SB269652 is an experimental dopamine D2 and D3 receptor negative allosteric modulator.[1][2] It is of interest in the potential development of novel antipsychotics for treatment of schizophrenia with reduced side effects, such as extrapyramidal symptoms.[1][2] The drug is described as a dual orthosteric and allosteric (i.e., bitopic) modulator of the dopamine D2 and D3 receptors, as an atypical allosteric modulator of these receptors, and as specifically targeting D2–D3 receptor dimers.[1][2] SB269652 was first described in the scientific literature by 1999.[3][4] It was originally thought to act purely as an antagonist of the dopamine D2 and D3 receptors, but was serendipitously found to be a negative allosteric modulator of these receptors in 2010.[1][2] It was the first dopamine D2 and D3 receptor negative allosteric modulator to be discovered.[1] More potent analogues of SB269652 have been developed.[2][5]

References

  1. ^ a b c d e Rossi M, Fasciani I, Marampon F, Maggio R, Scarselli M (June 2017). "The First Negative Allosteric Modulator for Dopamine D2 and D3 Receptors, SB269652 May Lead to a New Generation of Antipsychotic Drugs". Mol Pharmacol. 91 (6): 586–594. doi:10.1124/mol.116.107607. PMC 5438131. PMID 28265019.
  2. ^ a b c d e Fasciani I, Petragnano F, Aloisi G, Marampon F, Carli M, Scarselli M, Maggio R, Rossi M (November 2020). "Allosteric Modulators of G Protein-Coupled Dopamine and Serotonin Receptors: A New Class of Atypical Antipsychotics". Pharmaceuticals (Basel). 13 (11): 388. doi:10.3390/ph13110388. PMC 7696972. PMID 33202534.
  3. ^ Taylor, S. G., Riley, G., Hunter, A. J., Stemp, G., Routledge, C., Hagan, J. J., & Reavill, C. (1999). SB-269652 is a selective D3 receptor antagonist in vitro and in vivo. European Neuropsychopharmacology, (9), 266. https://scholar.google.com/scholar?cluster=9009628132294457655
  4. ^ Taylor, S. G., Riley, G., Hunter, A. J., Stemp, G., & Routledge, C. (1999). A selective dopamine D 3 receptor antagonist, SB-269652, shows functional selectivity for D 3 receptors in vivo. Monitoring molecules in neuroscience. SUNY at Stony Brook, New York, 254-255. https://scholar.google.com/scholar?cluster=7754123302347796269
  5. ^ Kopinathan A, Draper-Joyce C, Szabo M, Christopoulos A, Scammells PJ, Lane JR, Capuano B (January 2019). "Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-((trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity at the Dopamine D2 Receptor". J Med Chem. 62 (1): 371–377. doi:10.1021/acs.jmedchem.8b00192. PMID 29890071.


Allikas: http://en.wikipedia.org/wiki/SB269652
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