ORG-12962
Chemical compound
From Wikipedia, the free encyclopedia
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.[1][2]
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| Other names | ORG12962 |
| Routes of administration | Unknown[1] |
| Drug class | Serotonin 5-HT2 receptor agonist; Serotonin 5-HT2C receptor agonist; Serotonin 5-HT2A receptor agonist |
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| Formula | C10H11ClF3N3 |
| Molar mass | 265.66 g·mol−1 |
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It acts preferentially as a partial agonist of the serotonin 5-HT2C receptor (Ki = 12 nM; EC50 = 97.7 nM; Emax = 62%).[3][4][5] However, to a lesser extent, it is also a partial agonist of the serotonin 5-HT2A receptor (Ki = 65 nM; EC50 = 417 nM; Emax = 54%) and of the serotonin 5-HT2B receptor (EC50 = 525 nM; Emax = 41%).[3][4] In addition, ORG-12962 shows affinity for other serotonin receptors, such as the serotonin 5-HT1B receptor (Ki = 100 nM) and to a much lesser extent the serotonin 5-HT1A receptor (Ki = 2,500 nM).[5]
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.[4][6]
ORG-12962 was first described in the scientific literature by 1995.[7][8] It was developed by Organon.[1][2] The drug reached phase 2 clinical trials for depression prior to the discontinuation of its development.[1][2]