SB-206553 explained

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] Modified derivatives of SB-206553 have been used to probe the structure of the 5-HT2B receptor.[14]

Notes and References

  1. Forbes IT, Ham P, Booth DH, Martin RT, Thompson M, Baxter GS, Blackburn TP, Glen A, Kennett GA, Wood MD . 6 . 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 . July 1995 . 7629791 . 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 . 6 . 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 . February 1996 . 8821530 . 1909304 . 10.1111/j.1476-5381.1996.tb15208.x .
  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 . 6 . Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists . Journal of Medicinal Chemistry . 39 . 25 . 4966–77 . December 1996 . 8960557 . 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 . 6 . 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 . May 1998 . 9572885 . 10.1021/jm970741j .
  5. Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E . Selective blockade of serotonin2C/2B receptors enhances dopamine release in the rat nucleus accumbens . Neuropharmacology . 37 . 2 . 265–72 . 1998 . 9680252 . 10.1016/S0028-3908(98)00014-8 . 2366196 .
  6. McCreary AC, Cunningham KA . Effects of the 5-HT2C/2B antagonist SB 206553 on hyperactivity induced by cocaine . Neuropsychopharmacology . 20 . 6 . 556–64 . June 1999 . 10327425 . 10.1016/S0893-133X(98)00087-6 . free .
  7. Di Giovanni G, De Deurwaerdére P, Di Mascio M, Di Matteo V, Esposito E, Spampinato U . 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 . 1999 . 10366016 . 10.1016/S0306-4522(98)00655-1 . 23080031 .
  8. Takahashi RN, Berton O, Mormède P, Chaouloff F . 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 . May 2001 . 11323756 . 10.1590/s0100-879x2001000500017 . free .
  9. Porras G, Di Matteo V, Fracasso C, Lucas G, De Deurwaerdère P, Caccia S, Esposito E, Spampinato U . 6 . 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 . March 2002 . 11850146 . 10.1016/S0893-133X(01)00333-5 . free .
  10. Navailles S, De Deurwaerdère P, Porras G, Spampinato U . 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 . February 2004 . 14560323 . 10.1038/sj.npp.1300329 . free .
  11. Canal CE, Olaghere da Silva UB, Gresch PJ, Watt EE, Sanders-Bush E, Airey DC . The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen . Psychopharmacology . 209 . 2 . 163–74 . April 2010 . 20165943 . 2868321 . 10.1007/s00213-010-1784-0 .
  12. Graves SM, Napier TC . SB 206553, a putative 5-HT2C inverse agonist, attenuates methamphetamine-seeking in rats . BMC Neuroscience . 13 . 65 . June 2012 . 22697313 . 3441362 . 10.1186/1471-2202-13-65 . free .
  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 . 6 . 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 . March 2009 . 19050173 . 10.1124/jpet.108.146514 . 206500076 .
  14. Kim SK, Li Y, Abrol R, Heo J, Goddard III WA . Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors . Journal of Chemical Information and Modeling . 51 . 2 . 420–33 . February 2011 . 21299232 . 3070210 . 10.1021/ci100375b .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "SB-206553".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.