SB269652

Dopamine receptor modulator From Wikipedia, the free encyclopedia

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]

Other namesSB-269652; SB-269,652
CAS Number
Quick facts Clinical data, Other names ...
SB269652
Clinical data
Other namesSB-269652; SB-269,652
Drug classDopamine D2 and D3 receptor negative allosteric modulator
Identifiers
  • N-[4-[2-(7-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]-1H-indole-2-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
FormulaC27H30N4O
Molar mass426.564 g·mol−1
3D model (JSmol)
  • C1CC(CCC1CCN2CCC3=C(C2)C=C(C=C3)C#N)NC(=O)C4=CC5=CC=CC=C5N4
  • InChI=1S/C27H30N4O/c28-17-20-5-8-21-12-14-31(18-23(21)15-20)13-11-19-6-9-24(10-7-19)29-27(32)26-16-22-3-1-2-4-25(22)30-26/h1-5,8,15-16,19,24,30H,6-7,9-14,18H2,(H,29,32)
  • Key:JGLGOAQPUQITLD-UHFFFAOYSA-N
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