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Zaleplon

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Zaleplon Basic information
Zaleplon Chemical Properties
  • Melting point:186-1870C
  • Density 1.25±0.1 g/cm3(Predicted)
  • Flash point:9℃
  • storage temp. 2-8°C
  • solubility DMSO: ~20mg/mL
  • pka-1.47±0.50(Predicted)
  • color white
  • CAS DataBase Reference151319-34-5(CAS DataBase Reference)
Safety Information
MSDS
Zaleplon Usage And Synthesis
  • DescriptionZaleplon was introduced in Sweden and Denmark as a new treatment for insomnia, particularly in patients who have difficulty in falling asleep. Zaleplon is a non-benzodiazepine compound and is the first in a new generation belonging to the pyrazolopyrimidine class, showing therefore fewer benzodiazepine-like side effects. It can be synthesized in 3 steps from the corresponding acetophenone, the key step being the cyclization of the appropriate enaminone with 3-aminopyrazole-4-carbonitrile. Biochemically, Zaleplon is a full agonist at the benzodiazepine o)1 site of the gaba-A receptor complex, but its behavioural profile remains distinct from both benzodiazepine (e.g. Lorazepam) or non-benzodiazepine (e.g. Zopiclone or Zolpidem) sedativehypnotic drugs. Clinical pharmacokinetic analysis showed rapid absorption and elimination. In man, the main metabolic route was oxidative giving the major metabolites 5-oxo Zaleplon and its N-desethyl analog. Both were shown to have no effect at central benzodiazepine receptors and to be rapidly excreted as glucuronides. In patients with chronic insomnia, Zaleplon at 5 and 10 mg/kg significantly reduced sleep latency and improved the quality of sleep compared with placebo without altering the normal sleep architecture. Given its short halflife, the next-day residual effects such as hangover are minimized. It may have some advantages over benzodiazepines regarding unwanted amnesic effects and psychomotor impairment. There was no evidence for the occurrence of rebound insomnia at 10 mg/kg.
  • Chemical PropertiesOff-White Powder
  • OriginatorAmerican Home Products (US)
  • UsesSelective non-benzodiazepine GABAA receptor agonist
  • Usestopical antibacterial (topical)
  • DefinitionChEBI: A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.
  • brand nameSonata (Jones).
  • General DescriptionZaleplon (Sonata, a pyrazolopyrimidine) isanother short-acting nonbenzodiazepine hypnotic.Pharmacologically and pharmacokinetically, zaleplon is similarto zolpidem; both are hypnotic agents with short halflives.It also has selective high affinity for α1-subunit containingBzRs but produces effects at other BzR/GABAAsubtypes as well. Zaleplon is well absorbed following oraladministration with an absolute bioavailability of approximately30% because of significant presystemic metabolism.It exhibits a mean half-life of approximately 1 hour, with lessthan 1% of the dose excreted unchanged in urine. It is primarilymetabolized by aldehyde oxidase to 5-oxo-zaleplon andis also metabolized to a lesser extent by CYP3A4. Ndemethylationyields desethylzaleplon, which is quickly converted,presumably by aldehyde oxidase, to 5-oxo-desethylzaleplon.These oxidative metabolites are thenconverted to glucuronides and eliminated in urine. All of zaleplon’smetabolites are pharmacologically inactive. It mayhave a more rapid onset (about 1 hour) and termination of actionthan zolpidem, and therefore, it is good to initiate sleepinstead of keeping sleep.
  • Biological ActivityNon-benzodiazepine agent that acts as an agonist at the benzodiazepine site. Displays hypnotic, anxiolytic, myorelaxant and anticonvulsant activity.
Zaleplon Preparation Products And Raw materials
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