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Pruvanserin

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Pruvanserin
Clinical data
Other namesEMD-281,014; EMD-281014; LY-2422347; LY2422347; LSN2411347; LSN-2411347
Routes of
administration		Oral[1]
Drug classSerotonin 5-HT2A receptor antagonist
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Pharmacokinetic data
Onset of actionTmaxTooltip Time to peak levels: 2–3 hours (range 2–6 hours)[2]
Eliminationhalf-life8.6–9.5 hours (range 3.9–12.4 hours)[2]
Identifiers
  • 7-[4-[2-(4-fluorophenyl)ethyl]piperazine-1-carbonyl]-1H-indole-3-carbonitrile
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC22H21FN4O
Molar mass376.435 g·mol−1
3D model (JSmol)
  • C1CN(CCN1CCC2=CC=C(C=C2)F)C(=O)C3=CC=CC4=C3NC=C4C#N
  • InChI=1S/C22H21FN4O/c23-18-6-4-16(5-7-18)8-9-26-10-12-27(13-11-26)22(28)20-3-1-2-19-17(14-24)15-25-21(19)20/h1-7,15,25H,8-13H2
  • Key:AQRLDDAFYYAIJP-UHFFFAOYSA-N

Pruvanserin (INNTooltip International Nonproprietary Name;USANTooltip United States Adopted Name; developmental code namesEMD-281,014,LY-2422347) is aselectiveserotonin5-HT2A receptorantagonist which was under development byEli Lilly and Company for the treatment ofinsomnia.[1][3][4] It was inphase IIclinical trials in 2008 but appears to have been discontinued as it is no longer in the company's development pipeline.[5][6]

Pharmacology

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Pharmacodynamics

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Pruvanserin acts as aselectiveserotonin5-HT2A receptorantagonist. In addition to itssleep-improving properties,[7][8] pruvanserin has also been shown to haveantidepressant,anxiolytic, andworking memory-enhancing effects in animal studies.[9][10][11]

Pharmacodynamics

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Thetime to peak levels of pruvanserin is 2 to 3 hours, with a range of 2 to 6 hours.[2] The meanelimination half-life of pruvanserin is 8.6 to 9.5 hours, with a range of 3.9 to 12.4 hours.[2] However, its brain serotonin 5-HT2A receptor occupancy lasts much longer, with a half-life of approximately 24 hours.[2]

See also

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References

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  1. ^ab"Pruvanserin".AdisInsight. 19 August 2014. Retrieved16 January 2026.
  2. ^abcdeMamo D, Sedman E, Tillner J, Sellers EM, Romach MK, Kapur S (September 2004). "EMD 281014, a specific and potent 5HT2 antagonist in humans: a dose-finding PET study".Psychopharmacology (Berl).175 (3):382–388.doi:10.1007/s00213-004-1817-7.PMID 15007535.
  3. ^Bartoszyk GD, van Amsterdam C, Böttcher H, Seyfried CA (July 2003). "EMD 281014, a new selective serotonin 5-HT2A receptor antagonist".European Journal of Pharmacology.473 (2–3):229–30.doi:10.1016/S0014-2999(03)01992-7.PMID 12892843.
  4. ^Teegarden BR, Al Shamma H, Xiong Y (2008). "5-HT(2A) inverse-agonists for the treatment of insomnia".Current Topics in Medicinal Chemistry.8 (11):969–76.doi:10.2174/156802608784936700.PMID 18673166.
  5. ^"Efficacy Study of LY2422347 to Treat Insomnia - Full Text View - ClinicalTrials.gov". 24 January 2007.
  6. ^"Eli Lilly and Company » Research Pipeline".
  7. ^Monti JM, Jantos H (September 2006). "Effects of activation and blockade of 5-HT2A/2C receptors in the dorsal raphe nucleus on sleep and waking in the rat".Progress in Neuro-psychopharmacology & Biological Psychiatry.30 (7):1189–95.doi:10.1016/j.pnpbp.2006.02.013.PMID 16713054.S2CID 12837755.
  8. ^Monti JM, Jantos H (December 2006). "Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat".European Journal of Pharmacology.553 (1–3):163–70.doi:10.1016/j.ejphar.2006.09.027.PMID 17059817.
  9. ^Patel JG, Bartoszyk GD, Edwards E, Ashby CR (April 2004). "The highly selective 5-hydroxytryptamine (5-HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test".Synapse.52 (1):73–5.doi:10.1002/syn.10308.PMID 14755634.S2CID 21941333.
  10. ^Adamec R, Creamer K, Bartoszyk GD, Burton P (November 2004). "Prophylactic and therapeutic effects of acute systemic injections of EMD 281014, a selective serotonin 2A receptor antagonist on anxiety induced by predator stress in rats".European Journal of Pharmacology.504 (1–2):79–96.doi:10.1016/j.ejphar.2004.09.017.PMID 15507224.
  11. ^Terry AV, Buccafusco JJ, Bartoszyk GD (June 2005). "Selective serotonin 5-HT2A receptor antagonist EMD 281014 improves delayed matching performance in young and aged rhesus monkeys".Psychopharmacology.179 (4):725–32.doi:10.1007/s00213-004-2114-1.PMID 15619109.S2CID 30366683.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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