Pruvanserin
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Pruvanserin
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|---|---|
| Systematic (IUPAC) name | |
| 7-({4-[2-(4-fluorophenyl)ethyl]piperazin-1-yl}carbonyl)-1H-indole-3-carbonitrile | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Uncontrolled |
| Routes | Oral |
| Identifiers | |
| CAS number | 443144-26-1 443144-27-2 (hydrochloride) |
| ATC code | None |
| PubChem | CID 6433122 |
| ChemSpider | 4938310 |
| UNII | UL09X1D9EM  |
| ChEMBL | CHEMBL1215661 |
| Chemical data | |
| Formula | C22H21FN4O |
| Mol. mass | 376.43 g/mol |
| SMILES | eMolecules & PubChem |
Pruvanserin (EMD-281,014, LY-2,422,347) is a selective 5-HT2A receptor antagonist which was under development by Eli Lilly and Company for the treatment of insomnia.[1][2] It was in phase II clinical trials in 2008 but appears to have been discontinued as it is no longer in the company's development pipeline.[3][4] In addition to its sleep-improving properties,[5][6] pruvanserin has also been shown to have antidepressant, anxiolytic, and working memory-enhancing effects in animal studies.[7][8][9]
See also
References
- ^ 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. http://linkinghub.elsevier.com/retrieve/pii/S0014299903019927.
- ^ 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.
- ^ "Efficacy Study of LY2422347 to Treat Insomnia - Full Text View - ClinicalTrials.gov". http://clinicaltrials.gov/ct2/show/NCT00259311.
- ^ "Eli Lilly and Company » Research Pipeline". http://www.lilly.com/research/pipeline/.
- ^ 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. http://linkinghub.elsevier.com/retrieve/pii/S0278-5846(06)00072-8.
- ^ 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. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(06)01054-5.
- ^ 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.
- ^ 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. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(04)01039-8.
- ^ 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. ISBN [[Special:BookSources/0021300421141|0021300421141]]. PMID 15619109.
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