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Clinical data | |
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Other names | EMD-57455 |
Pharmacokinetic data | |
Metabolites | EMD-59983 |
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Chemical and physical data | |
Formula | C23H26N2O6 |
Molar mass | 426.469 g·mol |
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Panamesine (INNTooltip International Nonproprietary Name; 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※
References※
- ^ "Panamesine". AdisInsight.
- ^ Guitart X, "Codony X," Monroy X (2004). "Sigma receptors: biology and therapeutic potential". Psychopharmacology. 174 (3): 301–19. doi:10.1007/s00213-004-1920-9. PMID 15197533. S2CID 23606712.
- ^ Frieboes RM, "Murck H," Wiedemann K, Holsboer F, Steiger A (1997). "Open clinical trial on the sigma ligand panamesine in patients with schizophrenia". Psychopharmacology. 132 (1): 82–8. doi:10.1007/s002130050323. PMID 9272763. S2CID 20525608.
- ^ Huber MT, Gotthardt U, Schreiber W, Krieg JC (1999). "Efficacy and safety of the sigma receptor ligand EMD 57445 (panamesine) in patients with schizophrenia: an open clinical trial". Pharmacopsychiatry. 32 (2): 68–72. doi:10.1055/s-2007-979194. PMID 10333165. S2CID 12424244.
- ^ Gründer G, Müller MJ, Andreas J, Heydari N, Wetzel H, Schlösser R, Schlegel S, Nickel O, Eissner D, Benkert O (1999). "Occupancy of striatal D(2)-like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic". Psychopharmacology. 146 (1): 81–6. doi:10.1007/s002130051091. PMID 10485968. S2CID 7039752.
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