SB-206,553

С Википедије, слободне енциклопедије
SB-206,553
IUPAC ime
5-metil-1-(3-piridilkarbamoil)-1,2,3,5-tetrahidropirolo[2,3-f]indol
Identifikatori
CAS broj158942-04-2 ДаY
ATC kodnone
PubChemCID 5163
Hemijski podaci
FormulaC17H16N4O
Molarna masa292,334 g/mol
  • Cn2ccc(c2c3)cc1c3CCN1C(=O)Nc4cccnc4

SB-206,553 je lek koji deluje kao mešoviti antagonist za 5-HT2B i 5-HT2C serotoninske receptore.[1][2][3] On ima anksiolitička svojstava u životinjskim studijama i formira interakcije sa nizom drugih lekova.[4][5][6][7][8][9][10][11][12] On takođe deluje kao pozitivni alosterni modulator α7 nikotinskih acetilholinskih receptora.[13]

Reference[уреди | уреди извор]

  1. ^ Forbes IT, Ham P, Booth DH, Martin RT, Thompson M, Baxter GS, Blackburn TP, Glen A, Kennett GA, Wood MD (1995). „5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrrolo[2,3-f]indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral activity”. Journal of Medicinal Chemistry. 38 (14): 2524—30. PMID 7629791. doi:10.1021/jm00014a004. 
  2. ^ Kennett GA, Wood MD, Bright F, Cilia J, Piper DC, Gager T, Thomas D, Baxter GS, Forbes IT, Ham P, Blackburn TP (1996). „In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties”. British Journal of Pharmacology. 117 (3): 427—434. PMC 1909304 Слободан приступ. PMID 8821530. 
  3. ^ Forbes IT, Dabbs S, Duckworth DM, Ham P, Jones GE, King FD, Saunders DV, Blaney FE, Naylor CB, Baxter GS, Blackburn TP, Kennett GA, Wood MD (1996). „Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists”. Journal of Medicinal Chemistry. 39 (25): 4966—77. PMID 8960557. doi:10.1021/jm960571v. 
  4. ^ Bromidge SM, Dabbs S, Davies DT, Duckworth DM, Forbes IT, Ham P, Jones GE, King FD, Saunders DV, Starr S, Thewlis KM, Wyman PA, Blaney FE, Naylor CB, Bailey F, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD (1998). „Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines”. Journal of Medicinal Chemistry. 41 (10): 1598—612. PMID 9572885. doi:10.1021/jm970741j. 
  5. ^ Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E (1998). „Selective blockade of serotonin2C/2B receptors enhances dopamine release in the rat nucleus accumbens”. Neuropharmacology. 37 (2): 265—72. PMID 9680252. doi:10.1016/S0028-3908(98)00014-8. 
  6. ^ McCreary AC, Cunningham KA (1999). „Effects of the 5-HT2C/2B antagonist SB 206553 on hyperactivity induced by cocaine”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 20 (6): 556—64. PMID 10327425. doi:10.1016/S0893-133X(98)00087-6. 
  7. ^ Di Giovanni G, De Deurwaerdére P, Di Mascio M, Di Matteo V, Esposito E, Spampinato U (1999). „Selective blockade of serotonin-2C/2B receptors enhances mesolimbic and mesostriatal dopaminergic function: a combined in vivo electrophysiological and microdialysis study”. Neuroscience. 91 (2): 587—97. PMID 10366016. doi:10.1016/S0306-4522(98)00655-1. 
  8. ^ Takahashi RN, Berton O, Mormède P, Chaouloff F (2001). „Strain-dependent effects of diazepam and the 5-HT2B/2C receptor antagonist SB 206553 in spontaneously hypertensive and Lewis rats tested in the elevated plus-maze”. Brazilian Journal of Medical and Biological Research. 34 (5): 675—82. PMID 11323756. 
  9. ^ Porras G, Di Matteo V, Fracasso C, Lucas G, De Deurwaerdère P, Caccia S, Esposito E, Spampinato U (2002). „5-HT2A and 5-HT2C/2B receptor subtypes modulate dopamine release induced in vivo by amphetamine and morphine in both the rat nucleus accumbens and striatum”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 26 (3): 311—24. PMID 11850146. doi:10.1016/S0893-133X(01)00333-5. 
  10. ^ Navailles S, De Deurwaerdère P, Porras G, Spampinato U (2004). „In vivo evidence that 5-HT2C receptor antagonist but not agonist modulates cocaine-induced dopamine outflow in the rat nucleus accumbens and striatum”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 29 (2): 319—26. PMID 14560323. doi:10.1038/sj.npp.1300329. 
  11. ^ Canal CE, Olaghere da Silva UB, Gresch PJ, Watt EE, Sanders-Bush E, Airey DC (2010). „The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen”. Psychopharmacology. 209 (2): 163—74. PMC 2868321 Слободан приступ. PMID 20165943. doi:10.1007/s00213-010-1784-0. 
  12. ^ Graves, S. M.; Napier, T. C. (2012). „SB 206553, a putative 5-HT2C inverse agonist, attenuates methamphetamine-seeking in rats”. BMC Neuroscience. 13: 65. PMC 3441362 Слободан приступ. PMID 22697313. doi:10.1186/1471-2202-13-65. 
  13. ^ Dunlop J, Lock T, Jow B, Sitzia F, Grauer S, Jow F, Kramer A, Bowlby MR, Randall A, Kowal D, Gilbert A, Comery TA, Larocque J, Soloveva V, Brown J, Roncarati R (2009). „Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/C) receptor antagonist SB-206553 (3,5-dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b']di pyrrole-1(2H)-carboxamide)”. The Journal of Pharmacology and Experimental Therapeutics. 328 (3): 766—76. PMID 19050173. doi:10.1124/jpet.108.146514. 

Spoljašnje veze[уреди | уреди извор]

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