| 词条 | Naluzotan |
| 释义 |
| verifiedrevid = 444039968 | IUPAC_name = N-(3- | image = PRX-00023_structure.png | width = 250px | tradename = | pregnancy_category = | legal_status = | routes_of_administration = Oral[1] | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 740873-06-7 | ATC_prefix = None | ATC_suffix = | PubChem = 11430856 | ChemSpiderID = 9605731 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = LQ54E5B4EW | C = 23 | H = 38 | N = 4 | O = 3 | S = 1 | molecular_weight = 450.638 g/mol | smiles = O=C(Nc3cccc(N2CCN(CCCCNS(=O)(=O)CC1CCCCC1)CC2)c3)C | StdInChI = 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) | StdInChIKey = SPWZXWDPAWDKQE-UHFFFAOYSA-N }}Naluzotan (INN, USAN; PRX-00023) is a serotonergic drug of the phenylpiperazine class that was under investigation by EPIX Pharmaceuticals Inc for the treatment of generalized anxiety disorder and major depressive disorder.[1][2] It acts as a selective and potent 5-HT1A receptor partial agonist,[2][3] readily stimulating prolactin responses,[4] though it has also been found to bind to and activate the σ receptor.[5] Naluzotan was well tolerated in clinical trials,[4] with more patients in the control group dropping out due to adverse effects than in the active group in one study.[2] The most frequently reported side effect was headache in 15% of patients (compared to 10% for placebo).[2] In addition, naluzotan demonstrated significant antidepressant and anxiolytic effects as per the HAM-D and MADRS and the HAM-A, respectively, in some trials,[2] but in others it did not.[6][7] In the end it was not found to be significantly superior enough to placebo and development was stopped.[7] See also
References1. ^1 {{cite journal | vauthors = de Paulis T | title = Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression. | journal = Curr Opin Investig Drugs | volume = 8 | issue = 1 | pages = 78–86 | year = 2007 | pmid = 17263189 }} {{Serotonin receptor modulators}}{{Sigma receptor modulators}}{{Piperazines}}{{nervous-system-drug-stub}}2. ^1 2 3 4 {{cite journal | vauthors = Rickels K, Mathew S, Banov MD, Zimbroff DL, Oshana S, Parsons EC, Donahue SR, Kauffman M, Iyer GR, Reinhard JF | title = 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 | journal = J Clin Psychopharmacol | volume = 28 | issue = 2 | pages = 235–239 | year = 2008 | pmid = 18344738 | doi = 10.1097/JCP.0b013e31816774de }} 3. ^{{cite journal | vauthors = 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 | title = 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 | journal = J Med Chem | volume = 49 | issue = 11 | pages = 3116–3135 | year = 2006 | pmid = 16722631 | doi = 10.1021/jm0508641 }} 4. ^1 {{cite journal | vauthors = Iyer GR, Reinhard JF, Oshana S, Kauffman M, Donahue S | title = Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects. | journal = J Clin Pharmacol | volume = 47 | issue = 7 | pages = 817–824 | year = 2007 | pmid = 17495280 | doi = 10.1177/0091270007300953 }} 5. ^{{cite book | author = Prof John Kelly | title = Principles of CNS Drug Development: From Test Tube to Patient | publisher = Wiley | location = New York | year = 2010 | pages = | isbn = 0-470-51979-7 | oclc = | doi = | url = https://books.google.com/books?id=pfY3xcsu6EsC&lpg=PA265&dq=adatanserin&pg=PA265#v=onepage&q=PRX-00023}} 6. ^{{cite journal | vauthors = Mathew SJ, Garakani A, Reinhard JF, Oshana S, Donahue S | title = Short-term tolerability of a nonazapirone selective serotonin 1A agonist in adults with generalized anxiety disorder: a 28-day, open-label study | journal = Clin. Ther. | volume = 30 | issue = 9 | pages = 1658–1666 | year = 2008 | pmid = 18840371 | doi = 10.1016/j.clinthera.2008.09.006 }} 7. ^1 {{cite journal | vauthors = Kirchhoff VD, Nguyen HT, Soczynska JK, Woldeyohannes H, McIntyre RS | title = Discontinued psychiatric drugs in 2008 | journal = Expert Opinion on Investigational Drugs | volume = 18 | issue = 10 | pages = 1431–43 | date = October 2009 | pmid = 19715445 | doi = 10.1517/13543780903184591 | url = http://informahealthcare.com/doi/abs/10.1517/13543780903184591 }} 4 : 5-HT1A agonists|Acetanilides|Piperazines|Sulfonamides |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。