For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>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.<br>IC50 value: 0.2/0.5 nM [1]<br>Target: D3 receptor antagonist<br>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].</p>
| Catalog Number | I002652 |
| CAS Number | 215802-15-6 |
| Synonyms | N-((1r,4r)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide |
| Molecular Formula | C27H30N4O |
| Purity | ≥95% |
| Target | Dopamine Receptor |
| Solubility | 10 mM in DMSO |
| Storage | Desiccate at -20C |
| IC50 | 0.2/0.5 nM [1] |
| IUPAC Name | N-[4-[2-(7-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]-1H-indole-2-carboxamide |
| InChI | 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) |
| InChIKey | JGLGOAQPUQITLD-UHFFFAOYSA-N |
| SMILES | C1CC(CCC1CCN2CCC3=C(C2)C=C(C=C3)C#N)NC(=O)C4=CC5=CC=CC=C5N4 |
| Reference | </br>1:The First Negative Allosteric Modulator for Dopamine D<sub>2</sub> and D<sub>3</sub> Receptors, SB269652 May Lead to a New Generation of Antipsychotic Drugs. Rossi M, Fasciani I, Marampon F, Maggio R, Scarselli M.Mol Pharmacol. 2017 Jun;91(6):586-594. doi: 10.1124/mol.116.107607. Epub 2017 Mar 6. PMID: 28265019 </br>2:Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor. Shonberg J, Draper-Joyce C, Mistry SN, Christopoulos A, Scammells PJ, Lane JR, Capuano B.J Med Chem. 2015 Jul 9;58(13):5287-307. doi: 10.1021/acs.jmedchem.5b00581. Epub 2015 Jun 24. PMID: 26052807 |
