SB-277011 (hydrochloride)

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, 1B, and 5-HT1D receptors, respectively[1][2].

Product Specifications

CAS Number

[215804-67-4]

Product Name Alternative

SB-277011A (hydrochloride)

UNSPSC

12352005

Target

5-HT Receptor; 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-hydrochloride.html

Purity

99.59

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 16.67 mg/mL (ultrasonic)

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.[H]Cl

Molecular Formula

C28H31ClN4O

Molecular Weight

475.02

References & Citations

[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.|[2]Rui Song, et al. YQA14: A Novel Dopamine D3 Receptor Antagonist That Inhibits Cocaine Self-Administration in Rats and Mice, but Not in D3 Receptor-Knockout Mice. Addict Biol