[1] It is a partial agonist of benzodiazepine receptors and was shown in 1984 to possess both anxiolytic and sedative properties in humans but was never marketed.

It was also demonstrated that initial dosing with premazepam produces similar sedative effects as compared with diazepam, although psychomotor impairments are greater with premazepam than with diazepam after initial dosing.

However, with repeated dosing for more than one day premazepam causes less sedation and less psychomotor impairment than diazepam.

[2] Premazepam is a pyrrolodiazepine and acts as a partial agonist at benzodiazepine receptors.

Of the remaining 10% of the drug none of the metabolites showed any pharmacological activity.