Esmirtazapine

Esmirtazapine

Esmirtazapine
Systematic (IUPAC) name
(S)-1,2,3,4,10,14b-hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benzazepine
Clinical data
Legal status
  • Uncontrolled
Routes Oral
Pharmacokinetic data
Metabolism Liver ([1]
Identifiers
CAS number  YesY
ATC code None
PubChem
ChemSpider  YesY
UNII  YesY
KEGG  YesY
Chemical data
Formula C21H23N3O4 
Mol. mass 381.43 g/mol
Physical data
Melt. point 114–116 °C (237–241 °F)
Solubility in water Soluble in methanol and chloroform mg/mL (20 °C)
 YesY   

Esmirtazapine (ORG-50,081) is a [3][4][5] As of 2009 it is in phase III clinical trials.[2] Esmirtazapine is the (S)-(+)-enantiomer of mirtazapine and possesses similar overall pharmacology, including inverse agonist actions at H1 and 5-HT2 receptors and antagonist actions at α2-adrenergic receptors.[2][6] As of March 2010, Merck terminated internal clinical development program for esmirtazapine, for hot flashes and insomnia, for strategic reasons.[7]

See also

References

  1. ^ "A population analysis on the effects of the CYP2D6 deficiency on pharmacokinetics and exposure of esmirtazapine in healthy volunteers". 
  2. ^ a b c "Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net". 
  3. ^ "A Long-Term Safety Study of Org 50081 in Elderly Outpatients With Chronic Primary Insomnia (176005)(P05697) - Full Text View - ClinicalTrials.gov". 
  4. ^ Teegarden BR, Al Shamma H, Xiong Y (2008). "5-HT(2A) inverse-agonists for the treatment of insomnia". Current Topics in Medicinal Chemistry 8 (11): 969–76.  
  5. ^ Lewis V (November 2009). "Undertreatment of menopausal symptoms and novel options for comprehensive management". Current Medical Research and Opinion 25 (11): 2689–98.  
  6. ^ Depression and bipolar disorder: Stahl's essential psychopharmacology. Cambridge, UK: Cambridge University Press. 2008.  
  7. ^ http://www.merck.com/investors/financials/form-10-K-2009-final.pdf