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SML1936

Ro 64-6198

Name: Ro 64-6198
Brand: SIGMA

≥98% (HPLC), nociceptin receptor ORL-1 (ORL1) agonist , powder

Synonym(s):

(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 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, Ro64-6198

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About This Item

Empirical Formula (Hill Notation):

C₂₆H₃₁N₃O

CAS Number:

280783-56-4

Molecular Weight:

401.54

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD04113242

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Properties

Product Name

Ro 64-6198, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1C2(CCN([C@]3([H])C4=CC=CC5=C4[C@](CCC5)([H])CC3)CC2)N(C6=CC=CC=C6)CN1

InChI

1S/C26H31N3O/c30-25-26(29(18-27-25)21-9-2-1-3-10-21)14-16-28(17-15-26)23-13-12-20-7-4-6-19-8-5-11-22(23)24(19)20/h1-3,5,8-11,20,23H,4,6-7,12-18H2,(H,27,30)/t20-,23-/m0/s1

InChI key

JLFMYEAXZNPWBK-REWPJTCUSA-N

Description

Biochem/physiol Actions

A brain-penetrant, nonpeptidic, high-affinity, reversible, selective nociceptin receptor ORL-1 (ORL1) agonist that elicits anxiolytic-like effects in vivo.

Ro 64-6198 is a brain-penetrant, nonpeptidic, high-affinity (Ki = 0.389 nM against 0.1 nM OFQ for binding human ORL1) nociceptin/orphanin FQ (N/OFQ) receptor ORL-1 (KOR-3, NOP) agonist (EC50 = 38.9 nM by GTPγS binding assay; IC50 = 32.4 nM against forskolin-stimulated cellular cAMP accumulation) with >100-fold selectivity over other opioid receptor family members (Ki = 46.8 nM/μ, 89.1 nM/k, 1.38 μM/δ) and no significant affinity toward 48 other receptors and ion channels (IC50 >1 μM). Ro 64-6198 elicits ORL1-dependent anxiolytic-like effects in several rat models of spontaneous and conditioned anxiety states (0.3-3.2 mg/kg i.p) without antipanic, anticonvulsant, sedative, amnestic activity, or signs of tolerance to its anxiolytic-like effects following chronical dosing.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat.

F Jenck et al.

Proceedings of the National Academy of Sciences of the United States of America, 97(9), 4938-4943 (2000-04-12)

The biochemical and behavioral effects of a nonpeptidic, selective, and brain-penetrant agonist at the ORL1 receptor are reported herein. This low molecular weight compound [(1S,3aS)-8- (2,3,3a,4,5, 6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza- spiro[4. 5]decan-4-one] has high affinity for recombinant human ORL1 receptors and has 100-fold

Characterization of the Discriminative Stimulus Effects of a NOP Receptor Agonist Ro 64-6198 in Rhesus Monkeys.

Phillip A Saccone et al.

The Journal of pharmacology and experimental therapeutics, 357(1), 17-23 (2016-01-24)

Nociceptin/orphanin FQ receptor (NOP) agonists have been reported to produce antinociceptive effects in rhesus monkeys with comparable efficacy to μ-opioid receptor (MOP) agonists, but without their limiting side effects. There are also known to be species differences between rodents and

Pharmacological characterization of the novel nonpeptide orphanin FQ/nociceptin receptor agonist Ro 64-6198: rapid and reversible desensitization of the ORL1 receptor in vitro and lack of tolerance in vivo.

F M Dautzenberg et al.

The Journal of pharmacology and experimental therapeutics, 298(2), 812-819 (2001-07-17)

The novel nonpeptide orphanin FQ/nociceptin (OFQ/N) ligand [(1S,3aS)-8-(2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one] (Ro 64-6198) was characterized in vitro and in vivo for its agonistic potential. Ro 64-6198 was 130- to 3500-fold selective for the OFQ/N receptor (ORL1) compared with opiate receptors. In the cAMP

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Global Trade Item Number

SKU	GTIN
SML1936-5MG	04061832561202
SML1936-25MG	04061832561196