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Ro 64-6198
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Ro 64-6198图片
CAS NO:280783-56-4
包装与价格：
包装价格(元)
1mg电议
5mg电议

产品介绍
Ro 64-6198 是一种有效的，选择性的，非肽，高亲和力，高细胞通透性和脑渗透 N/OFQ 受体 (NOP) 激动剂，EC50 值为 25.6 nM。Ro 64-6198 对 NOP 受体的选择性至少是经典阿片受体的 100 倍。Ro 64-6198 可用于治疗压力和焦虑，成瘾，神经性疼痛，咳嗽和厌食症。
Cas No.280783-56-4
Canonical SMILESO=C1NCN(C2=CC=CC=C2)C13CCN([C@H]4CC[C@]5([H])CCCC6=C5C4=CC=C6)CC3
分子式C26H31N3O
分子量401.54
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used to treat stress and anxiety, addiction, neuropathic pain, cough, and anorexia[1][2].

Ro 64-6198 also produces rapid desensitization of the NOP receptor. In vitro studies shows that treatment with Ro 64-6198 results in a 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].Ro 64-6198 does recruit both arrestin3 (EC50 of 0.912 µM) and arrestin2 (EC50 of 1.20 µM) to the NOP receptor in a concentration-dependent manner comparably with N/OFQ[2].

At low doses Ro 64-6198 is anxiolytic in several neophobic tests, 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, at 1 mg/kg, i.p., Ro 64-6198 produces a decrease in the number of marbles buried, without altering locomotor activity, indicating a decrease in neophobia and anxiety. Ro 64-6198 selectively increases the number of open arm transitions and time spent in the open arms of the elevated plus maze at doses of 0.32-3 mg/kg, i.p., without affecting closed arm transitions or locomotor activity in the closed arms. In the open field test, Ro 64-6198, at doses of 0.32-3 mg/kg, attenuates the inhibition of exploration that results from the stress of a novel environment[1].

[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.