SB-277011 hydrochloride (SB-277011A hydrochloride) 是一种强效、选择性、口服生物利用度和脑透多巴胺 D₃ 受体(D₃R) 拮抗剂，其 K_i 值在啮齿动物和人D₃R 分别为 10.7 nM 和 11.2 nM。SB-277011 hydrochloride 对 D3 受体比其他多巴胺受体表现出 80-100 倍的选择性，，对 D₃，D₂，5-HT_1B 和 5-HT_1D 受体的 pK_i 值分别为 8.0，6.0，<5.2 和 5.9。

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D 3  receptor (D 3 R) antagonist with K i values of 10.7 nM and 11.2 nM at rodent and human D 3 R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pK i s of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT 1B , and 5-HT 1D receptors, respectively.

Solid

D3 Receptor 10.7-11.2 nM (Ki) D2 Receptor

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.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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 penetr
[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

In Vitro: DMSO : 50 mg/mL (105.26 mM; Need ultrasonic)H₂O : 16.67 mg/mL (35.09 mM; Need ultrasonic)配制储备液