CGS-12066

CGS-12066, also known as CGS-12066A and CGS-12066B, is a predominant serotonin 5-HT_1B receptor agonist which was under development for the treatment of anxiety disorders but was never marketed. Its route of administration is unknown.
In terms of affinity, it is moderately selective for the serotonin 5-HT_1B receptor over the serotonin 5-HT_1A receptor, where it is also an agonist. Although reported to be a selective serotonin 5-HT_1B receptor agonist, it was subsequently found to be equipotent as an agonist of the serotonin 5-HT_1B and 5-HT_1D receptors. The drug showed weak affinity for the serotonin 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors. It had minimal affinity for various adrenergic and dopamine receptors.
CGS-12066 produces anxiolytic-like, prosocial, and antiaggressive effects in rodents. There is rapid tolerance to its prosocial effects, thought to be due to desensitization of serotonin 5-HT_1B receptors. The drug also produces hyperlocomotion in rodents, although to a much lesser extent than RU-24969, perhaps due to its lower-efficacy partial agonism of the serotonin 5-HT_1B receptor. It produces wakefulness and reduces slow wave sleep and rapid [eye movement sleep|rapid eye movement] sleep in rodents. Some of the effects of CGS-12066 in animals, such as hypothermia and serotonin [behavioral syndrome], are not mediated by the serotonin 5-HT_1B receptor.
CGS-12066 was first described in the scientific literature by 1987. It reached the preclinical research stage of development for anxiety disorders prior to the discontinuation of its development in 1995.