Naluzotan

Naluzotan

Naluzotan
Systematic (IUPAC) name
N-(3-{4-[4-(1-cyclohexylmethanesulfonamido)butyl]piperazin-1-yl}phenyl)acetamide
Clinical data
Legal status
?
Routes Oral[1]
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
UNII  YesY
Chemical data
Formula C23H38N4O3S 
Mol. mass 450.638 g/mol
 YesY   

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. ^ a b de Paulis T. (2007). "Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression.". Curr Opin Investig Drugs. 8 (1): 78–86.  
  2. ^ a b c d e Rickels K, Mathew S, Banov MD, Zimbroff DL, Oshana S, Parsons EC Jr, Donahue SR, Kauffman M, Iyer GR, Reinhard JF Jr.; Mathew; Banov; Zimbroff; Oshana; Parsons Jr; Donahue; Kauffman; Iyer; Reinhard Jr (2008). "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.  
  3. ^ Becker OM, Dhanoa DS, Marantz Y, Chen D, Shacham S, Cheruku S, Heifetz A, Mohanty P, Fichman M, Sharadendu A, Nudelman R, Kauffman M, Noiman S.; Dhanoa; Marantz; Chen; Shacham; Cheruku; Heifetz; Mohanty; Fichman; Sharadendu; Nudelman; Kauffman; Noiman (2006). "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.  
  4. ^ a b de Paulis T.; Reinhard Jr, JF; Oshana, S; Kauffman, M; Donahue, S (2007). "Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects.". J Clin Pharmacol. 47 (7): 817–824.  
  5. ^ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley.  
  6. ^ Mathew SJ, Garakani A, Reinhard JF Jr, Oshana S, Donahue S.; Garakani; Reinhard; Oshana; Donahue (2008). "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.  
  7. ^ a b Kirchhoff VD, Nguyen HT, Soczynska JK, Woldeyohannes H, McIntyre RS; Nguyen; Soczynska; Woldeyohannes; McIntyre (October 2009). "Discontinued psychiatric drugs in 2008". Expert Opinion on Investigational Drugs 18 (10): 1431–43.