ABT-724 trihydrochloride

ABT-724 trihydrochloride用途

ABT-724-trihydrochloride 是一种有效且高度选择性的多巴胺 D4 受体激动剂,对人多巴胺 D4 受体的 EC50 为 12.4 nM。ABT-724 trihydrochloride 是大鼠 D4 (EC50 为 14.3 nM) 和雪貂 D4 受体 (EC50 为 23.2 nM) 的有效部分激动剂,对多巴胺 D1,D2,D3 或 D5 受体没有影响。ABT-724 trihydrochloride 可用于治疗勃起功能障碍,并具有较少的副作用。

ABT-724 trihydrochloride名称

[ CAS 号 ]:
587870-77-7

[ 中文名 ]:
ABT 724 三盐酸盐

[ 英文名 ]:
ABT 724 trihydrochloride

[英文别名 ]:

MFCD08703101
ABT-724 trihydrochloride

ABT-724 trihydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[ 靶点 ]

EC50: 12.4 nM (Human dopamine D4 receptor), 14.3 nM (Rat dopamine D4 receptor) and 23.2 nM (Ferret dopamine D4 receptor)[1]

[体外研究]

ABT-724表现出一种选择性的生化特性,这表明它对超过70种神经递质/摄取/离子通道缺乏结合亲和力,这些通道包括D2、D3或D5受体,浓度高达10μM。观察到对5-HT1A受体(Ki=2780nm)的弱亲和力。ABT-724在10μM浓度下不抑制PDE1、PDE5或PDE6的PDE活性[1]。

[体内研究]

ABT-724(8.8μg/kg；皮下注射；每日；连续5天；雄性成年Wistar大鼠)剂量依赖性地促进清醒大鼠接受s.c.时的阴茎勃起[1]。动物模型：雄性成年Wistar大鼠(~300g)[1]剂量：8.8μg/kg给药：皮下注射；每日；连续5d结果：剂量依赖性促进阴茎勃起。

[参考文献]

[1]. Brioni JD, et al. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6758-63.

ABT-724 trihydrochloride物理化学性质

[ 分子式 ]:
C₁₇H₂₂Cl₃N₅

[ 分子量 ]:
402.749

[ 精确质量 ]:
401.094086

[ 储存条件 ]:
2-8°C，干燥

ABT-724 trihydrochloride安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危险品运输编码 ]:
NONH for all modes of transport

ABT-724 trihydrochloride文献

Effects of selective dopaminergic compounds on a delay-discounting task.

Behav. Pharmacol. 22 , 300-11, (2011)

Impulsivity is widely regarded as a multidimensional trait that encompasses two or more distinct patterns of behavior, and dopaminergic systems are implicated in the expression of impulsive behavior i...

Dopamine D4 receptor involvement in the discriminative stimulus effects in rats of LSD, but not the phenethylamine hallucinogen DOI.

Psychopharmacology 203 , 265-77, (2009)

Lysergic acid diethylamide (LSD) differs from other types of hallucinogens in that it possesses direct dopaminergic effects. The exact nature of this component has not been elucidated.The present stud...

Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors.

Behav. Pharmacol. 20 , 303-11, (2009)

Dopamine (DA) is implicated in penile erection (PE) and yawning (YA) in rats through activation of D2-like receptors. However, the exact role of each subtype (D2, D3 and D4) of this receptor family in...

更多文献