Chemistry:Panadiplon
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| Formula | C18H17N5O2 |
| Molar mass | 335.367 g·mol−1 |
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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.[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
- ↑ "Behavioral effects of U-78875, a quinoxalinone anxiolytic with potent benzodiazepine antagonist activity". The Journal of Pharmacology and Experimental Therapeutics 259 (1): 248–54. October 1991. PMID 1681085.
- ↑ "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 289 (3): 1434–46. June 1999. PMID 10336537.
- ↑ "Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys". Drug and Alcohol Dependence 61 (3): 229–36. February 2001. doi:10.1016/s0376-8716(00)00142-3. PMID 11164687.
- ↑ "Induction of a hepatic toxic syndrome in the Dutch-belted rabbit by a quinoxalinone anxiolytic". Toxicology 98 (1–3): 187–98. April 1995. doi:10.1016/0300-483x(94)02951-p. PMID 7740546.
- ↑ "Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon". Chemico-Biological Interactions 134 (3): 251–70. May 2001. doi:10.1016/s0009-2797(01)00161-2. PMID 11336974.
- ↑ "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 313 (2): 658–67. May 2005. doi:10.1124/jpet.104.080275. PMID 15650112.
- ↑ "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 303 (2): 777–90. November 2002. doi:10.1124/jpet.102.036954. PMID 12388665.
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