Wikipedia:WikiProject Chemicals/Chembox validation/VerifiedDataSandbox and Panadiplon: Difference between pages

{{short description|Chemical compound}}

| verifiedrevid = 464197175

| legal_status = See [[Hepatotoxic]]

| routes_of_administration =

| excretion =

| CAS_number = 124423-84-3

'''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.<ref name="pmid1681085">{{cite journal | vauthors = Tang AH, Franklin SR, Himes CS, Ho PM | title = Behavioral effects of U-78875, a quinoxalinone anxiolytic with potent benzodiazepine antagonist activity | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 259 | issue = 1 | pages = 248–54 | date = October 1991 | pmid = 1681085 }}</ref>

Panadiplon acts as a high-affinity [[GABAA receptor|GABA_A]] receptor [[partial agonist]],<ref name="pmid10336537">{{cite journal | vauthors = Ator NA, Griffiths RR | title = Drug discrimination analysis of partial agonists at the benzodiazepine site. I. Differential effects of U-78875 across training conditions in baboons and rats | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 289 | issue = 3 | pages = 1434–46 | date = June 1999 | pmid = 10336537 }}</ref><ref name="pmid11164687">{{cite journal | vauthors = Rowlett JK, Woolverton WL | title = Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys | journal = Drug and Alcohol Dependence | volume = 61 | issue = 3 | pages = 229–36 | date = February 2001 | pmid = 11164687 | doi = 10.1016/s0376-8716(00)00142-3 }}</ref> 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.<ref name="pmid7740546">{{cite journal | vauthors = Ulrich RG, Bacon JA, Branstetter DG, Cramer CT, Funk GM, Hunt CE, Petrella DK, Sun EL | title = Induction of a hepatic toxic syndrome in the Dutch-belted rabbit by a quinoxalinone anxiolytic | journal = Toxicology | volume = 98 | issue = 1–3 | pages = 187–98 | date = April 1995 | pmid = 7740546 | doi = 10.1016/0300-483x(94)02951-p }}</ref><ref name="pmid11336974">{{cite journal | vauthors = Ulrich RG, Bacon JA, Brass EP, Cramer CT, Petrella DK, Sun EL | title = Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon | journal = Chemico-Biological Interactions | volume = 134 | issue = 3 | pages = 251–70 | date = May 2001 | pmid = 11336974 | doi = 10.1016/s0009-2797(01)00161-2 }}</ref> Panadiplon however continues to be used in animal research, mainly as a subtype-selective reference drug to compare other GABA_A agonists against.<ref name="pmid15650112">{{cite journal | vauthors = Platt DM, Duggan A, Spealman RD, Cook JM, Li X, Yin W, Rowlett JK | title = Contribution of alpha 1GABAA and alpha 5GABAA receptor subtypes to the discriminative stimulus effects of ethanol in squirrel monkeys | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 313 | issue = 2 | pages = 658–67 | date = May 2005 | pmid = 15650112 | doi = 10.1124/jpet.104.080275 | s2cid = 97681615 }}</ref><ref name="pmid12388665">{{cite journal | vauthors = 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 | title = 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 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 303 | issue = 2 | pages = 777–90 | date = November 2002 | pmid = 12388665 | doi = 10.1124/jpet.102.036954 | s2cid = 23880756 }}</ref>

== References ==

{{reflist}}

{{Anxiolytics}}

{{GABAAR PAMs}}

[[Category:Sedatives]]

[[Category:Anxiolytics]]

[[Category:Hepatotoxins]]

[[Category:Oxadiazoles]]

[[Category:Lactams]]

[[Category:Cyclopropanes]]

[[Category:GABAA receptor positive allosteric modulators]]

[[Category:Isopropyl compounds]]