SB-277011

Names

[ Name ]:
SB-277011

[Synonym ]:
N-{trans-4-[2-(6-Cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl}-4-quinolinecarboxamide
cc-478
4-Quinolinecarboxamide, N-[trans-4-[2-(6-cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl]-
N-{trans-4-[2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl]cyclohexyl}quinoline-4-carboxamide
SB-277011

Biological Activity

[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

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[References]

[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;

[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. Eur

[Related Small Molecules]