FR260010
Pharmaceutical compound
From Wikipedia, the free encyclopedia
FR260010 is a selective serotonin 5-HT2C receptor antagonist which was under development for the treatment of anxiety disorders but was never marketed.[1][3][2][4] It is taken orally.[1][2]
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| Other names | FR-260010 |
| Routes of administration | Oral[1][2] |
| Drug class | Serotonin 5-HT2C receptor antagonist |
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| Formula | C22H19N5 |
| Molar mass | 353.429 g·mol−1 |
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The drug shows high affinity for the serotonin 5-HT2C receptor (Ki = 1.1 nM) and high selectivity over the serotonin 5-HT2A receptor (Ki = 386 nM) and many other targets.[2] Similarly, it shows little affinity for the serotonin 5-HT2B receptor.[2] FR260010 is a silent antagonist of the serotonin 5-HT2C receptor.[2] It blocks the hypolocomotion and hypophagia induced by the serotonin 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP) in rodents.[2] Similarly to diazepam, the drug produces anxiolytic-like effects in multiple different animal models of anxiety, whereas buspirone was ineffective in the same models.[2][4] In contrast to diazepam but similarly to buspirone, FR260010 has modest adverse effect-like properties in rodents.[2]
FR260010 was under development by Astellas Pharma.[1][3] It was first described in the scientific literature by 2006.[2][4] No recent development has been reported as of 2016.[1] It reached the discovery stage of development prior to its discontinuation.[3]