SB269652

CAT: 0804-HY-12324-01Size: 1 mgDry Ice: NoHazardous: No

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CAT#:0804-HY-12324-01Size:1 mg

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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].

CAS Number

215802-15-6

UNSPSC

12352005

Target

Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/sb269652.html

Purity

98.13

Solubility

DMSO : 2 mg/mL (ultrasonic; warming)

Smiles

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

Molecular Formula

C27H30N4O

Molecular Weight

426.55

References & Citations

[1]Silvano E, et al. The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors. Mol Pharmacol. 2010 Nov;78 (5) :925-34.|[2]Lane JR, et al. A new mechanism of allostery in a G protein-coupled receptor dimer. Nat Chem Biol. 2014 Sep;10 (9) :745-52.|[3]Presgraves SP, et al. Involvement of dopamine D (2) /D (3) receptors and BDNF in the neuroprotective effects of S32504 and pramipexole against 1-methyl-4-phenylpyridinium in terminally differentiated SH-SY5Y cells. Exp Neurol. 2004 Nov;190 (1) :157-70.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

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A14191-10	SB269652 10mg
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A14191-100	SB269652 100mg
A14191-1	SB269652 1mg

SB269652

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