Buspirone hydrochloride

Manufactured by Merck Group

Sourced in United States, United Kingdom

Buspirone hydrochloride is a pharmaceutical compound used as a laboratory reagent. It is a white, crystalline powder that is soluble in water. Buspirone hydrochloride is commonly used in research and development applications, but its specific core function is not included in this factual and unbiased description.

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Buspirone (21 citations) Hydrochlorides (2 citations)

19 protocols using buspirone hydrochloride

Anxiolytic Effects of Buspirone and MTEP

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Treatments were administered systemically via intraperitoneal injection, 30 min prior to the onset of behavioral testing. Ten animals from each drinking group received a 5 mg/kg injection of buspirone hydrochloride (Sigma-Aldrich, Atlanta, GA) in sterile water. This buspirone dose was selected for study as it elicits anxiolytic effects in other drug-related behavioral paradigms (Ettenberg & Bernardi, 2006 (link); Nishimura et al., 1993 ; Risbrough et al., 2003 (link)). An additional 10 animals from each drinking group received a 3 mg/kg injection of the mGlu5 antagonist MTEP in sterile water. This MTEP dose was selected for study based on evidence of anxiolytic efficacy in rodents (Klodzinska et al., 2004 (link); Pietraszek et al., 2005 (link); Stachowicz et al., 2007 (link)). The remaining animals served as vehicle controls and received injections of sterile water (vol=0.01 ml/g).

Lee K.M., Coelho M.A., Sern K.R., Class M.A., Bocz M.D, & Szumlinski K.K. (2017). Anxiolytic Effects of Buspirone and MTEP in the Porsolt Forced Swim Test. Chronic Stress, 1, 2470547017712985.

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Pharmacological Interventions in Animal Study

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R(+)-baclofen hydrochloride (Sigma-Aldrich, St. Louis, MO, USA) was injected intraperitoneally (i.p.) 30 min before testing. CGP44532 was kindly donated by Novartis Pharma AG, and was injected subcutaneously (s.c.), 15 min before testing. Buspirone hydrochloride (Sigma-Aldrich) was injected s.c., 10 min before testing. All of the above compounds were dissolved in sterile 0.9% saline and injected in a volume of 1 ml/kg. BHF177 was synthesized as described previously (Li et al., 2013 (link)). BHF177 was suspended in 0.5% methylcellulose and administered orally (p.o.) in a volume of 2 ml/kg, 1 hr before testing. Rats were fasted for approximately 12 to 16 hrs before p.o. administration of BHF177. The doses of baclofen (0.4, 0.9 and 1.25 mg/kg) were chosen based on previously published studies (Cryan et al., 2004 (link); Frankowska et al., 2007 (link)). The doses of CGP44532 (0.065, 0.125 and 0.25 mg/kg) and BHF177 (10, 20, and 40 mg/kg) were chosen based on previous studies in our laboratory and others (Maccioni et al., 2009 (link); Paterson et al., 2008 (link); Vlachou et al., 2011a (link); Vlachou et al., 2011b (link)). The doses of buspirone (1 and 3 mg/kg) were chosen based on previous publications (Brodkin et al., 2002 (link); Commissaris et al., 2004 (link)).

Li X., Kaczanowska K., Finn M.G., Markou A, & Risbrough V.B. (2015). The GABAB receptor positive modulator BHF177 attenuated anxiety, but not conditioned fear, in rats. Neuropharmacology, 97, 357-364.

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Pharmacological Interventions in Neuroscience

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Desipramine hydrochloride, pargyline, l‐DOPA, benserazide hydrochloride and buspirone hydrochloride were obtained from Sigma‐Aldrich, while WAY‐100635 maleate and 8‐OH‐DPAT were obtained from Tocris‐Biogen. These drugs were prepared in 0.9% saline. Urethane and 6‐OHDA hydrobromide (Sigma‐Aldrich) were dissolved in Milli‐Q water and Milli‐Q water containing 0.02% ascorbic acid, respectively. All drug solutions were prepared on the day of the experiment.

Vegas‐Suárez S., Aristieta A., Requejo C., Bengoetxea H., Lafuente J.V., Miguelez C, & Ugedo L. (2021). The effect of 5‐HT1A receptor agonists on the entopeduncular nucleus is modified in 6‐hydroxydopamine‐lesioned rats. British Journal of Pharmacology, 178(12), 2516-2532.

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Zebrafish Larval Light-Dark Preference Test

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Embryo and larval exposures proceeded as per Section 2.6. Zebrafish larvae (at 7 dpf) were transferred into a 12-well plate with ERM. Twenty trials were conducted with n = 13–36 fish per treatment for the light/dark preference test (LDPT). A company-manufactured cover was placed over the plate to create light and dark zones in each well. Poorly tracked larvae were excluded from analysis and data from twenty distinct runs were blended into a single graph to reflect all runs. Buspirone hydrochloride at 60 µM (CAS number: 33386-08-2, Sigma-Aldrich, St. Louis, MO, USA) was used as a positive control in this assay since it is an anxiolytic compound that has been validated in the LDPT with zebrafish larvae [27 (link)]. The assay methodology is described in detail in our previous publication [5 (link)].

Iftikhar N., Konig I., English C., Ivantsova E., Souders CL I.I., Hashmi I, & Martyniuk C.J. (2023). Sulfamethoxazole (SMX) Alters Immune and Apoptotic Endpoints in Developing Zebrafish (Danio rerio). Toxics, 11(2), 178.

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Electrochemical Biosensing with AuNHA

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Carbon screen-printed electrodes (CSPE), DRP-110, used for EC sensing purposes, were bought from DropSens (Llanera, Asturias, Spain). EC measurements were conducted by an AUTOLAB PGSTAT204 (Metrohm AG, Herisau, Switzerland) compact and modular potentiostat/galvanostat. Gold nanohole arrays (AuNHA) were fabricated in-house as described elsewhere [28 (link)]. Optical measurements were performed with an inverted microscope (Nikon Eclipse-Ti, Tokio, Japan) and a CCD spectrometer (Andor Shamrock 303i, Andor Technology Ldt., Belfast, UK).
All chemicals used throughout the study; phosphate-buffered saline (PBS, 1×), K₄Fe(CN)₆, K₃Fe(CN)₆, KCl, dopamine hydrochloride, buspirone hydrochloride, etoposide, and acetaminophen (APAP), carboxylic acid-functionalized 50 nm gold nanoparticles coated with polyethylene glycol (PEG 3000), crosslinking reagents EDC, sulfo-NHS, bis(sulfosuccinimidyl)suberate (BS3), ethanolamine, bovine serum albumin (BSA), and Tween 20 were purchased from Sigma-Aldrich (Buchs, Switzerland). PEGylated alkanethiol compounds HS-C₆EG₄OH and HS-C₁₁EG₄OCH₂COOH were acquired from Prochimia Surfaces (Sopot, Poland). Dopamine (D3) receptor synthetic peptide (ab128688) was purchased from Abcam (Cambridge, UK).

Kilic T., Soler M., Fahimi-Kashani N., Altug H, & Carrara S. (2018). Mining the Potential of Label-Free Biosensors for In Vitro Antipsychotic Drug Screening. Biosensors, 8(1), 6.

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Characterization of Erythromycin Metabolism

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Erythromycin A dihydrate (analytical standard), CLA (≥95% standard), buspirone hydrochloride, dimethylsulfoxide (DMSO, 1.100 g/mL), and the reduced form of β-nicotinamide dinucleotide phosphate (NADPH, ≥93% standard) were purchased from Sigma-Aldrich (St. Louis, MO, USA). N-Desmethyl-erythromycin A and N-desmethyl clarithromycin were purchased from Santa Cruz Biotechnology (Santa Cruz, CA, USA). Potassium phosphate buffer (0.1 M, pH 7.4) was purchased from Biosesang (Seongnam, Korea). HPLC-grade methanol and acetonitrile (ACN) were supplied by J.T. Baker Chemical (Radnor, PA, USA). Chicken liver microsomes (PL-MIC-201) were purchased from PRIMACYT GmbH (Schwerin, FRG, Germany) and stored at −80 °C before use. All chemicals were of the highest purity available.

Wang B., Nam S., Kim E., Jeon H., Lee K, & Xie K. (2021). Identification of Erythromycin and Clarithromycin Metabolites Formed in Chicken Liver Microsomes Using Liquid Chromatography–High-Resolution Mass Spectrometry. Foods, 10(7), 1504.

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Preparation of Psychoactive Drug Solutions

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Yohimbine hydrochloride (Tocris, UK) was dissolved in distilled water. Citalopram hydrobromide (Tocris, UK), buspirone hydrochloride (Sigma, UK) amphetamine (Sigma, UK) and alpha-flupenthixol (Sigma, UK) were dissolved in 0.9 % saline. FG7142 (β-carboline-3-carboxylic acid N-methylamide) and diazepam (both Sigma, UK) were dissolved in 10 % dimethyl sulphoxide (DMSO; BDH Laboratory Supplies, UK), 20 % cremophor EL (Sigma, UK) and 70 % of 0.9 % saline. All drugs were administered at a final volume of 1 ml/kg.

Phelps C.E., Mitchell E.N., Nutt D.J., Marston H.M, & Robinson E.S. (2015). Psychopharmacological characterisation of the successive negative contrast effect in rats. Psychopharmacology, 232(15), 2697-2709.

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Anxiolytic Effects of Buspirone and MTEP

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Treatments were administered systemically via intraperitoneal injection, 30 min prior to
the onset of behavioral testing. Ten animals from each drinking group received a 5 mg/kg
injection of buspirone hydrochloride (Sigma-Aldrich, Atlanta, GA) in sterile water. This
buspirone dose was selected for study as it elicits anxiolytic effects in other
drug-related behavioral paradigms.^{30 (link)–32 (link, link)} An additional 10 animals from each
drinking group received a 3 mg/kg injection of the mGlu5 antagonist MTEP in sterile water.
This MTEP dose was selected for study based on evidence of anxiolytic efficacy in
rodents.^{33 (link)–35 (link, link)} The remaining animals served as vehicle
controls and received injections of sterile water (Vol = 0.01 ml/g).

Lee K.M., Coelho M.A., Sern K.R., Class M.A., Bocz M.D, & Szumlinski K.K. (2017). Anxiolytic Effects of Buspirone and MTEP in the Porsolt Forced Swim Test. Chronic Stress, 1, 2470547017712985.

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Substance Preparation for Neuroscience Study

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Ethanol (95% ethyl alcohol) was obtained from The Warner-Graham Company (Cockeysville, MD) and diluted each morning prior to mixing with Tang. (−)-Cocaine HCl was obtained from the National Institute on Drug Abuse (Bethesda, MD). (−)-Quinpirole hydrochloride, R(+)-SCH23390 hydrochloride, eticlopride hydrochloride and buspirone hydrochloride were obtained from Sigma-Aldrich (St. Louis, MO). Cocaine, quinpirole and eticlopride were dissolved in sterile 0.9% saline. Buspirone and SCH 23390 were dissolved in sterile water. Drugs, were sterile-filtered prior to intravenous administration. Doses are expressed based on the salt form.

, & Czoty P.W. (2015). Effects of chronic binge-like ethanol consumption on cocaine self-administration in rhesus monkeys. Drug and alcohol dependence, 153, 278-285.

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Attenuating Acute Hypersensitivity in Neonatal Rats

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For 5-HT3R antagonism, the selective 5-HT3R antagonist Ondansetron (OND; ondansetron hydrochloride dihydrate, Sigma-Aldrich, O3639) was dissolved in sterile saline in a concentration of 2 μg/μl. For 5-HT1aR agonism, the selective agonist Buspirone (BUS, buspirone hydrochloride; Sigma-Aldrich, B7148) was dissolved in sterile saline to a concentration of 10 μg/μl. Pilot studies testing 1, 3 and 5 mg/kg BUS and 0.3, 1 and 3 mg/kg OND showed that 3 mg/kg BUS and 3 mg/kg OND were most promising in preventing acute hypersensitivity associated with neonatal repetitive needle pricking (see Figure 1), without adverse side effects (including body weight changes or mortality). Based on pup's body weight per postnatal day, 50 μl solution containing OND (3 mg/kg) or BUS (3 mg/kg) was injected sc. twice daily (at 9 a.m. before the 1st needle prick and 11 a.m. before the 3 rd needle prick). TC and NP animals received an equivalent volume of saline.

de Kort A.R., Joosten E.A., Patijn J., Tibboel D, & van den Hoogen N.J. (2022). Selective Targeting of Serotonin 5-HT1a and 5-HT3 Receptors Attenuates Acute and Long-Term Hypersensitivity Associated With Neonatal Procedural Pain. Frontiers in Pain Research, 3, 872587.

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