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Trap-101 hydrochloride

CAS No. : 1216621-00-9

MCE 站：Trap-101 hydrochloride

产品活性：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 CHO_hNOP，NOP、μ-，κ- 和 δ 阿片受体的 pK_i 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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: Trap-101 hydrochloride (3, 30, and 300 nM) is inactive per se up to 10 μM, while in the range 3-300 nM, it produces a concentration dependent rightward shift of the concentration-response curve to N/OFQ without modifications of the maximal response to the agonist. Receptor binding affinities of Trap101 (pK_i?values) at recombinant human NOP, and classical opioid receptors expressed in CHO cell membranes are 8.65, 6.60, 6.14 and < 5 for NOP,?μ-,?κ-, and?δ-opioid receptors respectively.

In Vivo: Trap-101 hydrochloride (10-30 mg/kg; detected after 90 min) changes motor activity in na?ve rats, it causes a delayed increase in the immobility time in the bar test at 30 mg/kg, Moreover, it increased stepping activity and rotarod performance at 10 mg/kg and reduces them at 30 mg/kg.
6-OHDA lesioning produces motor asymmetry mostly affecting the contralateral paw and overall reduced motor performance. Trap-101 hydrochloride (intraperitoneal?injection; 10-30 mg/kg; detected after 90 min) alleviates akinesia/bradykinesia and improves overall gait ability in hemiparkinsonian rats, being effective starting at 1 mg/kg and without worsening motor deficit at 30 mg/kg.

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