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Panadiplon

Chemical compound

Chemical compound

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Panadiplon (U-78875) is an anxiolytic drug with a novel chemical structure that is not closely related to other drugs of this type. It has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and relatively little sedative or amnestic effect, and so is classified as a nonbenzodiazepine anxiolytic.

Panadiplon acts as a high-affinity GABAA receptor partial agonist, but despite showing a useful effects profile of a potent anxiolytic with little sedative effects, panadiplon was discontinued from clinical development for use in humans after showing evidence of liver damage in both animals and human trials. Panadiplon however continues to be used in animal research, mainly as a subtype-selective reference drug to compare other GABAA agonists against.

References

References

  1. (October 1991). "Behavioral effects of U-78875, a quinoxalinone anxiolytic with potent benzodiazepine antagonist activity". The Journal of Pharmacology and Experimental Therapeutics.
  2. (June 1999). "Drug discrimination analysis of partial agonists at the benzodiazepine site. I. Differential effects of U-78875 across training conditions in baboons and rats". The Journal of Pharmacology and Experimental Therapeutics.
  3. (February 2001). "Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys". Drug and Alcohol Dependence.
  4. (April 1995). "Induction of a hepatic toxic syndrome in the Dutch-belted rabbit by a quinoxalinone anxiolytic". Toxicology.
  5. (May 2001). "Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon". Chemico-Biological Interactions.
  6. (May 2005). "Contribution of alpha 1GABAA and alpha 5GABAA receptor subtypes to the discriminative stimulus effects of ethanol in squirrel monkeys". The Journal of Pharmacology and Experimental Therapeutics.
  7. (November 2002). "5-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5]imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide (RWJ-51204), a new nonbenzodiazepine anxiolytic". The Journal of Pharmacology and Experimental Therapeutics.
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sedatives anxiolytics hepatotoxins oxadiazoles lactams cyclopropyl-compounds gabaa-receptor-positive-allosteric-modulators isopropyl-compounds
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