PRX-00023

PRX-00023
(IUPAC) ime
	N-(3-[4-(4-cikloheksilmetansulfonilaminobutil)piperazin-1-il]fenil)acetamid
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	11430856
Hemijski podaci
Formula	C23H38N4O3S
Mol. masa	450,636 g/mol
SMILES	eMolekuli & PubHem
InChI
	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
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

PRX-00023 je lek iz fenilpiperazinske klase koji je razvijala kompanija EPIX Farmaceutikals za lečenje generalizovanog anksiznog poremećaja i kliničke depresije.^[3]^[4] On je bio dobro tolerisan u kliničkim ispitivanjima, ali je nije bio uspešan u dostizanju značajne remisije i stoga je razvoj prekinut.^[4]^[5]^[6]

PRX-00023 deluje kao selektivni ligand 5-HT_1A receptora i agonist σ receptora.^[4]^[7]^[8] Originalno se smatralo da on ima znatnu efikasnost kao agonist 5-HT_1A 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.^[9]

Povezano

Fenilpiperazin

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ 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.
↑ ^4,0 ^4,1 ^4,2 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.
↑ 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.

Literatura

Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[pmid17263189-3] 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.

[pmid18344738-4] 4,0 ^4,1 ^4,2 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.

[pmid17495280-5] 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.

[pmid18840371-6] 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.

[pmid16722631-7] 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.

[isbn0-470-51979-7-8] Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7.

[pmid17803293-9] 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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