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Tiospiron Vidi još Reference Мени за навигацију87691-91-6557521015034835C6UMO5SRCHEMBL35057286914610.1021/jm00153a010288536710.1097/00004850-198704000-0000632949202574893Contemporary issues in the treatment of schizophrenia858201610.1248/cpb.43.2139776628710.1016/0893-133X(94)00064-7852498510.1007/BF0231118511561089109919831778640610.1007/s00210-007-0182-6„Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia”1570754010.1017/S1461145704005000ууууу

3-PPP4-PPBP5-MeO-DMTAlazocin (SKF-10047)AmantadinANAVEX2-73ArketaminBD-737BD-1052KaptodiamCitalopramCGRPKloperastinKokainKutamezin (SA-4503)CiklazocinDehidroepiandrosteron (DHEA)prasteronDehidroepiandrosteron sulfat (DHEA-S)prasteron sulfatDekstralorfanDekstrometorfan (DXM)Dekstrorfan (DXO)DimemorfanDimetiltriptamin (DMT)Ditolilgvanidin (DTG)DonepezilEliprodilEscitalopramFabomotizol (afobazol)FluoksetinFluvoksaminIfenprodilIgmesin (JO-1784)IPABKetaminL-687384MDMA (midomafetamin)MemantinMetamfetaminMetoksetaminMetilfenidatNepinalonNeuropeptid YNoskapinOPC-14523OpipramolPentazocinPentoksiverin (karbetapentan)PRE-084PregnenolonPregnenolon sulfatPridopidinRacemetorfan (metorfan)Racemorfan (morfanol)UMB-23UMB-823-PPPAC-927BD-1008BD-1031BD-1047BD-1060BD-1063BD-1067BMY-14802 (BMS-181100)CM-156Dup-734E-5842E-52862 (S1RA)HaloperidolLR-132LR-172MS-377NE-100NPC-16377Panamesin (EMD-57455)PD-144418PentazocinProgesteronRimkazol (BW-234U)SertralinSR-31742AFenitoinMetilfenilpiracetamSOMCL-6683-Metoksidekstralorfan3-MeO-PCP4C-T-24-IBP4-IPBS4-MeO-PCP5-MeO-DALT5-MeO-DiPTAmitriptilinAzidopamilHlorpromazinKlemastinKlomipraminKlorgilinD-DeprenilDiPTDPTIbogainImipraminKCR-12-83.1NemonapridNoribogainRHL-033RS-67,333RTI-55ŠafranSafinamidSelegilinSpipetijanTrifluoperazinW-18YKP10ABerberinEtilketazocinForfitMetafitNalbufinNaluzotanTapentadolTenociklidinAHD1AZ66LamotriginNaloksonSM-21UMB-100UMB-101UMB-103UMB-116YZ-011YZ-069YZ-185SKF-8395918-MetoksikoronaridinBMY-13980ButaklamolKaramifenKarvotrolinHlorfenamin (hlorfeniramin)HlorpromazinCinarizinCinuperonKlocapraminDezocinEMD-59983HipericinkantarionFlufenazinGevotrolin (WY-47384)Mepiramin (pirilamin)MolindonPerfenazinPimozidProadifenPrometazinPropranololHinidinRemoksipridSL 82.0715SR-31747ATiospiron (BMY-13859)Venlafaksin


АнтипсихотициАзапирониБензотиазолиПиперазини


atipični antipsihotikazapironskešizofreniju1980-tihtipičnih antipsihotikaekstrapiramidalnenuspojavePerospironpotentnijiselektivnijiparcijalni agonist5-HT1A receptorainverzni agonist5-HT2A5-HT2C5-HT7 receptoraantagonistD2D4α1-adrenergičkog receptoraAzaperonBenperidolBromperidolDroperidolFluanizonHaloperidolLenperonMoperonPipamperonSpiperonTimiperonTrifluperidolKlopimozidFluspirilenPenfluridolPimozidAcepromazinAcetofenazinButaperazinKarfenazinHloracizinHlorproetazinHlorpromazinCijamemazinDiksirazinFluacizinFlufenazinLevomepromazin/MetotrimeprazinMezoridazinPerazinPericijazinPerfenazinPiperacetazinPipotiazinProhlorperazinPromazinPrometazinPropiomazinSulforidazinTietilperazinTiopropazatTioproperazinTioridazinTrifluoperazinTriflupromazinHlorprotiksenKlopentiksolFlupentiksolTiotiksenZuklopentiksolButaklamolFluotracenLoksapinTrimipraminCinuperonMelperonSetoperonIloperidonOkaperidonPaliperidonRisperidonLurasidonePerospironRevospironTiospironZiprasidonAmperozidAripiprazolBifeprunoksBrekspiprazolElopiprazolUmespironAmoksapinAsenapinKarpipraminKlocapraminKlorotepinKlotiapinKlozapinFluperlapinGevotrolinMetitepinMosapraminNDMCOlanzapinPihindonKvetijapinTenilapinZotepinWHO-EMPovučeniKlinička ispitivanjaFaza IIINije dospeo do faze IIIMPSOPSImeprdsrdodbpasspecspvoprocN5A5B5C6A6B6D










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Tiospiron




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Tiospiron
Tiospirone.png

IUPAC ime
8-[4-[4-(1,2-benzotiazol-3-il)piperazin-1-il]butil]-8-azaspiro[4.5]dekan-7,9-dion

Farmakokinetički podaci
MetabolizamHepatic
Poluvreme eliminacije1,4 sata
IzlučivanjeUrine

Identifikatori
CAS broj
87691-91-6 ДаY
ATC kodnone
PubChemCID 55752
IUPHAR/BPS101
ChemSpider50348
UNII
35C6UMO5SR ДаY
ChEMBLCHEMBL35057
Hemijski podaci
Formula
C24H32N4O2S
Molarna masa440,60 g/mol

Tiospiron (BMY-13,859, tiaspiron, tiosperon) je atipični antipsihotik iz azapironske klase.[1] On je istraživan kao tretman za šizofreniju tokom kasnih 1980-tih i poznato je da je efektivan ekvivalent tipičnih antipsihotika i da ne izaziva ekstrapiramidalne nuspojave.[2][3][4][5] Međutim, njegov razvoj je zaustavljen. Perospiron, jedan drugi derivat azapirona sa antipsihotičkim svojstvima, je sintetisan i karakterisan nekoliko godina kasnije.[6] Za njega je utvrđeno da je potentniji i selektivniji od tiospirona te je plasiran na tržište.[6]


Tiospiron deluje kao parcijalni agonist 5-HT1A receptora, inverzni agonist 5-HT2A, 5-HT2C, i 5-HT7 receptora, i antagonist D2, D4, i α1-adrenergičkog receptora.[7][8][9][10][11][12]



Vidi još


  • Azapiron


Reference




  1. ^ Yevich JP; New JS; Smith DW; et al. (1986). „Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents”. Journal of Medicinal Chemistry. 29 (3): 359—69. PMID 2869146. doi:10.1021/jm00153a010. 


  2. ^ Jain AK, Kelwala S, Moore N, Gershon S (1987). „A controlled clinical trial of tiaspirone in schizophrenia”. International Clinical Psychopharmacology. 2 (2): 129—33. PMID 2885367. doi:10.1097/00004850-198704000-00006. 


  3. ^ Moore NC, Meyendorff E, Yeragani V, LeWitt PA, Gershon S (1987). „Tiaspirone in schizophrenia”. Journal of Clinical Psychopharmacology. 7 (2): 98—101. PMID 3294920. 


  4. ^ Borison RL, Sinha D, Haverstock S, McLarnon MC, Diamond BI (1989). „Efficacy and safety of tiospirone vs. haloperidol and thioridazine in a double-blind, placebo-controlled trial”. Psychopharmacology Bulletin. 25 (2): 190—3. PMID 2574893. 


  5. ^ Nasrallah, Henry A.; Shriqui, Christian L (1995). Contemporary issues in the treatment of schizophrenia. Washington, DC: American Psychiatric Press. str. 313 [/863]. ISBN 0-88048-681-3. 


  6. ↑ 6,06,1 Ishizumi K, Kojima A, Antoku F, Saji I, Yoshigi M (1995). „Succinimide derivatives. II. Synthesis and antipsychotic activity of N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis- cyclohexanedicarboximide (SM-9018) and related compounds”. Chemical & Pharmaceutical Bulletin. 43 (12): 2139—51. PMID 8582016. doi:10.1248/cpb.43.2139. 


  7. ^ Sumiyoshi T; Suzuki K; Sakamoto H; et al. (1995). „Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy”. Neuropsychopharmacology. 12 (1): 57—64. PMID 7766287. doi:10.1016/0893-133X(94)00064-7. 


  8. ^ Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY (1995). „D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs”. Psychopharmacology. 120 (3): 365—8. PMID 8524985. doi:10.1007/BF02311185. 


  9. ^ Weiner DM; Burstein ES; Nash N; et al. (2001). „5-hydroxytryptamine2A receptor inverse agonists as antipsychotics”. The Journal of Pharmacology and Experimental Therapeutics. 299 (1): 268—76. PMID 11561089. 


  10. ^ Herrick-Davis K, Grinde E, Teitler M (2000). „Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors”. The Journal of Pharmacology and Experimental Therapeutics. 295 (1): 226—32. PMID 10991983. 


  11. ^ Rauly-Lestienne I, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Cussac D (2007). „Differential profile of typical, atypical and third generation antipsychotics at human 5-HT7a receptors coupled to adenylyl cyclase: detection of agonist and inverse agonist properties”. Naunyn-Schmiedeberg's Archives of Pharmacology. 376 (1–2): 93—105. PMID 17786406. doi:10.1007/s00210-007-0182-6. ISBN. 


  12. ^ Newman-Tancredi A, Assié MB, Leduc N, Ormière AM, Danty N, Cosi C (2005). „Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia”. The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP). 8 (3): 341—56. PMID 15707540. doi:10.1017/S1461145704005000. 




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19. јануар Садржај Догађаји Рођења Смрти Празници и дани сећања Види још Референце Мени за навигацијуу

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Israel Cuprins Etimologie | Istorie | Geografie | Politică | Demografie | Educație | Economie | Cultură | Note explicative | Note bibliografice | Bibliografie | Legături externe | Meniu de navigaresite web oficialfacebooktweeterGoogle+Instagramcanal YouTubeInstagramtextmodificaremodificarewww.technion.ac.ilnew.huji.ac.ilwww.weizmann.ac.ilwww1.biu.ac.ilenglish.tau.ac.ilwww.haifa.ac.ilin.bgu.ac.ilwww.openu.ac.ilwww.ariel.ac.ilCIA FactbookHarta Israelului"Negotiating Jerusalem," Palestine–Israel JournalThe Schizoid Nature of Modern Hebrew: A Slavic Language in Search of a Semitic Past„Arabic in Israel: an official language and a cultural bridge”„Latest Population Statistics for Israel”„Israel Population”„Tables”„Report for Selected Countries and Subjects”Human Development Report 2016: Human Development for Everyone„Distribution of family income - Gini index”The World FactbookJerusalem Law„Israel”„Israel”„Zionist Leaders: David Ben-Gurion 1886–1973”„The status of Jerusalem”„Analysis: Kadima's big plans”„Israel's Hard-Learned Lessons”„The Legacy of Undefined Borders, Tel Aviv Notes No. 40, 5 iunie 2002”„Israel Journal: A Land Without Borders”„Population”„Israel closes decade with population of 7.5 million”Time Series-DataBank„Selected Statistics on Jerusalem Day 2007 (Hebrew)”Golan belongs to Syria, Druze protestGlobal Survey 2006: Middle East Progress Amid Global Gains in FreedomWHO: Life expectancy in Israel among highest in the worldInternational Monetary Fund, World Economic Outlook Database, April 2011: Nominal GDP list of countries. 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Mentenanță CS1: Dată și anMentenanță CS1: Utilizare explicită a lui et al.IsraelȚări în Orientul MijlociuRepubliciSionismState membre ale Organizației Națiunilor Unite ebraicăarabărepublică parlamentarăOrientul MijlociuMării MediteraneLibanulSiriaIordaniaCisiordaniaEgiptFâșia GazaIerusalimTel AvivOrganizației Națiunilor Unite14 mai1948Mandatului britanic pentru PalestinaDavid Ben-GurionOrganizației SionisteAgenției Evreiești pentru PalestinaStatului IsraelONULiga ArabăpalestinieneRăzboiul arabo-israelian din 1948Conflict arabo-israelianTransiordaniaEgiptulRăzboiului de Șase ZileCisiordaniaPeninsula SinaiFâșia GazaÎnălțimile GolanBiroului Central de Statisticădruzicerchezisamariteniarmenidemocrație reprezentativăsistem parlamentarvot universalKnessetulgaze naturaleIndicelui Dezvoltării UmaneOCDEȚara I...
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Кастелфранко ди Сопра Становништво Референце Спољашње везе Мени за навигацију43°37′18″ СГШ; 11°33′32″ ИГД / 43.62156° СГШ; 11.55885° ИГД / 43.62156; 11.5588543°37′18″ СГШ; 11°33′32″ ИГД / 43.62156° СГШ; 11.55885° ИГД / 43.62156; 11.558853179688„The GeoNames geographical database”„Istituto Nazionale di Statistica”проширитиууWorldCat156923403n850174324558639-1cb14643287r(подаци)

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