Ketanserin tartrate

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Sourced in United States, United Kingdom

Ketanserin tartrate is a laboratory chemical compound used in research applications. It functions as a selective antagonist of the 5-HT2 receptor. This product is intended for use in controlled laboratory settings by qualified researchers.

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Ketanserin (14 citations)

11 protocols using ketanserin tartrate

Serotonin Receptor Modulation in Neurons

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Glycine (30 µM), 5-HT (10 µM), and the chemical substances for ACSF were bought from Sigma (St. Louis, MO, USA). SB-269970 (10 µM), 8-OH-DPAT (30 µM), WAY-100635 (1 µM), ketanserin tartrate (30 µM), and α-methyl-5-HT maleate (30 µM) were bought from Tocris Bioscience (Ellisville, MO, USA).
Stocks of all chemicals were made according to their solubility in distilled water, except SB-269970 and ketanserin tartrate, which were prepared in dimethyl sulfoxide. Stock solutions were diluted to desired final concentrations in ACSF immediately before cell treatment. Chemicals were applied to the neurons via bath application.

Nguyen H.T., Cho D.H., Jang S.H., Han S.K, & Park S.J. (2019). Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice. The Korean Journal of Physiology & Pharmacology : Official Journal of the Korean Physiological Society and the Korean Society of Pharmacology, 23(4), 271-279.

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Serotonin Receptor Pharmacology Assay

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Cyclohexylamine was purchased from Wako, Japan. Ketanserin tartrate and methysergide male-ate were purchased from Tocris, USA. Serotonin and propranolol were bought from Sigma-Aldrich, USA. All drugs were dissolved in millipore water. The composition of Kreb's solution is expressed as follows (mM/L): NaCl 119; NaHCO₃ 24.9; D-Glucose 11; KH₂PO₄ 1.2; KCl 4.6; MgSO₄ · 7H₂O 1.2; CaCl₂ · 2H₂O 1.5.

Chen Y.F., Wang Y.W., Chen I.S, & Tsai H.Y. (2020). Cyclohexylamine, an active compound from Toddalia asiatica, contracts epididymal vas deferens via serotonergic receptors. BioMedicine, 10(2), 12-22.

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Lipid Signaling Pathway Reagents

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Unless otherwise specified, all reagents were purchased from Fisher Scientific. Polyethyleneimine (Polysciences Inc., Cat# 24765), ritanserin ≥99% by HPLC (Tocris Bioscience, Cat# 1955), ketanserin tartrate ≥97% by HPLC (Tocris Bioscience, Cat# 0908), 1-stearoyl-2-arachidonoyl-d8-sn-glycerol (SAG-d8; Cayman Chemical Company, Cat# 10009872), and arachidonic acid-d8 (AA-d8; Cayman Chemical Company, Cat# 390010).

Ware T.B., Franks C.E., Granade M.E., Zhang M., Kim K.B., Park K.S., Gahlmann A., Harris T.E, & Hsu K.L. (2020). Reprogramming fatty acyl specificity of lipid kinases via C1 domain engineering. Nature chemical biology, 16(2), 170-178.

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Electrophysiology Experiment Reagents

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Alpha-methyl-5-hydroxytryptamine (α-m5HT) maleate, ketanserin tartrate, and bicuculline methiodide were purchased from Tocris Cookson (Ellisville, MO, USA). Ethanol (95%) was purchased from Warner–Graham Company (Cockeysville, MD, USA). Sucrose and salts used in the electrophysiology experiments were all purchased from Sigma–Aldrich (St. Louis, MO, USA).

McCool B.A., Christian D.T., Fetzer J.A, & Chappell A.M. (2014). Lateral/basolateral amygdala serotonin type-2 receptors modulate operant self-administration of a sweetened ethanol solution via inhibition of principal neuron activity. Frontiers in Integrative Neuroscience, 8, 5.

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Pharmacological Modulation of Serotonin Receptors

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5-HT hydrochloride, α-Me-5-HT maleate, ketanserin tartrate, and tetrodotoxin were purchased from Tocris (Bristol, UK). Naftopidil was synthesized at the Asahi Kasei Pharma Corporation (Tokyo, Japan). Prazosin hydrochloride was obtained from Sigma-Aldrich (St-Quentin-Fallavier, France). Stock solutions of naftopidil and ketanserin were prepared on each day of experimentation at a concentration of 0.01M in DMSO. Further dilution was carried out using a mixture of distilled water and DMSO.

Hattori T., Lluel P., Rouget C., Rekik M, & Yoshiyama M. (2017). Ketanserin and Naftopidil Enhance the Potentiating Effect of Alpha-Methyl-Serotonin on the Neurally-Induced Contraction of Human Isolated Urinary Bladder Muscle Strips. International Neurourology Journal, 21(1), 20-28.

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Pharmacological Effects of MDMA and M100907

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Racemic MDMA [(±)-3,4-methylenedioxymethamphetamine hydrochloride] and M100907 were kindly provided by the National Institute of Drug Abuse (Baltimore, MD, USA). Ketanserin tartrate and methyllycaconitine citrate were purchased from TOCRIS (Ellisville, MO, USA). Hexamethonium bromide, midazolam hydrochloride, and WAY100,635 maleate were purchased from Sigma (St. Louis, MO, USA). Drug dosages (mg/kg) were expressed as the weight of the salt and injected at a constant volume of 1 mL/kg (dissolved in 0.9% NaCl). MDMA and ketanserin were injected intraperitoneally, and other drugs were administered subcutaneously.

Tao R., Shokry I.M., Callanan J.J., Adams H.D, & Ma Z. (2014). Mechanisms and environmental factors that underlying the intensification of 3,4-methylenedioxymethamphetamine (MDMA, Ecstasy)-induced serotonin syndrome in rats. Psychopharmacology, 232(7), 1245-1260.

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Investigating MDMA-Induced Sensory Gating Deficits

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All drugs were diluted and prepared to an injection volume of 1 mL/kg on the day of the testing session. Drug doses used were in accordance with previous literature. A 2 mg/kg dose of MDMA ((±) 3,4 methylene-dioxymethamphetamine hydrochloride, Sigma Aldrich, St. Louis, MO, USA) was injected intraperitoneally. This was previously shown to elicit a paired-pulse sensory gating deficit [25 (link)]. Pretreatment drugs, haloperidol (Serenace®, Aspen Pharma Pty Ltd, St Leonards, NSW, Australia) 0.25 mg/kg, SCH23390 (Tocris Bioscience, Bristol, UK) 0.1 mg/kg, ketanserin tartrate (Tocris Bioscience, Bristol, UK) 2 mg/kg and WAY100635 maleate (Tocris Bioscience, Bristol, UK) 1 mg/kg, were all injected subcutaneously. The doses of these drugs were chosen on the basis of literature and preliminary experiments. Saline was injected subcutaneously for pretreatment control, but intraperitoneally for the treatment control injection. The pretreatment drug (saline or antagonist) was administered 30 min prior to the treatment drug (saline or MDMA). Recordings began 10 min after the treatment injection to allow time for the drug to take its effects and for the rat to settle into the chamber.

Lee J., Thwaites S., Gogos A, & van den Buuse M. (2020). Pharmacological Mechanisms Involved in Sensory Gating Disruption Induced by (±)-3,4-Methylene- Dioxymethamphetamine (MDMA): Relevance to Schizophrenia. Brain Sciences, 10(1), 44.

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Quantifying D1R Binding Sites

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D1R binding sites were labeled with [³H]SCH23390 using the procedure described by Savasta with minor modifications (Savasta et al. 1986). After removing endogenous dopamine, sections were incubated for 30 min at 20°C in buffer solution containing 1.5 nmol/L [³H]SCH23390 and 30 nM ketanserin tartrate (Tocris Bioscience, Ellisville, Missouri, USA, Cat. #0908, CAS. #83846‐83‐7) to block 5‐HT₂ receptors. Non‐specific binding was determined in the presence of 1 µM (+)‐butaclamol (Sigma‐Aldrich, Cat. #D033‐5MG, CAS. #55528‐07‐9) as previously described (Novick et al. 2008; Lim et al. 2011).

Li H., Yang P., Knight W., Guo Y., Perlmutter J.S., Benzinger T.L., Morris J.C, & Xu J. (2019). The interactions of dopamine and oxidative damage in the striatum of patients with neurodegenerative diseases. Journal of Neurochemistry, 152(2), 235-251.

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Synthesis and Characterization of 5-MeO-Tryptamines

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5-MeO-tryptamines were synthesized as hydrochloride salts (Supplementary Fig. 1), identified and characterized as described in the Supplementary Material. WAY100635 maleate and ketanserin tartrate were obtained from Tocris (Bio-Techne R&D Systems, S.L.U., Madrid, Spain). Solutions for injection were freshly prepared daily in isotonic saline solution (0.9% NaCl, pH 7.4). The radioligands [ 3 H]5-HT (33.2 Ci/mmol), [ 3 H]ketanserin (22.8 Ci/ mmol), [ 3 H]8-OH-DPAT (200 Ci/mmol), [ 3 H]imipramine (40 Ci/mmol) and the membrane preparations expressing human 5-HT1A and 5-HT2A receptors (h5-HT1AR and h5-HT2AR) were purchased from Perkin Elmer, Inc. (Waltham, MA, USA). p-Chloroamphetamine (pCA) and paroxetine were purchased from Sigma Aldrich. All other reagents were of analytical grade and purchased from several commercial sources. See the Supplementary Material for buffers and solutions composition.

Puigseslloses P., Nadal-Gratacós N., Ketsela G., Weiss N., Berzosa X., Estrada-Tejedor R., Islam M.N., Holy M., Niello M., Pubill D., Camarasa J., Escubedo E., Sitte H.H, & López-Arnau R. (2024). Structure-activity relationships of serotonergic 5-MeO-DMT derivatives: insights into psychoactive and thermoregulatory properties. Molecular psychiatry.

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Lipid Signaling Pathway Reagents

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