eptapirone
Sign in to saveEptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family. Its affinity for the 5-HT1A receptor was reported to be 4.8 nM (Ki) (or 8.33 (pKi)), and its intrinsic activity approximately equal to that of serotonin (i.e., 100%).
Wikidata facts
- Mass
- 345.191
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- chemical formula
- C₁₆H₂₃N₇O₂
- canonical SMILES
- CN1C(=O)C=NN(C1=O)CCCCN2CCN(CC2)C3=NC=CC=N3
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4 sectionsContents
- Animal studies
- Human studies
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- References
Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family. Its affinity for the 5-HT1A receptor was reported to be 4.8 nM (Ki) (or 8.33 (pKi)), and its intrinsic activity approximately equal to that of serotonin (i.e., 100%).
Eptapirone and related high-efficacy 5-HT1A full and super agonists such as befiradol and F-15,599 were developed under the hypothesis that the maximum exploitable therapeutic benefits of 5-HT1A receptor agonists might not be able to be seen without the drugs employed possessing sufficiently high intrinsic activity at the receptor. As 5-HT1A 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-HT1A receptor agonists like buspirone and tandospirone, which act merely as weak-to-moderate partial agonists of the receptor.