Hyperforin has been reported to be strongly involved in the pharmacological and clinical antidepressant activity of Hypericum perforatum L.
Hyperforin, as such, never got proposal for drug development due to its high chemical instability. The new hyperforin derivative named IDN 5491, has been selected as the most interesting candidate for pharmaceutical development among a wide number of compounds screened. Several preclinical pharmacological tests, performed in vitro and in vivo, demonstrated the great potential of IDN 5491 as an antidepressant agent endowed with a peculiar mechanism of action. The compound is well tolerated in preliminary toxicological studies.

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