SB-277011
Product Specifications
UNSPSC Description
SB-277011 is a potent and delective 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.
IC50 value: 8.0 (pKi)
Target: D3 receptor
Target Antigen
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/sb-277011.html
Solubility
10 mM in DMSO
Smiles
O=C(C1=CC=NC2=CC=CC=C21)N[C@@H]3CC[C@H](CC3)CCN4CC5=C(CC4)C=C(C#N)C=C5
Molecular Weight
438.564
References & Citations
[1]Clément P, Pozzato C, Heidbreder C, Alexandre L, Giuliano F, Melotto S.Delay of ejaculation induced by SB-277011, a selective dopamine D3 receptor antagonist, in the rat.J Sex Med. 2009 Apr;6(4):980-8. Epub 2008 Feb 4.|[2]Gyertyán I, Sághy K.The selective dopamine D3 receptor antagonists, SB 277011-A and S 33084 block haloperidol-induced catalepsy in rats.Eur J Pharmacol. 2007 Oct 31;572(2-3):171-4. Epub 2007 Jun 29.|[3]Southam E, Lloyd A, Jennings CA, Cluderay JE, Cilia J, Gartlon JE, Jones DN.Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain.Brain Res. 2007 May 29;1149:50-7. Epub 2007 Feb 28.|[4]Pak AC, Ashby CR Jr, Heidbreder CA, Pilla M, Gilbert J, Xi ZX, Gardner EL.The selective dopamine D3 receptor antagonist SB-277011A reduces nicotine-enhanced brain reward and nicotine-paired environmental cue functions.Int J Neuropsychopharmacol. 2006 Oct;9(5):585-602. Epub 2006 Aug 31.|[5]Higley, Amanda E.; Kiefer, Stephen W.; Li, Xia; Gaal, Jozsef; Xi, Zheng-Xiong; Gardner, Eliot L. Dopamine D3 receptor antagonist SB-277011A inhibits methamphetamine self-administration and methamphetamine-induced reinstatement of drug-seeking in rats. European journal of pharmacology (2011), 659(2-3), 187-192.
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10847/SB-277011-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10847/
Clinical Information
No Development Reported
CAS Number
215803-78-4
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