| 词条 | Bicifadine |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 462798006 | IUPAC_name = 1-(4-Methylphenyl)-3-azabicyclo[3.1.0]hexane | image = Bicifadine.svg | width = 170 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Unscheduled | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | elimination_half-life = 1.6 hours | excretion = renal | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 71195-57-8 | ATC_prefix = none | ATC_suffix = | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 511099 | PubChem = 47953 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = B0SV3N7J3H | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 9889978 | smiles = c1cc(ccc1C)[C@]32CNC[C@@H]2C3 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C12H15N/c1-9-2-4-10(5-3-9)12-6-11(12)7-13-8-12/h2-5,11,13H,6-8H2,1H3/t11-,12+/m0/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = OFYVIGTWSQPCLF-NWDGAFQWSA-N | C=12 | H=15 | N=1 | molecular_weight = 173.25 g/mol | melting_point = | melting_high = }}Bicifadine (DOV-220,075) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) discovered at American Cyanamid as an analgesic drug candidate, and licensed to DOV Pharmaceutical in 1998 after American Cyanamid was acquired by Wyeth.[1][2][3] In January 2007, Dov licensed the rights to bicifadine to XTL Biopharmaceuticals after bicifadine failed in a Phase III clinical trial for chronic lower back pain.[4][5][6] XTL ran a PhaseIIb clinical trial for pain caused by diabetic neuropathy, which failed in 2008;[7] XTL terminated the agreement in 2010.[8] In 2010 Dov was acquired by Euthymics Bioscience which intended to continue development of other candidates from Dov's portfolio.[9] Bicifadine has a non-opioid, non-NSAID mechanism for the treatment of pain, which should have less abuse potential than opioid drugs and less propensity to cause gastric ulcers than NSAID drugs.[10] While the drug is purported to be a serotonin (SERT) and noradrenaline transporter (NET) inhibitor, it also has effects at the dopamine transporter (DAT), effectively making it a broad-spectrum monoamine transporter inhibitor or "triple reuptake inhibitor."[11] See also
References1. ^Marks DM, Pae CU, Patkar AA. Triple reuptake inhibitors: a premise and promise. Psychiatry Investig. 2008 Sep;5(3):142-7. {{PMID|20046357}} {{PMC|2796030}} {{Analgesics}}{{Antidepressants}}{{Monoamine reuptake inhibitors}}2. ^[https://www.sec.gov/Archives/edgar/data/1066833/000114420404018172/v08017_ex10-51.txt SEC Filing: Wyeth-DOV Restated License Agreement] Page accessed July 15, 2015] 3. ^Neubauer, DN. "Indiplon". pp 453-464 in GABA and Sleep: Molecular, Functional and Clinical Aspects. Eds Jaime M. Monti, Seithikurippu Ratnas Pandi-Perumal, Hanns Möhler. Springer Science & Business Media, 2010 {{ISBN|9783034602266}} 4. ^BioCentury, July 26, 2010 {{full citation needed|date=July 2017}} 5. ^{{cite web | url = http://euthymics.com/wp-content/uploads/2011/12/EUTHYMICS_BIOSCIENCE_ECP_BERNSTEIN_REPORT_120511bc1.pdf | title = Euthymics: Balancing act | page = A13 | publisher = BioCentury, The Bernstein Report on Biobusiness | date = December 5, 2011}} 6. ^John Caroll for Fierce Biotech. Jan 07, 2007 XTL licenses development rights to pain therapy 7. ^Fierce Biotech. December 9, 2008 Tiny XTL cuts costs, jobs 8. ^XTL Form 6-K March, 2013 9. ^Fierce Biotech July 22, 2010 Euthymics lands $24M to fund antidepressant work 10. ^{{Cite journal | last1 = Wang | first1 = R. I. | last2 = Johnson | first2 = R. P. | last3 = Lee | first3 = J. C. | last4 = Waite | first4 = E. M. | title = The Oral Analgesic Efficacy of Bicifadine Hydrochloride in Postoperative Pain | journal = Journal of Clinical Pharmacology | volume = 22 | issue = 4 | pages = 160–164 | year = 1982 | pmid = 7096604 | doi=10.1002/j.1552-4604.1982.tb02157.x}} 11. ^{{Cite journal| last1 = Basile | first1 = A.| last2 = Janowsky | first2 = A.| last3 = Golembiowska | first3 = K.| last4 = Kowalska | first4 = M.| last5 = Tam | first5 = E.| last6 = Benveniste | first6 = M.| last7 = Popik | first7 = P.| last8 = Nikiforuk | first8 = A.| last9 = Krawczyk | first9 = M.| last10 = Nowak | first10 = G.| last11 = Krieter | first11 = P. A.| last12 = Lippa | first12 = A. S.| last13 = Skolnick | first13 = P.| last14 = Koustova | first14 = E.| title = Characterization of the Antinociceptive Actions of Bicifadine in Models of Acute, Persistent, and Chronic Pain| journal = The Journal of Pharmacology and Experimental Therapeutics| volume = 321| issue = 3| pages = 1208–1225| year = 2007| pmid = 17325229| doi = 10.1124/jpet.106.116483}} 5 : Abandoned drugs|Analgesics|Cyclopropanes|Pyrrolidines|Serotonin-norepinephrine-dopamine reuptake inhibitors |
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