Panamesine (INN ; developmental code name EMD-57455) is a sigma receptor antagonist that was under development by Merck as a potential antipsychotic for the treatment of schizophrenia in the 1990s but was never marketed.[1] It is a selective antagonist of both sigma receptor subtypes, the σ1 and σ2 receptors (IC50 = 6 nM).[2][additional citation(s) needed] In addition, the major metabolite of the drug, EMD-59983, has high affinity for the sigma receptors (IC50 = 24 nM) and the dopamine D2 (IC50 = 23 nM) and D3 receptors, with potent antidopaminergic activity.[3][4][5] Panamesine reached phase II clinical trials for schizophrenia prior to the discontinuation of its development.[1]
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Other names | EMD-57455 |
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Metabolites | EMD-59983 |
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Formula | C23H26N2O6 |
Molar mass | 426.469 g·mol−1 |
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