SB-277011

• 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

• Product Name Alternative:

  SB-277011A

• 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/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 Formula:

  C28H30N4O

• Molecular Weight:

  438.56

• 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

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  5-HT1 Receptor

• CAS Number:

  215803-78-4