Chemistry:Naluzotan

From HandWiki
Short description: Chemical compound
Naluzotan
Naluzotan.svg
Clinical data
Routes of
administration		Oral[1]
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC23H38N4O3S
Molar mass450.64 g·mol−1
3D model (JSmol)
  (verify)

Naluzotan (INN, USAN; PRX-00023) is a serotonergic drug of the phenylpiperazine class that was under investigation by EPIX Pharmaceuticals Inc for the treatment of generalized anxiety disorder and major depressive disorder.[1][2] It acts as a selective and potent 5-HT1A receptor partial agonist,[2][3] readily stimulating prolactin responses,[4] though it has also been found to bind to and activate the σ receptor.[5] Naluzotan was well tolerated in clinical trials,[4] with more patients in the control group dropping out due to adverse effects than in the active group in one study.[2] The most frequently reported side effect was headache in 15% of patients (compared to 10% for placebo).[2] In addition, naluzotan demonstrated significant antidepressant and anxiolytic effects as per the HAM-D and MADRS and the HAM-A, respectively, in some trials,[2] but in others it did not.[6][7] In the end it was not found to be significantly superior enough to placebo and development was stopped.[7]

See also

References

  1. ↑ 1.0 1.1 "Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression.". Curr Opin Investig Drugs 8 (1): 78–86. 2007. PMID 17263189. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "Effects of PRX-00023, a novel, selective serotonin 1A receptor agonist on measures of anxiety and depression in generalized anxiety disorder: results of a double-blind, placebo-controlled trial". J Clin Psychopharmacol 28 (2): 235–239. 2008. doi:10.1097/JCP.0b013e31816774de. PMID 18344738. 
  3. ↑ "An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression". J Med Chem 49 (11): 3116–3135. 2006. doi:10.1021/jm0508641. PMID 16722631. 
  4. ↑ 4.0 4.1 "Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects.". J Clin Pharmacol 47 (7): 817–824. 2007. doi:10.1177/0091270007300953. PMID 17495280. 
  5. ↑ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 978-0-470-51979-0. https://books.google.com/books?id=pfY3xcsu6EsC&q=PRX-00023&pg=PA265. 
  6. ↑ "Short-term tolerability of a nonazapirone selective serotonin 1A agonist in adults with generalized anxiety disorder: a 28-day, open-label study". Clin. Ther. 30 (9): 1658–1666. 2008. doi:10.1016/j.clinthera.2008.09.006. PMID 18840371. 
  7. ↑ 7.0 7.1 "Discontinued psychiatric drugs in 2008". Expert Opinion on Investigational Drugs 18 (10): 1431–43. October 2009. doi:10.1517/13543780903184591. PMID 19715445. http://informahealthcare.com/doi/abs/10.1517/13543780903184591. 




Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:Naluzotan&oldid=3710923"