SB-271,046
IUPAC ime | |
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5-hloro-N-(4-metoksi-3-piperazin-1-ilfenil)-3-metil-1-benzotiofen-2-sulfonamid | |
Identifikatori | |
ATC kod | none |
PubChem | CID 5312149 |
IUPHAR/BPS | 276 |
ChEMBL | CHEMBL431298 Y |
Hemijski podaci | |
Formula | C20H22ClN3O3S2 |
Molarna masa | 451,989 g/mol |
SMILES
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SB-271,046 je lek koji se koristi u naučnim istraživanjima. On je bio jedan od prvih selektivnih antagonista 5-HT6 receptora.[1] SB-271,046 je potentan i selektivan in vitro i dobrom oralnom biodostupnošću in vivo, ali ima slabu penetraciju kroz krvno moždanu barijeru, te su razvijeni poboljšani 5-HT6 antagonisti kao što su SB-357,134 i SB-399,885.[2]
SB-271,046 povišava nivoe ekscitatornih aminokiselinskih neurotransmitera glutamata i aspartata,[3] kao i dopamina i noradrenalina[4] u frontalnom korteksu i hipokampusu pacova.[5] Pokazano je da 5-HT6 antagonisti proizvode nootropne efekte u brojnim studijama na životinjama.[6][7][8] Smatrase da ovaj lekovi ove klase mogu da nađu primenu u tretmanu šizofrenije i drugih psihijatrijskih poremećaja.[9][10][11][12]
Reference
- ^ Bromidge, SM; Brown, AM; Clarke, SE; Dodgson, K; Gager, T; Grassam, HL; Jeffrey, PM; Joiner, GF; King, FD (1999). „5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist”. Journal of Medical Chemistry. 42 (2): 202—5. PMID 9925723. doi:10.1021/jm980532e.
- ^ Ahmed, M; Briggs, MA; Bromidge, SM; Buck, T; Campbell, L; Deeks, NJ; Garner, A; Gordon, L; Hamprecht, DW (2005). „Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists”. Bioorganic & Medicinal Chemistry Letters. 15 (21): 4867—71. PMID 16143522. doi:10.1016/j.bmcl.2005.06.107.
- ^ Dawson, LA; Nguyen, HQ; Li, P (2000). „In vivo effects of the 5-HT6 antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartate”. British Journal of Pharmacology. 130 (1): 23—6. PMC 1572041 . PMID 10780993. doi:10.1038/sj.bjp.0703288.
- ^ Lacroix, LP; Dawson, LA; Hagan, JJ; Heidbreder, CA (2004). „5-HT6 receptor antagonist SB-271046 enhances extracellular levels of monoamines in the rat medial prefrontal cortex”. Synapse. 51 (2): 158—64. PMID 14618683. S2CID 6539467. doi:10.1002/syn.10288.
- ^ Dawson, LA; Nguyen, HQ; Li, P (2001). „The 5-HT(6) receptor antagonist SB-271046 selectively enhances excitatory neurotransmission in the rat frontal cortex and hippocampus”. Neuropsychopharmacology. 25 (5): 662—8. PMID 11682249. S2CID 25358343. doi:10.1016/S0893-133X(01)00265-2.
- ^ Rogers, DC; Hagan, JJ (2001). „5-HT6 receptor antagonists enhance retention of a water maze task in the rat”. Psychopharmacology. 158 (2): 114—9. PMID 11702084. S2CID 29472459. doi:10.1007/s002130100840.
- ^ Foley, AG; Murphy, KJ; Hirst, WD; Gallagher, HC; Hagan, JJ; Upton, N; Walsh, FS; Regan, CM (2004). „The 5-HT(6) receptor antagonist SB-271046 reverses scopolamine-disrupted consolidation of a passive avoidance task and ameliorates spatial task deficits in aged rats”. Neuropsychopharmacology. 29 (1): 93—100. PMID 14571256. S2CID 21898284. doi:10.1038/sj.npp.1300332.
- ^ Marcos, B; Chuang, TT; Gil-Bea, FJ; Ramirez, MJ (2008). „Effects of 5-HT6 receptor antagonism and cholinesterase inhibition in models of cognitive impairment in the rat”. British Journal of Pharmacology. 155 (3): 434—40. PMC 2567877 . PMID 18622410. doi:10.1038/bjp.2008.281.
- ^ Minabe, Y; Shirayama, Y; Hashimoto, K; Routledge, C; Hagan, JJ; Ashby Jr, CR (2004). „Effect of the acute and chronic administration of the selective 5-HT6 receptor antagonist SB-271046 on the activity of midbrain dopamine neurons in rats: an in vivo electrophysiological study”. Synapse. 52 (1): 20—8. PMID 14755629. S2CID 25687099. doi:10.1002/syn.20002.
- ^ De Foubert, G; O'Neill, MJ; Zetterström, TS (2007). „Acute onset by 5-HT(6)-receptor activation on rat brain brain-derived neurotrophic factor and activity-regulated cytoskeletal-associated protein mRNA expression”. Neuroscience. 147 (3): 778—85. PMID 17560041. S2CID 37184427. doi:10.1016/j.neuroscience.2007.04.045.
- ^ Marcos, B; Aisa, B; Ramírez, MJ (2008). „Functional interaction between 5-HT(6) receptors and hypothalamic-pituitary-adrenal axis: cognitive implications”. Neuropharmacology. 54 (4): 708—14. PMID 18206183. S2CID 21417069. doi:10.1016/j.neuropharm.2007.11.019.
- ^ Loiseau, F; Dekeyne, A; Millan, MJ (2008). „Pro-cognitive effects of 5-HT6 receptor antagonists in the social recognition procedure in rats: implication of the frontal cortex”. Psychopharmacology. 196 (1): 93—104. PMID 17922111. S2CID 35795618. doi:10.1007/s00213-007-0934-5.
Spoljašnje veze
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Лиганди 5-HT2 рецептора | |||||||
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Лиганди 5-HT3, 5-HT4, 5-HT5, 5-HT6, и 5-HT7 рецептора | |||||||||||
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Аминоиндани: 5-IAI • AMMI • ETAI • MDAI • MDMAI • MMAI • TAI; Aminotetralini: 6-CAT • 8-OH-DPAT • MDAT • MDMAT; Оксазолини: 4-Metilaminoreks • Аминорекс • Кломинорекс • Флуминорекс; Фенетиламини (такође Амфетамини, Катинони, Фентермини, итд): 2-Метил-МДА • 4-CAB • 4-FA • 4-FMA • 4-HA • 4-MTA • 5-APDB • 5-Метил-МДА • 6-APDB • 6-Метил-МДА • AEMMA • Амифламин • BDB • BOH • Брефедрон • Бутилон • Хлорфентермин • Клофорекс • Амфепрамон • Метамфепрамон • DFMDA • DMA • DMMA • EBDB • EDMA • Етилон • Етолорекс • Фенфлурамин (Дексфенфлурамин) • Флефедрон • IAP • IMP • Лофофин • MBDB • MDA • MDEA • MDHMA • MDMA • MDMPEA • MDOH • MDPEA • Мефедрон • Метедрон • Метилон • MMA • MMDA • MMDMA • MMMA • NAP • Norfenfluramin • 4-TFMA • pBA • pCA • pIA • PMA • PMEA • PMMA • TAP; Piperazini: 2C-B-BZP • 2-BZP • 3-MeOPP • BZP • DCPP • MBZP • mCPP • MDBZP • MeOPP • Mepiprazol • pCPP • pFPP • pTFMPP • TFMPP; Триптамини: 4-Метил-αET • 4-Metil-αMT • 5-CT • 5-MeO-αET • 5-MeO-αMT • 5-MT • αET • αMT • DMT • Триптамин (sam); Други: Инделоксазин • Трамадол • Виqуалин |
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