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Panamesine
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Clinical data | |
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Other names | EMD-57455 |
Pharmacokinetic data | |
Metabolites | EMD-59983 |
Identifiers | |
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CAS Number | |
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ChEMBL | |
CompTox Dashboard (EPA) | |
Chemical and physical data | |
Formula | C23H26N2O6 |
Molar mass | 426.469 g·mol−1 |
3D model (JSmol) | |
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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. It is a selective antagonist of both sigma receptor subtypes, the σ1 and σ2 receptors (IC50 = 6 nM). 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. Panamesine reached phase II clinical trials for schizophrenia prior to the discontinuation of its development.
See also
σ1 |
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σ2 | |
Unsorted |
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See also: Receptor/signaling modulators |