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| Other names | Ro64-6198 |
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| Formula | C26H31N3O |
| Molar mass | 401.554 g·mol−1 |
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Ro64-6198 is an opioid drug used in scientific research. It acts as a potent and selective agonist for thenociceptin receptor, also known as the ORL-1 (opiate receptor like-1) receptor, with over 100x selectivity over the other opioid receptors.[1] It producesanxiolytic effects in animal studies equivalent to those ofbenzodiazepine drugs,[2] but has noanticonvulsant 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 hasantitussive 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 reducealcohol 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 theconditioned 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 haveanalgesic effects but without producingrespiratory depression or reinforcing effects.[15]
