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Ro 64-6198

Catalog No. 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

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25 mg	Inquiry	$ 995.00

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Description	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.
In vitro	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].
In vivo	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].

Molecular Weight	401.54
Formula	C26H31N3O
CAS No.	280783-56-4

Storage

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

References and Literature

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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Keywords

Ro 64-6198 280783-56-4 Others Ro 646198 Ro 64 6198 inhibitor inhibit

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