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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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Is there any way to stop a user from creating executables and running them? What is this "Table of astronomy" about? How far did Gandalf and the Balrog drop from the bridge in Moria? Can "être sur" mean "to be about" ? Is there a Morita cocycle for the mapping class group Mod(g,n) when n > 1? Why isn’t SHA-3 in wider use? AsyncDictionary - Can you break thread safety? What is this 1990s horror game of otherworldly PCs dealing with monsters on modern Earth? On the Rømer experiments and the speed of light visible indication that a cell is not evaluatable Is 悪いところを見つかった proper Japanese? Is this n-speak? Can sampling rate be a floating point number? Creating multi-attribute primary key in table in ArcGIS Desktop TEMPO: play a sound in animated GIF/PDF/SVG Can a PC use the Levitate spell to avoid movement speed reduction from exhaustion? How much maintenance time did it take to make an F4U Corsair ready for another flight? I
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Кампала Садржај Географија Географија Историја Становништво Привреда Партнерски градови Референце Спољашње везе Мени за навигацију0°11′ СГШ; 32°20′ ИГД / 0.18° СГШ; 32.34° ИГД / 0.18; 32.340°11′ СГШ; 32°20′ ИГД / 0.18° СГШ; 32.34° ИГД / 0.18; 32.34МедијиПодациЗванични веб-сајту

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Главни градови у АфрициГрадови у Уганди енгл.Уганде1890ЕнтебеТанзанијом19781979Иди АминВикторијиног језера (function()var node=document.getElementById("mw-dismissablenotice-anonplace");if(node)node.outerHTML="u003Cdiv class="mw-dismissable-notice"u003Eu003Cdiv class="mw-dismissable-notice-close"u003E[u003Ca tabindex="0" role="button"u003Eсакријu003C/au003E]u003C/divu003Eu003Cdiv class="mw-dismissable-notice-body"u003Eu003Cdiv id="localNotice" lang="sr" dir="ltr"u003Eu003Cdiv style="position:relative; overflow:hidden; background-color:#5E9DC8; text-align:center; color:white; font-size:1.25em; font-weight:bold; line-height:1.5em; margin-top: 5px;"u003Eu003Cuu003Eu003Ca href="/wiki/%D0%92%D0%B8%D0%BA%D0%B8%D0%BF%D0%B5%D0%B4%D0%B8%D1%98%D0%B0:%D0%A2%D0%B0%D0%BA%D0%BC%D0%B8%D1%87%D0%B5%D1%9A%D0%B5_%D1%83_%D0%BF%D0%B8%D1%81%D0%B0%D1%9A%D1%83_%D1%87%D0%BB%D0%B0%D0%BD%D0%B0%D0%BA
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19. јануар Садржај Догађаји Рођења Смрти Празници и дани сећања Види још Референце Мени за навигацијуу

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1.2.3.4.5.6.7.8.9.10.11.12.13.14.15.16.17.18.19.20.21.22.23.24.25.26.27.28.29.30.31.1.2.3.4.5.6.7.8.9.10.11.12.13.14.15.16.17.18.19.20.21.22.23.24.25.26.27.28.29.30.31.1.2.3.4.5.6.7.8.9.10.11.12.13.14.15.16.17.18.19.20.21.22.23.24.25.26.27.28.29.30.31.1.2.3.4.5.6.7.8.9.10.11.12.13.14.15.16.17.18.19.20.21.22.23.24.25.26.27.28.29.30.31.1.2.3.4.5.6.7.8.9.10.11.12.13.14.15.16.17.18.19.20.21.22.23.24.25.26.27.28.29.30.1.2.3.4.5.6.7.8.9.10.11.12.13.14.15.16.17.18.19.20.21.22.23.24.25.26.27.28.29.30. ЈануарДани деветнаестиГрегоријанском календарупреступним годинама (function()var node=document.getElementById("mw-dismissablenotice-anonplace");if(node)node.outerHTML="u003Cdiv class="mw-dismissable-notice"u003Eu003Cdiv class="mw-dismissable-notice-close"u003E[u003Ca tabindex="0" role="button"u003Eсакријu003C/au003E]u003C/divu003Eu003Cdiv class="mw-dismissable-notice-body"u003Eu003Cdiv id="localNotice" lang="sr&
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