| 词条 | Pruvanserin |
| 释义 |
| IUPAC_name = 7-({4-[2-(4-fluorophenyl)ethyl]piperazin-1-yl}carbonyl)-1H-indole-3-carbonitrile | image = Pruvanserin.png | tradename = | pregnancy_category = | legal_status = Uncontrolled | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 443144-26-1 | CAS_supplemental = 443144-27-2 (hydrochloride) | ATC_prefix = none | ATC_suffix = | PubChem = 6433122 | ChemSpiderID = 4938310 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = UL09X1D9EM | ChEMBL = 1215661 | C=22 | H=21 | F=1 | N=4 | O=1 | molecular_weight = 376.43 g/mol | smiles = N#Cc2c1cccc(c1[nH]c2)C(=O)N4CCN(CCc3ccc(F)cc3)CC4 }}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
References1. ^{{cite journal |vauthors=Bartoszyk GD, van Amsterdam C, Böttcher H, Seyfried CA | title = EMD 281014, a new selective serotonin 5-HT2A receptor antagonist | journal = European Journal of Pharmacology | volume = 473 | issue = 2–3 | pages = 229–30 |date=July 2003 | pmid = 12892843 | doi = 10.1016/S0014-2999(03)01992-7| url = http://linkinghub.elsevier.com/retrieve/pii/S0014299903019927}} {{Hypnotics}}{{Serotonergics}}2. ^{{cite journal |vauthors=Teegarden BR, Al Shamma H, Xiong Y | title = 5-HT(2A) inverse-agonists for the treatment of insomnia | journal = Current Topics in Medicinal Chemistry | volume = 8 | issue = 11 | pages = 969–76 | year = 2008 | pmid = 18673166 | doi = 10.2174/156802608784936700| url = }} 3. ^{{cite web | url = http://clinicaltrials.gov/ct2/show/NCT00259311 | title = Efficacy Study of LY2422347 to Treat Insomnia - Full Text View - ClinicalTrials.gov | format = | work = | accessdate = }} 4. ^{{cite web | url = http://www.lilly.com/research/pipeline/ | title = Eli Lilly and Company » Research Pipeline | format = | work = | accessdate = }} 5. ^{{cite journal |vauthors=Monti JM, Jantos H | title = Effects of activation and blockade of 5-HT2A/2C receptors in the dorsal raphe nucleus on sleep and waking in the rat | journal = Progress in Neuro-psychopharmacology & Biological Psychiatry | volume = 30 | issue = 7 | pages = 1189–95 |date=September 2006 | pmid = 16713054 | doi = 10.1016/j.pnpbp.2006.02.013 | url = http://linkinghub.elsevier.com/retrieve/pii/S0278-5846(06)00072-8}} 6. ^{{cite journal |vauthors=Monti JM, Jantos H | title = 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 | journal = European Journal of Pharmacology | volume = 553 | issue = 1–3 | pages = 163–70 |date=December 2006 | pmid = 17059817 | doi = 10.1016/j.ejphar.2006.09.027 | url = http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(06)01054-5}} 7. ^{{cite journal |vauthors=Patel JG, Bartoszyk GD, Edwards E, Ashby CR | title = 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 | journal = Synapse | volume = 52 | issue = 1 | pages = 73–5 |date=April 2004 | pmid = 14755634 | doi = 10.1002/syn.10308}} 8. ^{{cite journal |vauthors=Adamec R, Creamer K, Bartoszyk GD, Burton P | title = 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 | journal = European Journal of Pharmacology | volume = 504 | issue = 1–2 | pages = 79–96 |date=November 2004 | pmid = 15507224 | doi = 10.1016/j.ejphar.2004.09.017 | url = http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(04)01039-8}} 9. ^{{cite journal |vauthors=Terry AV, Buccafusco JJ, Bartoszyk GD | title = Selective serotonin 5-HT2A receptor antagonist EMD 281014 improves delayed matching performance in young and aged rhesus monkeys | journal = Psychopharmacology | volume = 179 | issue = 4 | pages = 725–32 |date=June 2005 | pmid = 15619109 | doi = 10.1007/s00213-004-2114-1}} 6 : 5-HT2A antagonists|Eli Lilly and Company|Indoles|Nitriles|Piperazines|Carboxamides |
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