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Ro64-6198

Chemical compound

Field	Value
Verifiedfields	changed
verifiedrevid	451981063
IUPAC_name	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
image	Ro64-6198.svg
image_class	skin-invert-image
pregnancy_AU
pregnancy_US
legal_AU
CAS_number_Ref
CAS_number	280783-56-4
UNII_Ref
UNII	HKN6H9XXS6
PubChem	9844019
IUPHAR_ligand	1684
DrugBank_Ref
ChemSpiderID_Ref
ChemSpiderID	8019734
ChEMBL_Ref
ChEMBL	2088034
C	26	H=31	N=3	O=1
smiles	C1C[C@H]2CCC@@HN4CCC5(CC4)C(=O)NCN5C6=CC=CC=C6
StdInChI_Ref
StdInChI	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
StdInChIKey_Ref
StdInChIKey	JLFMYEAXZNPWBK-REWPJTCUSA-N
synonyms	Ro64-6198

| elimination_half-life =

Ro64-6198 is an opioid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 (opiate receptor like-1) receptor, with over 100x selectivity over the other opioid receptors. It produces anxiolytic effects in animal studies equivalent to those of benzodiazepine drugs, but has no anticonvulsant effects and does not produce any overt effects on behaviour. However it does impair short-term memory, and counteracts stress-induced anorexia. It also has antitussive effects, and reduces the rewarding and analgesic effects of morphine, although it did not prevent the development of dependence. It has been shown to reduce alcohol self-administration in animals and suppressed relapses in animal models of alcoholism, and ORL-1 agonists may have application in the treatment of alcoholism.

Ro64-6198 was able to be recognised as a discriminative stimulus by rats distinct from other opioid receptor ligands, but was not able to produce the conditioned place preference thought to be indicative of addictive potential. Consequently, while the role of ORL-1 receptors in the body is complex and remains poorly understood, Ro64-6198 has demonstrated multiple pharmacological actions and has been very useful in the study of the ORL-1 receptor system, especially in relation to anxiety and anorexia; however, due to poor oral bioavailability, Ro 64-6198 will most likely not be pursued clinically. Studies in primates showed it to have analgesic effects but without producing respiratory depression or reinforcing effects.

References

(August 2001). "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". The Journal of Pharmacology and Experimental Therapeutics.
(October 2005). "Characterization of the nociceptin receptor (ORL-1) agonist, Ro64-6198, in tests of anxiety across multiple species". Psychopharmacology.
(April 2000). "A synthetic agonist at the orphanin FQ/nociceptin receptor ORL1: anxiolytic profile in the rat". Proceedings of the National Academy of Sciences of the United States of America.
(March 2002). "A combined pharmacological and genetic approach to investigate the role of orphanin FQ in learning and memory". The European Journal of Neuroscience.
(May 2002). "Reversal of stress- and CRF-induced anorexia in rats by the synthetic nociceptin/orphanin FQ receptor agonist, Ro 64-6198". Psychopharmacology.
(August 2004). "Nociceptin/orphanin FQ acts as a functional antagonist of corticotropin-releasing factor to inhibit its anorectic effect". Physiology & Behavior.
(July 2004). "Antitussive profile of the NOP agonist Ro-64-6198 in the guinea pig". Pharmacology.
(March 2003). "Non-peptidergic OP4 receptor agonist inhibits morphine antinociception but does not influence morphine dependence". NeuroReport.
(September 2005). "The effect of a systemically active ORL-1 agonist, Ro 64-6198, on the acquisition, expression, extinction, and reinstatement of morphine conditioned place preference". Neuropharmacology.
(January 2008). "Effects of nociceptin/orphanin FQ receptor (NOP) agonist, Ro64-6198, on reactivity to acute pain in mice: comparison to morphine". European Journal of Pharmacology.
(April 2007). "The nociceptin/orphanin FQ receptor agonist Ro 64-6198 reduces alcohol self-administration and prevents relapse-like alcohol drinking". Neuropsychopharmacology.
(November 2004). "The opioid receptor like-1 receptor agonist Ro 64-6198 (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) produces a discriminative stimulus in rats distinct from that of a mu, kappa, and delta opioid receptor agonist cue". The Journal of Pharmacology and Experimental Therapeutics.
(March 2002). "The orphanin receptor agonist RO 64-6198 does not induce place conditioning in rats". NeuroReport.
(2007). "The pharmacology of Ro 64-6198, a systemically active, nonpeptide NOP receptor (opiate receptor-like 1, ORL-1) agonist with diverse preclinical therapeutic activity". CNS Drug Reviews.
(August 2009). "Behavioral effects of a synthetic agonist selective for nociceptin/orphanin FQ peptide receptors in monkeys". Neuropsychopharmacology.

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opioids lactams nitrogen-heterocycles drugs-developed-by-hoffmann-la-roche nociceptin-receptor-agonists spiro-compounds heterocyclic-compounds-with-2-rings

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