SML2133
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
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About This Item
Empirical Formula (Hill Notation):
C25H25N3O · HCl
CAS Number:
Molecular Weight:
419.95
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
InChI key
CTPVGIUCSWWLNA-UHFFFAOYSA-N
SMILES string
O=C1NCN(C2=CC=CC=C2)C13CCN(C4CC5=C6C4=CC=CC6=CC=C5)CC3.Cl
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Related Categories
Biochem/physiol Actions
A selective, nonpeptidic, high-affinity nociceptin receptor ORL-1 (ORL1) agonist that elicits anxiolytic-like effects in vivo.
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
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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
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
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
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