Chemistry:Panamesine
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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.[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]
CNS review:[6]
See also
References
- ↑ 1.0 1.1 "Panamesine". AdisInsight. http://adisinsight.springer.com/drugs/800001428.
- ↑ "Sigma receptors: biology and therapeutic potential". Psychopharmacology 174 (3): 301–19. 2004. doi:10.1007/s00213-004-1920-9. PMID 15197533.
- ↑ "Open clinical trial on the sigma ligand panamesine in patients with schizophrenia". Psychopharmacology 132 (1): 82–8. 1997. doi:10.1007/s002130050323. PMID 9272763.
- ↑ "Efficacy and safety of the sigma receptor ligand EMD 57445 (panamesine) in patients with schizophrenia: an open clinical trial". Pharmacopsychiatry 32 (2): 68–72. 1999. doi:10.1055/s-2007-979194. PMID 10333165.
- ↑ "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. 1999. doi:10.1007/s002130051091. PMID 10485968.
- ↑ "EMD 57445: A Selective Sigma Receptor Ligand with the Profile of an Atypical Neuroleptic". CNS Drug Reviews 2 (2): 175–194. June 1996. doi:10.1111/j.1527-3458.1996.tb00296.x.
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