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Уреди везе
PRX-00023
IUPAC ime
N-(3-[4-(4-cikloheksilmetansulfonilaminobutil)piperazin-1-il]fenil)acetamid
Identifikatori
ATC kodnone
PubChemCID 11430856
Hemijski podaci
FormulaC23H38N4O3S
Molarna masa450,636 g/mol
  • CC(=O)Nc2cccc(c2)N1CCN(CC1)CCCCNS(=O)(=O)CC3CCCCC3

PRX-00023 je lek iz fenilpiperazinske klase koji je razvijala kompanija EPIX Farmaceutikals za lečenje generalizovanog anksiznog poremećaja i kliničke depresije.[1][2] On je bio dobro tolerisan u kliničkim ispitivanjima, ali je nije bio uspešan u dostizanju značajne remisije i stoga je razvoj prekinut.[2][3][4]

PRX-00023 deluje kao selektivni ligand 5-HT1A receptora i agonist σ receptora.[2][5][6] Originalno se smatralo da on ima znatnu efikasnost kao agonist 5-HT1A receptora. Kasnije studije su utvrdile da poseduje veoma nisku efikasnost (6-7% relativno na 5-HT) i da se ponaša više kao antagonist, što je verovatan uzrok njegovog neuspeha kao antidepresiv/anksiolitik u kliničkim ispitivanjima.[7]

Vidi još

Reference

  1. ^ 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. ^ а б в Rickels K, Mathew S, Banov MD, Zimbroff DL, Oshana S, Parsons EC Jr, Donahue SR, Kauffman M, Iyer GR, Reinhard JF 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. PMID 18344738. doi:10.1097/JCP.0b013e31816774de. 
  3. ^ 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. PMID 17495280. doi:10.1177/0091270007300953. 
  4. ^ Mathew SJ, Garakani A, Reinhard JF Jr, 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. PMID 18840371. doi:10.1016/j.clinthera.2008.09.006. 
  5. ^ 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. PMID 16722631. doi:10.1021/jm0508641. 
  6. ^ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7. 
  7. ^ Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B (2007). „High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity”. Journal of Medicinal Chemistry. 50 (20): 5024—33. PMID 17803293. doi:10.1021/jm070714l. 

Literatura


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source: https://sr.wikipedia.org/wiki/PRX-00023