SB-277011 dihydrochloride  (Synonyms: SB-277011A dihydrochloride)

SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor antagonist, with pK_is of 8.0, 6.0, <5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1D receptors, respectively.

SB-277011 dihydrochloride 是一种口服有效的、选择性的脑穿透多巴胺 D₃ 受体拮抗剂，对 D₂ 受体、5-HT_1B 受体、5-HT_1D 受体可恢复 ≥100 倍的选择性，对 D₃、D₂、5-HT_1B、5-HT_1D 受体的 pK_i 分别为 8.0、6.0、5.2 和 5.9^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SB-277011 dihydrochloride (SB 277011；3 mg/kg，口服)完全逆转喹诺兰对大鼠伏隔核的影响，但不逆转喹诺兰在 93 mg/kg 大鼠纹状体中的影响^[1]。
SB-277011A dihydrochloride (腹腔注射；12.5-25 mg/kg)显著且剂量依赖性地抑制大鼠的自身给药行为。当增加至 50 mg/kg时，SB-277011A dihydrochloride 显著抑制大鼠的基础运动和成瘾剂增强运动^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

511.49

C₂₈H₃₂Cl₂N₄O

1226917-67-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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  [Content Brief]