SB 277011A dihydrochloride

Modify Date: 2024-01-06 10:46:25

SB 277011A dihydrochloride structure	Common Name	SB 277011A dihydrochloride
	CAS Number	1226917-67-4	Molecular Weight	511.486
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₈H₃₂Cl₂N₄O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of SB 277011A dihydrochloride

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.

Name	N-{trans-4-[2-(6-Cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl}-4-quinolinecarboxamide dihydrochloride
Synonym	More Synonyms

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.

Molecular Formula	C₂₈H₃₂Cl₂N₄O
Molecular Weight	511.486
Exact Mass	510.195313
Storage condition	-20°C

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

SB 277011A dihydrochloride

Use of SB 277011A dihydrochloride

Names

SB 277011A dihydrochloride Biological Activity

Chemical & Physical Properties

Synonyms