Ro64-6198
Encyclopedia
Ro64-6198 is an nociceptoid
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 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.
Nociceptin receptor
The nociceptin receptor or NOP also known as the orphanin FQ receptor or kappa-type 3 opioid receptor is a protein that in humans is encoded by the OPRL1 gene. The nociceptin receptor is a G protein-coupled receptor whose natural ligand is known as nociceptin or orphanin FQ, a 17 amino acid...
drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor
Nociceptin receptor
The nociceptin receptor or NOP also known as the orphanin FQ receptor or kappa-type 3 opioid receptor is a protein that in humans is encoded by the OPRL1 gene. The nociceptin receptor is a G protein-coupled receptor whose natural ligand is known as nociceptin or orphanin FQ, a 17 amino acid...
, also known as the ORL-1 (opiate receptor like-1) receptor, with over 100x selectivity over other opioid receptors. It produces anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
effects in animal studies equivalent to those of benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
drugs, but has no anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
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
Conditioned place preference
Conditioned place preference is a technique commonly used in animal studies to evaluate preferences for environmental stimuli that have been associated with a positive or negative reward...
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
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
effects but without producing respiratory depression or reinforcing effects.