1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. SB269652

SB269652 

Cat. No.: HY-12324
Handling Instructions

SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.

For research use only. We do not sell to patients.

SB269652 Chemical Structure

SB269652 Chemical Structure

CAS No. : 215802-15-6

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Description

SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology. IC50 value: 0.2/0.5 nM [1] Target: D3 receptor antagonist SB269,652 potently (low nanomolar range) abolished specific binding of [(3)H]nemanopride and [(3)H]spiperone to Chinese hamster ovary-transfected D(3) receptors when radioligands were used at 0.2 and 0.5 nM, respectively. However, even at high concentrations (5 μM), SB269,652 only submaximally inhibited the specific binding of these radioligands when they were employed at 10-fold higher concentrations. By analogy, although SB269,652 potently blocked D(3) receptor-mediated activation of Gα(i3) and phosphorylation of extracellular-signal-regulated kinase (ERK)1/2, when concentrations of dopamine were increased by 10-fold, from 1 μM to 10 μM, SB269,652 only submaximally inhibited dopamine-induced stimulation of Gα(i3) [1].

Molecular Weight

426.55

Formula

C₂₇H₃₀N₄O

CAS No.

215802-15-6

SMILES

O=C(C1=CC2=C(C=CC=C2)N1)N[[email protected]]3CC[[email protected]](CCN(CC4)CC5=C4C=CC(C#N)=C5)CC3

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SB269652SB 269652SB-269652Dopamine ReceptorInhibitorinhibitorinhibit

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