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Naluzotan

May 07, 2024

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]

Naluzotan
Clinical data
Routes of
administration		Oral[1]
ATC code
  • None
Identifiers
  • N-(3-{4-[4-(1-cyclohexylmethanesulfonamido)butyl]piperazin-1-yl}phenyl)acetamide
CAS Number
  • 740873-06-7
PubChem CID
  • 11430856
ChemSpider
  • 9605731
UNII
  • LQ54E5B4EW
CompTox Dashboard (EPA)
  • DTXSID40995527
Chemical and physical data
FormulaC23H38N4O3S
Molar mass450.64 g·mol−1
3D model (JSmol)
  • Interactive image
  • O=C(Nc3cccc(N2CCN(CCCCNS(=O)(=O)CC1CCCCC1)CC2)c3)C
  • InChI=1S/C23H38N4O3S/c1-20(28)25-22-10-7-11-23(18-22)27-16-14-26(15-17-27)13-6-5-12-24-31(29,30)19-21-8-3-2-4-9-21/h7,10-11,18,21,24H,2-6,8-9,12-17,19H2,1H3,(H,25,28)
  • Key:SPWZXWDPAWDKQE-UHFFFAOYSA-N
  (verify)

See also edit

References edit

  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. PMID 17263189.
  2. ^ a b c d e Rickels K, Mathew S, Banov MD, Zimbroff DL, Oshana S, Parsons EC, Donahue SR, Kauffman M, Iyer GR, Reinhard JF (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. doi:10.1097/JCP.0b013e31816774de. PMID 18344738. S2CID 40515142.
  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 (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. doi:10.1021/jm0508641. PMID 16722631.
  4. ^ a b Iyer GR, Reinhard 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. doi:10.1177/0091270007300953. PMID 17495280. S2CID 30536648.
  5. ^ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 978-0-470-51979-0.
  6. ^ Mathew SJ, Garakani A, Reinhard JF, Oshana S, Donahue S (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. doi:10.1016/j.clinthera.2008.09.006. PMID 18840371.
  7. ^ a b Kirchhoff VD, Nguyen HT, Soczynska JK, Woldeyohannes H, McIntyre RS (October 2009). "Discontinued psychiatric drugs in 2008". Expert Opinion on Investigational Drugs. 18 (10): 1431–43. doi:10.1517/13543780903184591. PMID 19715445. S2CID 34201544.


 

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May 07, 2024
naluzotan, usan, 00023, serotonergic, drug, phenylpiperazine, class, that, under, investigation, epix, pharmaceuticals, treatment, generalized, anxiety, disorder, major, depressive, disorder, acts, selective, potent, ht1a, receptor, partial, agonist, readily, . 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 s 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 NaluzotanClinical dataRoutes ofadministrationOral 1 ATC codeNoneIdentifiersIUPAC name N 3 4 4 1 cyclohexylmethanesulfonamido butyl piperazin 1 yl phenyl acetamideCAS Number740873 06 7PubChem CID11430856ChemSpider9605731UNIILQ54E5B4EWCompTox Dashboard EPA DTXSID40995527Chemical and physical dataFormulaC 23H 38N 4O 3SMolar mass450 64 g mol 13D model JSmol Interactive imageSMILES O C Nc3cccc N2CCN CCCCNS O O CC1CCCCC1 CC2 c3 CInChI InChI 1S C23H38N4O3S c1 20 28 25 22 10 7 11 23 18 22 27 16 14 26 15 17 27 13 6 5 12 24 31 29 30 19 21 8 3 2 4 9 21 h7 10 11 18 21 24H 2 6 8 9 12 17 19H2 1H3 H 25 28 Key SPWZXWDPAWDKQE UHFFFAOYSA N verify See also editPhenylpiperazineReferences edit 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 PMID 17263189 a b c d e Rickels K Mathew S Banov MD Zimbroff DL Oshana S Parsons EC Donahue SR Kauffman M Iyer GR Reinhard JF 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 doi 10 1097 JCP 0b013e31816774de PMID 18344738 S2CID 40515142 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 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 doi 10 1021 jm0508641 PMID 16722631 a b Iyer GR Reinhard 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 doi 10 1177 0091270007300953 PMID 17495280 S2CID 30536648 Prof John Kelly 2010 Principles of CNS Drug Development From Test Tube to Patient New York Wiley ISBN 978 0 470 51979 0 Mathew SJ Garakani A Reinhard JF Oshana S Donahue S 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 doi 10 1016 j clinthera 2008 09 006 PMID 18840371 a b Kirchhoff VD Nguyen HT Soczynska JK Woldeyohannes H McIntyre RS October 2009 Discontinued psychiatric drugs in 2008 Expert Opinion on Investigational Drugs 18 10 1431 43 doi 10 1517 13543780903184591 PMID 19715445 S2CID 34201544 nbsp This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Naluzotan amp oldid 1156529295, wikipedia, wiki, book, books, library,

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