Sb242084

Manufactured by Merck Group

Sourced in United States

SB242084 is a laboratory equipment product manufactured by Merck Group. It is designed for use in research and scientific applications. The core function of SB242084 is to provide a reliable and precise tool for researchers and scientists to conduct their experiments and analyses.

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Lab products found in correlation

9 protocols using sb242084

Social Approach in Mice with 5-HT2c Antagonist

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20 minutes prior to testing, mice tested for social approach with 5-HT_2cR antagonist were given an intraperitoneal injection of SB 242084 (Sigma-Aldrich) diluted to 0.3mg/ml in a 10% (2-hydroxypropyl)-β-cyclodextrin (Sigma-Aldrich) in sterile 25mM citric acid vehicle, or equivalent volume vehicle. For all injections, care was taken to handle animals gently to minimize stress.

Séjourné J., Llaneza D., Kuti O.J, & Page D.T. (2015). Social Behavioral Deficits Coincide with the Onset of Seizure Susceptibility in Mice Lacking Serotonin Receptor 2c. PLoS ONE, 10(8), e0136494.

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Pharmaceutical Compound Preparation and Administration

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WAY163909 [(7b-R,10a-R)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta[b][1,4]diazepino[6,7,1hi]indole] was a gift from Pfizer, Inc. (New York, NY) and dissolved in 0.9% NaCl (vehicle employed for comparison to WAY163909). SB242084 [6-chloro-5-methyl-1-[[2-(2-methylpyrid-3-yloxy)pyrid-5-yl]carbamoyl]indoline dihydrochloride; Sigma Chemical Co., St. Louis, MO, USA] was dissolved in saline containing 10 mmol/L citric acid (Sigma Chemical Co.) and 8% 2-hydroxypropyl-β-cyclodextrin (Trappsol Hydroxpropyl Beta Cyclodextrin, pharmaceutical grade, Cyclodextrin Technologies Development Inc., High Springs, FL, USA) with the final pH of the solution adjusted to 5.6. SB242084, WAY163909, and compound 16 were injected intraperitoneally (ip) at a volume of 1 mL/kg.

Wild C.T., Miszkiel J.M., Wold E.A., Soto C.A., Ding C., Hartley R.M., White M.A., Anastasio N.C., Cunningham K.A, & Zhou J. (2018). Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT2C Receptor. Journal of medicinal chemistry, 62(1), 288-305.

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Pharmacological Evaluation of WAY163909

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WAY163909 [(7b-R,10a-R)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta[b][1,4] diazepino[6,7,1hi]indole] was a gift from Pfizer, Inc. (New York, NY) and was dissolved in 0.9% NaCl (vehicle employed for comparison to WAY163909). SB242084 [6-chloro-5-methyl-1-[[2-(2-methylpyrid-3-yloxy)pyrid-5-yl]carbamoyl]indoline dihydrochloride; Sigma Chemical Co., St. Louis, MO, USA] was dissolved in saline containing 10 mmol/L citric acid (Sigma Chemical Co.) and 8% 2-hydroxypropyl-β-cyclodextrin (Trappsol hydroxpropyl β cyclodextrin, pharmaceutical grade, Cyclodextrin Technologies Development Inc., High Springs, FL, USA) with the final pH of the solution adjusted to 5.6. SB242084, WAY163909, and compound 12 were injected ip at a volume of 1 mL/kg.

Wold E.A., Garcia E.J., Wild C.T., Miszkiel J.M., Soto C.A., Chen J., Pazdrak K., Fox R.G., Anastasio N.C., Cunningham K.A, & Zhou J. (2020). Discovery of 4-Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5-HT2C Receptor-Positive Allosteric Modulators with Enhanced Drug-like Properties. Journal of medicinal chemistry, 63(14), 7529-7544.

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Pharmacological Modulation of Neuronal Receptors

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1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane HCl (DOI), N-Methyl-D-aspartic acid (NMDA), (S)-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and (2-hydroxyethyl)trimethylammonium chloride carbamate (carbachol) (Sigma-Aldrich, St. Louis, MO) and 2-aminoethyl disulfide dihydrochloride (cystamine) (MP Biomedicals, Solon, OH) were dissolved in saline or water and further diluted before application to cell cultures. SB 242084 (Sigma-Aldrich, St. Louis, MO) was dissolved in ethanol (the final concentration of ethanol exposure to cells was 0.1%). MDL100907 was kindly provided by Sanofi Aventis (Bridgewater, NJ) and dissolved in DMSO (the final concentration of DMSO exposure to cells was 0.01%).

Mi Z., Si T., Kapadia K., Li Q, & Muma N.A. (2017). Receptor-stimulated Transamidation Induces Activation of Rac1 and Cdc42 and the Regulation of Dendritic Spines. Neuropharmacology, 117, 93-105.

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Pharmacological Manipulation of Serotonin Signaling

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MDL 100907, TCB-2, and 25CN-NBOH were purchased from Tocris (Bristol, UK), escitalopram oxalate was purchased from Shodana Labs (Hyderabad, India), pimavanserin was purchased from MedChem Express (Monmouth Junction, NJ, USA), psilocybin was purchased from Chiron Corporation (Emeryville, CA, USA), and SB 242084 was purchased from Sigma-Aldrich (St. Louis, MO, USA). Escitalopram and 25CN-NBOH were dissolved in 0.9% saline. SB 242084 was dissolved in 0.9% saline, 8% cyclodextrin, and 0.48% citric acid. All other drugs were dissolved in 0.9% saline by adding a small volume of 1 M HCl while the solution was heated and stirred. When required, pH was readjusted by adding NaOH. Controls received 0.9% saline. All injections were given subcutaneously with an injection volume of approximately 1 mL. For time points of injections, see Figure 1.

Hagsäter S.M., Pettersson R., Pettersson C., Atanasovski D., Näslund J, & Eriksson E. (2021). A Complex Impact of Systemically Administered 5-HT2A Receptor Ligands on Conditioned Fear. International Journal of Neuropsychopharmacology, 24(9), 749-757.

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Pharmacological Modulation of 5-HT Receptors

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The injectable anesthetic (+/−)-ketamine and the mixed 5-HT_2A/2C receptor agonist (+/−)2,5-Dimethoxy-4-iodoamphetamine (DOI) (Fantegrossi et al., 2008 (link)) were purchased from Sigma-Aldrich (St. Louis, MO) and dissolved in saline. The selective 5-HT_2C receptor antagonist, SB-242084 (Kennett et al., 1997 (link)), was purchased from SigmaAldrich (St. Louis, MO) and dissolved in 5% Tween 80, 5% ethanol, and brought to final volume in saline. The selective 5-HT_2C receptor agonist, WAY-163909 (Grauer et al., 2009 (link); Marquis et al., 2007 (link)), was provided as a gift from Pfizer (New York, NY) and dissolved in 5% Tween 80 and brought to final volume in saline. All injections were administered intraperitoneally at a volume of 0.01 ml of the drug solution per g body weight of each mouse. All doses are reported in the salt form.

Murphy T.J, & Murnane K.S. (2018). The serotonin 2C receptor agonist WAY-163909 attenuates ketamine-induced hypothermia in mice. European journal of pharmacology, 842, 255-261.

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Serotonin and Dopamine Modulation in Behavioral Testing

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SB242084 (Sigma-Aldrich, Atlanta, GA), a 5-HT2C antagonist, was suspended in a vehicle of 0.5% DMSO in saline in the doses of 0.3, 1, and 3 mg/kg (Yoshimoto et al., 2012 (link)). Buspirone (Sigma-Aldrich), a 5-HT1A partial agonist and dopamine D2, D3, D4 antagonist, was dissolved in saline in the doses of 1, 3, and 10 mg/kg (Martin et al., 1992 (link); Rodgers et al., 1997 (link)). Drugs were administered intraperitoneally in a volume of 10 ml/kg 20 min before either testing for two-bottle choice consumption or locomotor activity in the open field.

Ko Y.E, & Hwa L.S. (2023). Serotonin regulation of intermittent and continuous alcohol drinking in male and female C57BL/6J mice with systemic SB242084 and buspirone. Alcohol and Alcoholism (Oxford, Oxfordshire), 58(3), 280-288.

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Pharmacological Modulation of MDMA Effects

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MDMA (5 mg/kg), Ketanserin (5 mg/kg), SB242084 (3 mg/kg), Pindolol (0.3 mg/kg) and RU486 (7.5 mg, approximately 30 mg/kg) were purchased from Sigma-Aldrich Co. (Sigma-Aldrich, Israel). All drugs were dissolved in saline (0.9% NaCl) and injected intraperitoneally (i.p.) in a 250 µl volume. Based on the literature [32 (link)–34 (link)] and in considering our preliminary study which didn’t find any significantly differences between saline and MDMA 3 mg/kg in LMA and because of the possibility of neurotoxicity produced by higher dose of 10 mg/kg [35 (link)], the 5 mg/kg dose was chosen for this study. The doses of Ketanserin and SB242084 were selected based on Shinoda’s report [36 (link)]. The dose of Pindolol was selected based on Nash’s report [22 (link)]. The dose of RU486 was selected based on our previous study [37 (link)]. All pre-treatments were administered i.p. 60 min prior to MDMA injection.

Arluk S., Matar M.A., Carmi L., Arbel O., Zohar J., Todder D, & Cohen H. (2022). MDMA treatment paired with a trauma-cue promotes adaptive stress responses in a translational model of PTSD in rats. Translational Psychiatry, 12, 181.

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Ferroptosis Inducers and Inhibitors Protocol

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Erastin (S7242), RSL3 (S8155), ferrostatin-1 (S7243), liproxstatin-1 (S7699), Z-VAD-FMK (S7023), necrosulfonamide (S8251), staurosporine (S1421), CCT137690 (S2744), olanzapine (S2493), idebenone (S2605), telmisartan (S1738), nisoldipine (S1748), azelnidipine (S3053), and risperidone (S1615) were obtained from Selleck Chemicals (Houston, TX). Cerulein (C9026), L-arginine (A5006), alcohol (PHR1373), 2-mercaptoethanol (M6250), trypsin (T1426), soybean trypsin inhibitor (650357), SB204741 (S0693), and SB242084 (5.06417) were obtained from Sigma-Aldrich (Burlington, MA). Dimethyl sulfoxide (472301; Sigma-Aldrich) was used to prepare the stock solution of most drugs. The final concentration of Dimethyl sulfoxide in the drug working solution in the cells was less than 0.01%. In addition, 0.01% Dimethyl sulfoxide was used as a vehicle control in the corresponding cell culture assays.
The antibodies to PSMD4 (sc-398033) and actin beta (ACTB, sc-8432) were obtained from Santa Cruz Biotechnology (Dallas, TX). The antibodies to GPX4 (ab125066) and SLC7A11 (ab175186) were obtained from Abcam (Cambridge, MA). The antibodies to ferritin heavy chain 1 (3998) and ARNTL (14020) were obtained from Abcam. The antibodies to SLC40A1 (NBP1-21502) and apoptosis inducing factor mitochondria-associated 2 (H00084883-D01P) were obtained from NOVUS (Saint Charles, MO).

Liu K., Liu J., Zou B., Li C., Zeh H.J., Kang R., Kroemer G., Huang J, & Tang D. (2021). Trypsin-Mediated Sensitization to Ferroptosis Increases the Severity of Pancreatitis in Mice. Cellular and Molecular Gastroenterology and Hepatology, 13(2), 483-500.

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