SB 277011A dihydrochloride

Names

[ Name ]:
SB 277011A dihydrochloride

[Synonym ]:
N-{trans-4-[2-(6-Cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl}-4-quinolinecarboxamide dihydrochloride
4-Quinolinecarboxamide, N-[trans-4-[2-(6-cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl]-, hydrochloride (1:2)
MFCD16627999
SB 277011A dihydrochloride

Biological Activity

[Description]:

SB 277011A dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

[Related Catalog]:

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

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

pKi: 8.0 (D3 receptor), 6.0 (D2 receptor), <5.2 (5-HT1B receptor), 5.9 (5-HT1D receptor)[1]

[In Vitro]

SB 277011A dihydrochloride is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, and restores ≥100-fold selectivity against the D2, 5-HT1B, and 5-HT1D receptors, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1].

[In Vivo]

SB 277011A (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats[1].

[References]

[1]. Stemp G, et al. 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 dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. J Med Chem. 2000 May 4;43(9):1878-85.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₃₂Cl₂N₄O

[ Molecular Weight ]:
511.486

[ Exact Mass ]:
510.195313

[ Storage condition ]:
-20°C

SB 277011A dihydrochloride

Names

Biological Activity

Chemical & Physical Properties

Related Compounds