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Other names | Ro64-6198 |
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Chemical and physical data | |
Formula | C26H31N3O |
Molar mass | 401.554 g·mol−1 |
3D model ( JSmol) | |
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(what is this?) (verify) |
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]
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]
Clinical data | |
---|---|
Other names | Ro64-6198 |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
ChEMBL | |
Chemical and physical data | |
Formula | C26H31N3O |
Molar mass | 401.554 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(what is this?) (verify) |
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]
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]