Skip to Content
MilliporeSigma
All Photos(1)

Documents

SML2133

Sigma-Aldrich

Ro 65-6570 Hydrochloride

≥98% (HPLC)

Synonym(s):

(RS)-8-(1,2-Dihydro-1-acenaphthylenyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one Hydrochloride, (RS)-8-Acenaphthen-1-yl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one hydrochloride, Ro65-6570 Hydrochloride

Sign Into View Organizational & Contract Pricing
All Photos(1)

About This Item

Empirical Formula (Hill Notation):
C25H25N3O · HCl
CAS Number:
228246-34-2
Molecular Weight:
419.95
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1NCN(C2=CC=CC=C2)C13CCN(C4CC5=C6C4=CC=CC6=CC=C5)CC3.Cl

Biochem/physiol Actions

Ro 65-6570 is a nonpeptidic, high-affinity (Ki = 0.52 against 0.1 nM OFQ for binding human ORL1) nociceptin/orphanin FQ (N/OFQ) receptor ORL-1 (KOR-3, NOP) agonist (EC50 = 40 nM by GTPγS binding assay; IC50 = 0.28 nM against 1 μM forskolin-stimulated cellular cAMP accumulation) with good selectivity over opioid receptors μ, k, δ (Ki = 5.9, 26, 250 nM against 1.5 nM naloxone, 3 nM naloxone, 0.3 nM [Ile5,6]-deltorphin II for binding respective receptors), dopamine and serotonin receptors (Ki = 520 nM/D2, 1210 nM/D3,350 nM/D4.4; Ki ≥1 μM for 5HT 1Dα, 2A, 2C, 6, 7). Ro 65-6570 elicits ORL1-dependent anxiolytic-like effects in rats in vivo (0.32-3.2 mg/kg i.p.; elevated plus maze) without affecting spontaneous locomotion. Unlike OFQ, Ro 65-6570 does not affect cocaine-induced conditioned place preference (CPP) in rats.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

J Kotlińska et al.
Behavioural pharmacology, 13(3), 229-235 (2002-07-18)
The present study investigated the effect of orphanin FQ/nociceptin (OFQ/N), the endogenous ligand of the opioid receptor-like 1 (ORL-1) receptor on the expression of cocaine-induced conditioned place preference (CPP) in rats. To extend this study, the new non-peptidic compound Ro
J Wichmann et al.
Bioorganic & medicinal chemistry letters, 9(16), 2343-2348 (1999-09-07)
A series of 8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan+ ++-4-one derivatives 1 was studied with respect to the binding affinity for the orphanin FQ (OFQ) and opioid (mu, kappa, delta) receptors. The influence of stereochemistry as well as the substitution pattern of the phenyl-ring in
D Malfacini et al.
PloS one, 10(8), e0132865-e0132865 (2015-08-08)
Nociceptin/orphanin FQ (N/OFQ) controls several biological functions by selectively activating an opioid like receptor named N/OFQ peptide receptor (NOP). Biased agonism is emerging as an important and therapeutically relevant pharmacological concept in the field of G protein coupled receptors including
S Röver et al.
Journal of medicinal chemistry, 43(7), 1329-1338 (2001-02-07)
The discovery of 8-(5,8-dichloro-1,2,3,4-tetrahydro-naphthalen-2-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, 1a, as a high-affinity ligand for the human ORL1 (orphanin FQ/nociceptin) receptor led to the synthesis of a series of optimized ligands. These compounds exhibit high affinity for the human ORL1 receptor, exhibit moderate to good
L Asth et al.
Neuropharmacology, 105, 434-442 (2016-02-13)
Nociceptin/orphanin FQ (N/OFQ) receptor (NOP) agonists produce anxiolytic-like effects in rodents while antagonists promote antidepressant-like effects. The aim of this study was to investigate the effect on anxiety and depression of NOP receptor partial agonists such as the peptides [F/G]N/OFQ(1-13)NH2
View All Related Papers

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service