What is "eptapirone"

n. A potent azaspirodecanedione drug.

Eptapirone (F-11,440) is a very potent and highly selective 5-HT receptor full agonist of the azapirone family. Its affinity for the 5-HT receptor was reported to be 4.8 nM (K) (or 8.33 (pK)), and its intrinsic activity approximately equal to that of serotonin (i.e., 100%).

Eptapirone and related high-efficacy 5-HT full and super agonists such as befiradol and F-15,599 were developed under the hypothesis that the maximum exploitable therapeutic benefits of 5-HT receptor agonists might not be able to be seen without the drugs employed possessing sufficiently high intrinsic activity at the receptor. As 5-HT receptor agonism, based on animal and other research, looked extremely promising for the treatment of depression from a theoretical perspective, this idea was developed as a potential explanation for the relatively modest clinical effectiveness seen with already available 5-HT receptor agonists like buspirone and tandospirone, which act merely as weak-to-moderate partial agonists of the receptor.