SB-206553

SB-206553
Identifiers
CAS Number 158942-04-2
PubChem (CID) 5163
IUPHAR/BPS 189
Chemical and physical data
Formula C17H16N4O
Molar mass 292.334 g/mol
3D model (Jmol) Interactive image

SB-206553 is a drug which acts as a mixed antagonist for the 5-HT2B and 5-HT2C serotonin receptors.[1][2][3] It has anxiolytic properties in animal studies and interacts with a range of other drugs.[4][5][6][7][8][9][10][11][12] It has also been shown to act as a positive allosteric modulator of α7 nicotinic acetylcholine receptors.[13]

References

  1. ↑ Forbes IT; Ham P; Booth DH; Martin RT; Thompson M; Baxter GS; Blackburn TP; Glen A; Kennett GA; Wood MD (July 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. doi:10.1021/jm00014a004. PMID 7629791.
  2. ↑ Kennett GA; Wood MD; Bright F; Cilia J; Piper DC; Gager T; Thomas D; Baxter GS; Forbes IT; Ham P; Blackburn TP (February 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. doi:10.1111/j.1476-5381.1996.tb15208.x. PMC 1909304Freely accessible. 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 (December 1996). "Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists". Journal of Medicinal Chemistry. 39 (25): 4966–77. doi:10.1021/jm960571v. PMID 8960557.
  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 (May 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. doi:10.1021/jm970741j. PMID 9572885.
  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. doi:10.1016/S0028-3908(98)00014-8. PMID 9680252.
  6. ↑ McCreary AC; Cunningham KA (June 1999). "Effects of the 5-HT2C/2B antagonist SB 206553 on hyperactivity induced by cocaine". Neuropsychopharmacology. 20 (6): 556–64. doi:10.1016/S0893-133X(98)00087-6. PMID 10327425.
  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. doi:10.1016/S0306-4522(98)00655-1. PMID 10366016.
  8. ↑ Takahashi RN; Berton O; Mormède P; Chaouloff F (May 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. doi:10.1590/s0100-879x2001000500017. PMID 11323756.
  9. ↑ Porras G; Di Matteo V; Fracasso C; Lucas G; De Deurwaerdère P; Caccia S; Esposito E; Spampinato U (March 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. 26 (3): 311–24. doi:10.1016/S0893-133X(01)00333-5. PMID 11850146.
  10. ↑ Navailles S; De Deurwaerdère P; Porras G; Spampinato U (February 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. 29 (2): 319–26. doi:10.1038/sj.npp.1300329. PMID 14560323.
  11. ↑ Canal CE; Olaghere da Silva UB; Gresch PJ; Watt EE; Sanders-Bush E; Airey DC (April 2010). "The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen". Psychopharmacology. 209 (2): 163–74. doi:10.1007/s00213-010-1784-0. PMC 2868321Freely accessible. PMID 20165943.
  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. doi:10.1186/1471-2202-13-65. PMC 3441362Freely accessible. PMID 22697313.
  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 (March 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. doi:10.1124/jpet.108.146514. PMID 19050173.


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