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ORG-12962

Chemical compound

Chemical compound

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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; EC50 = 417nM; = 54%) and of the serotonin 5-HT2B receptor (EC50 = 525nM; Emax = 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.

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.

References

References

  1. (22 January 2007). "ORG 12962".
  2. (17 January 2026). "Delving into the Latest Updates on Org-12962 with Synapse".
  3. (September 1999). "Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells". [[British Journal of Pharmacology]].
  4. (July 2006). "5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents". J Med Chem.
  5. (2008). "5-HT2C ligands: recent progress". Progress in Medicinal Chemistry.
  6. 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
  7. Price, Gary W. (1995). "Meeting Highlights: 3rd IUPHAR Satellite Meeting on Serotonin July 30 - August 3 1994, Chicago, USA: Serotonin 94". Expert Opinion on Investigational Drugs.
  8. Kerrigan, Frank. (1998). "Antidepressant patents: 1995 - 1997". Expert Opinion on Therapeutic Patents.
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