For research use only. Not for therapeutic Use.
SB269652 （Cat No.: I002652） is a negative allosteric modulator of dopamine D2 and D3 receptors, representing a novel class of non-competitive inhibitors. Unlike traditional dopamine antagonists, SB269652 binds at an allosteric site, reducing receptor activity without directly blocking the orthosteric binding site. This unique mechanism offers potential therapeutic applications in neuropsychiatric disorders such as schizophrenia and drug addiction. By selectively modulating dopamine receptor function, SB269652 provides insights into receptor dimerization and signaling, contributing to the development of next-generation dopaminergic therapeutics with improved specificity.
| 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 | Neuronal Signaling |
| 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 |
