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Gaboxadol hydrochloride

Manufactured by Merck Group

Gaboxadol hydrochloride is a chemical compound developed by Merck Group for use in pharmaceutical research and development. It functions as a selective agonist of the GABAA receptor, which plays a role in the inhibitory neurotransmission in the central nervous system. The compound is utilized in various in vitro and in vivo laboratory studies to investigate the effects of GABAA receptor modulation.

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4 protocols using gaboxadol hydrochloride

1

Preparation and Administration of Neuroactive Steroids

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Gaboxadol hydrochloride (Sigma-Aldrich Co., St. Louis, MO) was dissolved in sterile 0.9% saline. Pregnanolone (5β-pregnan-3α-ol-20-one; National Institute on Drug Abuse Drug Supply Program, Bethesda, MD) was dissolved in 45% (w/v) 2-hydroxypropyl-β-cyclodextrin. Midazolam hydrochloride (Bedford Laboratories, Bedford, OH) and ethanol were purchased as commercially prepared solutions and diluted with sterile 0.9% saline. Flumazenil (Enzo Life Sciences, Farmingdale, NY) was dissolved in a vehicle comprising 10% ethanol, 40% propylene glycol, and 50% sterile water. Drugs were administered i.p. typically in a volume of 1 ml/kg body weight with the exception of ethanol for which a 15% v/v solution was used for all injections. Doses are expressed in the form listed above in mg/kg or g/kg body weight.
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2

Cocaine and Gaboxadol Hydrochloride Experiments

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Cocaine hydrochloride, a gift of the National Institute on Drug Abuse through the Research Triangle Institute (Research Triangle Park, NC), and Gaboxadol hydrochloride (Sigma-Aldrich, St. Louis, MO) were used in the experiments. All drugs were diluted in saline and injected at 1 ml/kg body weight except in Experiment 3, in which intracranial injections of GBX were used.
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3

Gaboxadol-Enriched Paraquat Exposure

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Gaboxadol hydrochloride (Sigma-Aldrich, St. Louis, MO) was dissolved in water and added to melted cornmeal food to a final concentration of 0.1–0.2 mg/mL. Flies were flipped onto Gaboxadol-containing food for 3 days prior to paraquat injection and remained on Gaboxadol-containing food postinjection. Control food was made by adding the appropriate amount of vehicle alone (H2O) to melted cornmeal food.
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4

Selective Modulation of GABA Receptor Subtypes

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Drugs were injected i.h. at a volume of 0.25 µL per side at a rate of 0.5 µL min−1 or i.p. at a volume of 200 µL 20–30 min prior to fear conditioning or retrieval test. α4δ- and/or α6δ-subunit-containing GABAAR were activated by gaboxadol hydrochloride (0.5 µg per DH, dissolved in artificial cerebrospinal fluid; Sigma-Aldrich) also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP); α1-3-subunit-containing GABAAR were activated by zolpidem (25 µg per DH, 100% dimethyl sulfoxide (DMSO); Sigma-Aldrich); and α5-subunit-containing GABAAR were activated by SH-053-R-CH3-2'F (20 µg per DH, dissolved in 90% DMSO; synthesized at University of Wisconsin–Milwaukee) or MP-III-022 (12.5 µg per DH; dissolved in 60% DMSO; synthesized at University of Wisconsin–Milwaukee).
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