PRX-00023

PRX-00023
Systematic (IUPAC) name
	N-(3-[4-(4-cyclohexylmethanesulfonylaminobutyl)piperazin-1-yl]phenyl)acetamide
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
ATC code	None
PubChem	CID 11430856
UNII	LQ54E5B4EW
Chemical data
Formula	C23H38N4O3S
Mol. mass	450.636 g/mol
SMILES	eMolecules & PubChem
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PRX-00023 is a drug of the phenylpiperazine class that was being developed by EPIX Pharmaceuticals Inc for the treatment of generalized anxiety disorder and major depressive disorder.^[1]^[2] It was well tolerated in clinical trials but failed to reach significant remission on the Hammilton Rating Scales and development was subsequently discontinued.^[2]^[3]^[4]

PRX-00023 acts as a selective 5-HT_1A receptor ligand and σ receptor agonist.^[2]^[5]^[6] Originally believed to have appreciable intrinsic activity as an agonist of the 5-HT_1A receptor, later studies found it to possess very low efficacy (6-7% relative to 5-HT) and to behave more like an antagonist, likely underlying its failure as an antidepressant/anxiolytic in clinical trials.^[7]

[edit] See also

Phenylpiperazine

[edit] References

^ 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 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. doi:10.1097/JCP.0b013e31816774de. PMID 18344738.
^ 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. doi:10.1177/0091270007300953. PMID 17495280.
^ 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. doi:10.1016/j.clinthera.2008.09.006. PMID 18840371.
^ 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.
^ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7. http://books.google.com/?id=pfY3xcsu6EsC&lpg=PA265&dq=adatanserin&pg=PA265#v=onepage&q=PRX-00023.
^ Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B (October 2007). "High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity". Journal of Medicinal Chemistry 50 (20): 5024–33. doi:10.1021/jm070714l. PMID 17803293.

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[pmid17263189-0] 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.

[pmid18344738-1] 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. doi:10.1097/JCP.0b013e31816774de. PMID 18344738.

[pmid17495280-2] 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. doi:10.1177/0091270007300953. PMID 17495280.

[pmid18840371-3] 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. doi:10.1016/j.clinthera.2008.09.006. PMID 18840371.

[pmid16722631-4] 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.

[isbn0-470-51979-7-5] Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7. http://books.google.com/?id=pfY3xcsu6EsC&lpg=PA265&dq=adatanserin&pg=PA265#v=onepage&q=PRX-00023.

[pmid17803293-6] Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B (October 2007). "High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity". Journal of Medicinal Chemistry 50 (20): 5024–33. doi:10.1021/jm070714l. PMID 17803293.

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PRX-00023

[edit] See also

[edit] References

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