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 (Ki = 12nM; = 97.7nM; = 62%). However, to a lesser extent, it is also a partial agonist of the serotonin 5-HT2A receptor (Ki = 65nM; = 417nM; = 54%) and of the serotonin 5-HT2B receptor ( = 525nM; = 41%). In addition, ORG-12962 shows affinity for other serotonin receptors, such as the serotonin 5-HT1B receptor (Ki = 100nM) and to a much lesser extent the serotonin 5-HT1A receptor (Ki = 2,500nM).
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.Connell, J., Sennef, C., & Deakin, J. F. W. (1999). The effects of ORG 12962, 5-HT2C receptor agonist, in two models of experimentally induced anxiety in healthy female volunteers. International Journal of Neuropsychopharmacology, 2, S136–S137. https://scholar.google.com/scholar?cluster=2357514178179946021
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.
See also Substituted piperazine 2C-B-PP 2,3-Dichlorophenylpiperazine 3-Chloro-4-fluorophenylpiperazine CPD-1 ORG-37684 Quipazine
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