SB-277011 hydrochloride

Research use only, not for human use.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R.

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, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

——

SB-277011 hydrochloride has an excellent pharmacokinetic profile, exhibits oral bioavailability 43%, half-life:2.0 h, plasma clearance 19 mL/min/kg) and to be highly brain-penetrant (brain:blood ratio of 3.6:1), with a clean P450 profile in the rat.SB-277011 hydrochloride (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.SB-277011 (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011 can significantly inhibit basal and cocaine-enhanced locomotion in rats.

——

GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

——

——

215804-67-4

475.03

C28H31ClN4O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (105.26 mM; Ultrasonic )H2O : 16.67 mg/mL (35.09 mM; Ultrasonic)

C(N[C@@H]1CC[C@@H](CCN2CC=3C(CC2)=CC(C#N)=CC3)CC1)(=O)C=4C5=C(N=CC4)C=CC=C5.Cl

——

(-20℃)

With Ice Pack

≥ 2 years