Chemistry:FR260010

FR260010 is a selective serotonin 5-HT_2C receptor antagonist which was under development for the treatment of anxiety disorders but was never marketed. It is taken orally.

The drug shows high affinity for the serotonin 5-HT_2C receptor (K_i = 1.1 nM) and high selectivity over the serotonin 5-HT_2A receptor (K_i = 386 nM) and many other targets. Similarly, it shows little affinity for the serotonin 5-HT_2B receptor. FR260010 is a silent antagonist of the serotonin 5-HT_2C receptor. It blocks the hypolocomotion and hypophagia induced by the serotonin 5-HT_2C receptor agonist meta-chlorophenylpiperazine (mCPP) in rodents. Similarly to diazepam, the drug produces anxiolytic-like effects in multiple different animal models of anxiety, whereas buspirone was ineffective in the same models. In contrast to diazepam but similarly to buspirone, FR260010 has modest adverse effect-like properties in rodents.

FR260010 was under development by Astellas Pharma. It was first described in the scientific literature by 2006. No recent development has been reported as of 2016. It reached the discovery stage of development prior to its discontinuation.

See also

• List of investigational anxiety disorder drugs