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Panamesine

Panamesine
Panamesine.svg
Clinical data
SynonymsEMD-57455
Pharmacokinetic data
MetabolitesEMD-59983
Identifiers
CAS Number
PubChem CID
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H26N2O6
Molar mass426.469 g·mol−1
3D model (JSmol)

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]

See also

References

  1. ^ a b "Panamesine". AdisInsight.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.