All Photos(1)
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
Empirical Formula (Hill Notation):
C25H25N3O · HCl
Recommended Products
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.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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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
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
Anna Rizzi et al.
Pharmacology research & perspectives, 4(4), e00247-e00247 (2017-01-25)
The aim of the study was to investigate the in vitro and in vivo pharmacological profile of cebranopadol, a novel agonist for opioid and nociceptin/orphanin FQ (N/OFQ) receptors (NOP). In vitro cebranopadol was assayed in calcium mobilization studies in cells coexpressing NOP
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