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Panadiplon

Catalog No. T28294   CAS 124423-84-3
Synonyms: FG10571, FG-10571, FD-10571, PNU 78875, FG 10571, FD10571, FD 10571

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

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Panadiplon Chemical Structure
Panadiplon, CAS 124423-84-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 143.00
5 mg In stock $ 360.00
10 mg In stock $ 530.00
25 mg In stock $ 859.00
50 mg In stock $ 1,180.00
100 mg In stock $ 1,590.00
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Purity: 100%
Purity: 99.75%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.
In vitro Panadiplon (10 μg/ml; 48 h; under normoxic conditions; hepatocytes) reduced ATP and glycogen levels by 40% but did not cause an increase in LDH leakage. Cells treated with panadiplon, then exposed to hypoxia conditions, showed a significant level of injury compared to normoxic control cultures, and a further reduction in ATP. No additional decrease in glycogen was observed. In an attempt to prevent panadiplon-mediated injury, glycolytic substrates (dihydroxyacetone or pyruvate) were included during normoxic and hypoxic incubations. Both treatments reduced the level of LDH leakage produced by panadiplon during hypoxia. Cotreatment did not generally increase ATP or glycogen levels (compared to panadiplon treatment groups) during hypoxia, though individual experiments showed a slight increase in ATP levels. During normoxia, both cotreatments with panadiplon resulted in significantly higher glycogen levels than in panadiplon cultures alone. These results suggest that cellular glycogen and subsequently ATP levels are reduced during panadiplon exposure, metabolically predisposing hepatocytes to hypoxic injury.[2]
Synonyms FG10571, FG-10571, FD-10571, PNU 78875, FG 10571, FD10571, FD 10571
Molecular Weight 335.36
Formula C18H17N5O2
CAS No. 124423-84-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Platt DM, et al. Contribution of alpha 1GABAA and alpha 5GABAA receptor subtypes to the discriminative stimulus effects of ethanol in squirrel monkeys. J Pharmacol Exp Ther. 2005;313(2):658-667. 2. Bacon JA, et al. Potentiation of hypoxic injury in cultured rabbit hepatocytes by the quinoxalinone anxiolytic, panadiplon. Toxicology. 1996;108(1-2):9-16. 3. Rowlett JK, et al. Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys. Drug Alcohol Depend. 2001;61(3):229-236. 4. Ulrich RG, et al. Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon. Chem Biol Interact. 2001;134(3):251-270. 5. Ulrich RG, et al. Disruption of mitochondrial activities in rabbit and human hepatocytes by a quinoxalinone anxiolytic and its carboxylic acid metabolite. Toxicology. 1998;131(1):33-47.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Panadiplon 124423-84-3 Membrane transporter/Ion channel Neuroscience GABA Receptor FG10571 PNU78875 FG-10571 PNU-78875 FD-10571 PNU 78875 FG 10571 FD10571 FD 10571 inhibitor inhibit

 

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