Trap-101 hydrochloride

Trap-101 hydrochloride用途

Trap-101 hydrochloride 是一种有效的,选择性和竞争性的 NOP receptors 拮抗剂 ,对 NOP 受体的选择性高于对其他的阿片受体。Trap-101 刺激 GTPγ35S 结合到 CHOhNOP,NOP、μ-,κ- 和 δ 阿片受体的 pKi 值分别为 8.65, 6.60, 6.14 和 <5。Trap-101 减弱帕金森病大鼠运动缺陷,可用于神经系统疾病的研究。

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Trap-101 hydrochloride名称

[ CAS 号 ]:
1216621-00-9

[ 英文名 ]:
Trap 101

[英文别名 ]:

Trap-101 hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[ 靶点 ]

pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5 (δ-opioid receptor)[1]

[体外研究]

Trap-101盐酸盐(3、30和300 nM)本身在10μM以下是不活跃的,而在3-300 nM范围内,它产生浓度依赖性的浓度响应曲线向N/OFQ右移,而不改变对激动剂的最大响应。重组人NOP和CHO细胞膜上表达的经典阿片受体Trap101(pKi值)的受体结合亲和力分别为8.65、6.60、6.14和<5。

[体内研究]

Trap-101盐酸盐(10-30mg/kg；90min后检测)改变了幼年大鼠的运动活性,使30mg/kg的棒试验中的不动时间延迟增加,并且在10mg/kg时增加了步进活动和旋转木马性能,在30mg/kg时降低了它们[1]。6-OHDA减压术产生的运动不对称性主要影响对侧足和整体运动性能的降低。Trap-101盐酸盐(腹腔注射；10-30 mg/kg；90分钟后检测)减轻偏瘫帕金森大鼠的运动障碍/运动迟缓,并改善整体步态能力,从1 mg/kg开始有效,在30 mg/kg时不会恶化运动障碍[1]。动物模型：6-OHDA半脑损伤大鼠[1]剂量：10-30mg/kg给药：腹腔注射；10-30mg/kg；90min后检测结果：大鼠帕金森样运动障碍减弱。

[参考文献]

[1]. Matteo Marti, et al. The novel nociceptin/orphanin FQ receptor antagonist Trap-101 alleviates experimental parkinsonism through inhibition of the nigro-thalamic pathway: positive interaction with L-DOPA. J Neurochem. 2008 Dec;107(6):1683-96.

Trap-101 hydrochloride物理化学性质

[ 分子式 ]:
C₂₄H₃₆ClN₃O₂

[ 分子量 ]:
434.01500

[ 精确质量 ]:
433.25000

[ PSA ]:
50.40000

[ LogP ]:
4.83240

Trap-101 hydrochlorideMSDS

详细MSDS(安全技术说明书)

Trap-101 hydrochloride安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

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