mentions)
Pyrilamine maleate, by Merck Group (1 mentions)
Clobenpropit, by Bio-Techne (1 mentions)
6 protocols using thioperamide maleate
1
Pharmacological Agents Preparation and Administration
2
Histamine H3 Receptor Characterization
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Buffers and media for cell culturing were all purchased from Invitrogen (Paisley, United Kingdom) whereas non-enzymatic dissociation solution, HEPES (4-(2-hydroxyethyl)piperazine-1-ethanesulfonic acid) and additional assay buffer supplements were from Sigma-Aldrich (St. Louis, MO, USA). The IP-One Tb assay kit was purchased from Cisbio (Codolet, France). The human histamine H3 DNA (Genbank accession no. AF321910.1) in a pSI expression vector was identical to a previously used one58 (link). The G protein Gqi5 was a kind gift from Dr. Evi Kostenis, University of Bonn, Germany. Histamine hydrochloride and thioperamide maleate were obtained from Sigma-Aldrich and Abcam Biochemicals (Cambridge, UK), respectively.
3
Acquisition of Pharmacological Compounds
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Thioperamide maleate, (R)-α-methylhistamine dihydrochloride, indomethacin, pyrilamine maleate, and histamine dihydrochloride were purchased from Sigma Aldrich (Saint Louis, MO, USA).
4
Radiosynthesis of Dihydroquinolinone Derivatives
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Dihydroquinolinone derivatives (Fig. 1 ), 1-(4-methoxyphenyl)-6-{3-[(2R)-2-methylpyrrolidin-1-yl]propoxy}-3,4-dihydroquinolin-2(1H)-one (TASP0390136), 6-[(1-Cyclobutylpiperidin-4-yl)oxy]-1-(6-methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one (TASP0410457), 6-[(1-cyclobutylpiperidin-4-yl)oxy]-1-(4-methoxyphenyl)-3,4-dihydroquinolin-2(1H)-one (TASP0434988), 1-(3-methoxyphenyl)-6-{3-[(2R)-2-methylpyrrolidin-1-yl]propoxy}-3,4-dihydroquinolin-2(1H)-one (TASP0390174), 1-(3-fluoro-5-methoxyphenyl)-6-{3-[(2R)-2-methylpyrrolidin-1-yl]propoxy}-3,4-dihydroquinolin-2(1H)-one (TASP0410426), and 1-(2,4-dimethoxyphenyl)-6-{3-[(2R)-2-methylpyrrolidin-1-yl]propoxy}-3,4-dihydroquinolin-2(1H)-one (TASP0410427) were synthesized at Taisho Research Laboratories (Saitama, Japan). Procedures for synthesizing TASP0390136, TASP0410457, and TASP0434988 and precursors for 11C-labeling of these compounds are provided in Additional file 1 : Supplemental methods. Thioperamide maleate and ciproxifan hydrochloride were purchased from Sigma-Aldrich (St. Louis, MO). Clobenpropit was purchased from Tocris Bioscience (Bristol, UK).![]()
Radiosynthesis of [11C]TASP0390136, [11C]TASP0410457, and [11C]TASP0434988, and chemical structure of TASP0390174, TASP0410426, and TASP0410427
5
Pharmacological Manipulation of Histaminergic Signaling
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All chemicals were used as received from the supplier. Diphenhydramine hydrochloride (20 mg kg -1 ; Sigma Aldrich, St. Louis, MO, USA), zolantidine dimaleate (10 mg kg -1 ; Tocris, Minneapolis, MN, USA), immepip dihydrobromide (5 mg kg -1 ; Sigma Aldrich), thioperamide maleate (20 mg kg -1 or 50 mg kg -1 Sigma Aldrich and Tocris), tacrine hydrochloride (2 mg kg -1 ; Tocris), and α-fluoromethylhistidine (20 mg kg -1 ; Toronto Research Chemicals, North York, ON, CAN) were all dissolved in sterile saline (0.9% NaCl solution, Mountainside Medical Equipment, NY, USA) at 5 mL kg -1 . Reserpine (10 mg kg -1 ; Sigma Aldrich) was dissolved in 0.1 % acetic acid (Sigma Aldrich) in sterile saline at 5 mL kg -1 . Tetrabenazine (Sigma Aldrich) was dissolved in 10 % DMSO (Sigma Aldrich) in saline with 1 M HCl (10 µL mL -1 injection volume). All solutions were made fresh at the time of injection and all injections were given via intraperitoneal (i.p.) injection. Urethane (Sigma Aldrich) was dissolved in sterile saline as a 25 % w/v solution and administered at 7 µL kg -1 .
6
Pharmacological Manipulation of Histaminergic Signaling
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All chemicals were used as received from the supplier. Diphenhydramine hydrochloride (20 mg kg -1 ; Sigma Aldrich, St. Louis, MO, USA), zolantidine dimaleate (10 mg kg -1 ; Tocris, Minneapolis, MN, USA), immepip dihydrobromide (5 mg kg -1 ; Sigma Aldrich), thioperamide maleate (20 mg kg -1 or 50 mg kg -1 Sigma Aldrich and Tocris), tacrine hydrochloride (2 mg kg -1 ; Tocris), and α-fluoromethylhistidine (20 mg kg -1 ; Toronto Research Chemicals, North York, ON, CAN) were all dissolved in sterile saline (0.9% NaCl solution, Mountainside Medical Equipment, NY, USA) at 5 mL kg -1 . Reserpine (10 mg kg -1 ; Sigma Aldrich) was dissolved in 0.1 % acetic acid (Sigma Aldrich) in sterile saline at 5 mL kg -1 . Tetrabenazine (Sigma Aldrich) was dissolved in 10 % DMSO (Sigma Aldrich) in saline with 1 M HCl (10 µL mL -1 injection volume). All solutions were made fresh at the time of injection and all injections were given via intraperitoneal (i.p.) injection. Urethane (Sigma Aldrich) was dissolved in sterile saline as a 25 % w/v solution and administered at 7 µL kg -1 .
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