Ro64-6198

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.^[1] It produces anxiolytic effects in animal studies equivalent to those of benzodiazepine drugs,^[2] but has no anticonvulsant effects and does not produce any overt effects on behaviour.^[3] However it does impair short-term memory,^[4] and counteracts stress-induced anorexia.^[5][6] It also has antitussive effects,^[7] and reduces the rewarding and analgesic effects of morphine, although it did not prevent the development of dependence.^[8][9][10] 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.^[11]

Other namesRo64-6198

CAS Number

• 280783-56-4 ^N

PubChem CID

• 9844019

IUPHAR/BPS

• 1684

Quick facts Clinical data, Other names ...

Ro64-6198

Clinical data
Other names	Ro64-6198
Identifiers
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
CAS Number	280783-56-4 N
PubChem CID	9844019
IUPHAR/BPS	1684
ChemSpider	8019734 N
UNII	HKN6H9XXS6
ChEMBL	ChEMBL2088034 N
CompTox Dashboard (EPA)	DTXSID901018435
Chemical and physical data
Formula	C26H31N3O
Molar mass	401.554 g·mol−1
3D model (JSmol)	Interactive image
SMILES C1C[C@H]2CC[C@@H](C3=CC=CC(=C23)C1)N4CCC5(CC4)C(=O)NCN5C6=CC=CC=C6
InChI InChI=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 N Key:JLFMYEAXZNPWBK-REWPJTCUSA-N N
NY (what is this?)  (verify)

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Ro64-6198 was able to be recognised as a discriminative stimulus by rats distinct from other opioid receptor ligands,^[12] but was not able to produce the conditioned place preference thought to be indicative of addictive potential.^[13] 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.^[14] Studies in primates showed it to have analgesic effects but without producing respiratory depression or reinforcing effects.^[15]