ORG-12962
ORG-12962 is a serotonin 5-HT2 receptor agonist of the pyridinylpiperazine family which was under development for the treatment of major [depressive disorder] but was never marketed.
It acts preferentially as a partial agonist of the serotonin 5-HT2C receptor. However, to a lesser extent, it is also a partial agonist of the serotonin 5-HT2A receptor and of the serotonin 5-HT2B receptor. In addition, ORG-12962 shows affinity for other serotonin receptors, such as the serotonin 5-HT1B receptor and to a much lesser extent the serotonin 5-HT1A receptor.
In addition to depression, it was studied as a potential anxiolytic, but was discontinued from human trials after tests in a public speaking challenge showed that its anti-anxiety effects were accompanied by side effects such as dizziness and a "spacey" feeling, which were attributed as being possibly due to poor selectivity in vivo over the hallucinogenic serotonin 5-HT2A receptor.
ORG-12962 was first described in the scientific literature by 1995. It was developed by Organon. The drug reached phase 2 clinical trials for depression prior to the discontinuation of its development.