CGS-12066
Chemical compound
From Wikipedia, the free encyclopedia
CGS-12066, also known as CGS-12066A and CGS-12066B, is a predominant serotonin 5-HT1B receptor agonist which was under development for the treatment of anxiety disorders but was never marketed.[1][2][3][4] Its route of administration is unknown.[1]
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| Other names | CGS12066; CGS-12066A; CGS12066A; CGS-12066B; CGS12066B |
| Routes of administration | Unknown[1] |
| Drug class | Serotonin 5-HT1B receptor agonist |
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| Formula | C17H17F3N4 |
| Molar mass | 334.346 g·mol−1 |
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In terms of affinity, it is moderately (17-fold) selective for the serotonin 5-HT1B receptor over the serotonin 5-HT1A receptor, where it is also an agonist.[3][4][5] Although reported to be a selective serotonin 5-HT1B receptor agonist, it was subsequently found to be equipotent as an agonist of the serotonin 5-HT1B and 5-HT1D receptors.[6] The drug showed weak affinity for the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors (Ki = 871–4,270 nM).[7] It had minimal affinity for various adrenergic and dopamine receptors.[4][8]
CGS-12066 produces anxiolytic-like,[9][10] prosocial,[11] and antiaggressive effects in rodents.[12][13] There is rapid tolerance to its prosocial effects, thought to be due to desensitization of serotonin 5-HT1B receptors.[11] 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-HT1B receptor.[14] It produces wakefulness and reduces slow wave sleep (SWS) and rapid eye movement (REM) sleep in rodents.[15][16][17] Some of the effects of CGS-12066 in animals, such as hypothermia and serotonin behavioral syndrome, are not mediated by the serotonin 5-HT1B receptor.[18]
CGS-12066 was first described in the scientific literature by 1987.[4] It reached the preclinical research stage of development for anxiety disorders prior to the discontinuation of its development in 1995.[1][2]