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Submit ReviewSB 277011A dihydrochloride is a selective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively). Brain penetrant.
Sold for research purposes under agreement from GlaxoSmithKline.
M. Wt | 511.49 |
Formula | C28H30N4O.2HCl |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 1226917-67-4 |
PubChem ID | 75358288 |
InChI Key | HEZIOTGUXSPDAK-UHFFFAOYSA-N |
Smiles | O=C(N[C@@H]3CC[C@@H](CCN4CC(C=CC(C#N)=C5)=C5CC4)CC3)C1=C2C(C=CC=C2)=NC=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 25.57 | 50 |
The following data is based on the product molecular weight 511.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 3.91 mL | 19.55 mL | 39.1 mL |
2.5 mM | 0.78 mL | 3.91 mL | 7.82 mL |
5 mM | 0.39 mL | 1.96 mL | 3.91 mL |
25 mM | 0.08 mL | 0.39 mL | 0.78 mL |
References are publications that support the biological activity of the product.
Reavill et al (2000) Pharmacological actions of a novel, high-affinity, and selective human DA D3 receptor antagonist, SB-277011-A. J.Pharmacol.Exp.Ther. 294 1154 PMID: 10945872
Stemp et al (2000) Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): a potent and selective DA D3 receptor antagonist with high oral bioavailability and CNS pe J.Med.Chem. 43 1878 PMID: 10794704
If you know of a relevant reference for SB 277011A dihydrochloride, please let us know.
Keywords: SB 277011A dihydrochloride, SB 277011A dihydrochloride supplier, SB277011A, dihydrochloride, dopamine, dopaminergic, receptors, antagonists, selective, d3, D3, Receptors, 4207, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for SB 277011A dihydrochloride include:
Chen et al (2013) Electroacupuncture reduces cocaine-induced seizures and mortality in mice. Nat Neurosci 2013 134610 PMID: 23690833
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.