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Ro 64-6198

产品编号 T16772 CAS 280783-56-4

Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors.

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Ro 64-6198, CAS 280783-56-4

规格	价格/CNY		货期	数量
25 mg	￥ 10,500		待询

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Ro 64-6198 is a nonpeptide, high-affinity, and brain penetration N/OFQ receptor (NOP) agonist (EC50: 25.6 nM). Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors.
体外活性	Ro 64-6198 does recruit both arrestin3 (EC50 of 0.912 μM) and arrestin2 (EC50: 1.20 μM) to the NOP receptor in a concentration-dependent manner comparably with N/OFQ. Ro 64-6198 also produces rapid desensitization of the NOP receptor. Ro 64-6198 causes functional desensitization of the receptor, a loss in binding sites, and an apparent decrease in binding affinity. The desensitization produced by Ro 64-6198 is not reversed by acidic washes [1][2].
体内活性	Ro 64-6198 is anxiolytic in several neophobic tests at low doses, including the marble burying test in mice, the elevated plus-maze in rats, and the open field test in rats. In the marble burying test, Ro 64-6198 (1 mg/kg, i.p.,) produces a decrease in the number of marbles buried, without altering locomotor activity, indicating a decrease in neophobia and anxiety. Ro 64-6198 (0.32-3 mg/kg, i.p.,) selectively increases the number of open arm transitions and time spent in the open arms of the elevated plus-maze without affecting closed-arm transitions or locomotor activity in the closed arms. Ro 64-6198 (0.32-3 mg/kg) attenuates the inhibition of exploration that results from the stress of a novel environment [1].

分子量	401.54
分子式	C26H31N3O
CAS No.	280783-56-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Shoblock JR. The pharmacology of Ro 64-6198, a systemically active, nonpeptide NOP receptor (opiate receptor-like 1, ORL-1) agonist with diverse preclinical therapeutic activity. CNS Drug Rev. 2007 Spring;13(1):107-36. 2. Chang SD, et al. Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198). ACS Chem Neurosci. 2015 Dec 16;6(12):1956-64.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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