SB-277011 (dihydrochloride)

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, 3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

Product Specifications

CAS Number

[1226917-67-4]

Product Name Alternative

SB-277011A (dihydrochloride)

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_277011A_dihydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC=NC2=CC=CC=C12)N[C@H]3CC[C@H](CCN4CC5=C(C=C(C#N)C=C5)CC4)CC3.[H]Cl.[H]Cl

Molecular Formula

C28H32Cl2N4O

Molecular Weight

511.49

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