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Panadiplon
Systematic (IUPAC) name
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5 -propan-2-ylimidazo[5,1-c]quinoxalin-4-one
Identifiers
CAS number 124423-84-3
ATC code none
PubChem 3033821
Chemical data
Formula C 18H17N5O2  
Mol. mass 335.36 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?


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.[1]

Panadiplon acts as a high-affinity GABAA receptor partial agonist,[2][3] 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.[4][5] Panadiplon however continues to be used in animal research, mainly as a subtype-selective reference drug to compare other GABAA agonists against.[6][7]

References

  1. ^ Tang AH, Franklin SR, Himes CS, Ho PM. Behavioral effects of U-78875, a quinoxalinone anxiolytic with potent benzodiazepine antagonist activity. J Pharmacol Exp Ther. 1991 Oct;259(1):248-54.
  2. ^ Ator NA, Griffiths RR. Drug discrimination analysis of partial agonists at the benzodiazepine site. I. Differential effects of U-78875 across training conditions in baboons and rats. J Pharmacol Exp Ther. 1999 Jun;289(3):1434-46.
  3. ^ Rowlett JK, Woolverton WL. Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys. Drug Alcohol Depend. 2001 Feb 1;61(3):229-36.
  4. ^ Ulrich RG, Bacon JA, Branstetter DG, Cramer CT, Funk GM, Hunt CE, Petrella DK, Sun EL. Induction of a hepatic toxic syndrome in the Dutch-belted rabbit by a quinoxalinone anxiolytic. Toxicology. 1995 Apr 12;98(1-3):187-98.
  5. ^ Ulrich RG, Bacon JA, Brass EP, Cramer CT, Petrella DK, Sun EL. Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon. Chem Biol Interact. 2001 May 16;134(3):251-70.
  6. ^ Platt DM, Duggan A, Spealman RD, Cook JM, Li X, Yin W, Rowlett JK. Contribution of alpha 1GABAA and alpha 5GABAA receptor subtypes to the discriminative stimulus effects of ethanol in squirrel monkeys. J Pharmacol Exp Ther. 2005 May;313(2):658-67.
  7. ^ Dubinsky B, Vaidya AH, Rosenthal DI, Hochman C, Crooke JJ, DeLuca S, DeVine A, Cheo-Isaacs CT, Carter AR, Jordan AD, Reitz AB, Shank RP. 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. J Pharmacol Exp Ther. 2002 Nov;303(2):777-90.
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