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SML1936 Sigma-Aldrich

Ro 64-6198

≥98% (HPLC)

Synonym: (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

  • CAS Number 280783-56-4

  • Empirical Formula (Hill Notation) C26H31N3O

  • Molecular Weight 401.54

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Properties

assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 2 mg/mL, clear
storage temp.   2-8°C

Description

Biochem/physiol Actions

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.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
RTECS 
XX9275500

Documents

Certificate of Analysis

Protocols & Articles
Peer-Reviewed Papers
15

References

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