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  • 1
    ISSN: 1432-2072
    Keywords: Key words EMD 57445 ; Sigma receptor ; Antipsychotic ; Dopamine receptor ; Iodobenzamide ; Single photon emission computed tomography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  Rationale: EMD 57445 (panamesine) is a high affinity sigma ligand with the profile of an atypical antipsychotic in animal studies. It has been reported recently to have antipsychotic activity in schizophrenia. However, its metabolite, EMD 59983, binds also to D2 and D3 dopamine (DA) receptors. Objectives: The aim of this study was to test, using single photon emission computed tomography (SPECT) and [123I]iodobenzamide (IBZM) as the radiotracer, whether EMD 59983 would pass the blood-brain barrier and to what extent it would contribute to the effects of EMD 57445 in schizophrenia. Methods: Two IBZM SPECT-scans were performed in five neuroleptic-free schizophrenic patients (DSM IV), one before and one after treatment with 60 mg panamesine daily for a treatment duration of 12–26 days. Results: A high occupancy of striatal D2-like DA receptors similar to that induced by typical neuroleptics was observed in all patients treated with EMD 57445. Conclusions: Our results suggest that a possible antipsychotic activity of EMD 57445 in schizophrenia is not necessarily attributable to its affinity for sigma receptors, but could be simply due to the potent antidopaminergic effects of EMD 59983, its main metabolite.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 1999 (1999), S. 2277-2281 
    ISSN: 1434-1948
    Keywords: Boron ; Iron ; Nickel ; Carbyne complexes ; Chemistry ; General Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The μ3-boryloxycarbyne complexes [{Fe(CO)3}3{μ3-COBCl{NtBu(SiMe3)}}2] (1) and [{(η5-C5H5)Ni}3{μ3-COBX(NR2)}μ3-CO] (2a: NR2 = NtBu(SiMe3), × = Cl; 2b: NR2 = N(SiMe3)2, × = Cl; 2c: NR2 = NMe2, × = BNMe2Cl) were obtained by reaction of the anionic complexes K2[{Fe(CO)3}3{μ3-CO}2] and K[{(η5-C5H5)Ni(CO)] with the corresponding chloroboranes Cl2BNR2 {NR2 = NtBu(SiMe3), N(SiMe3)2}, or 1,2-dichlorodiboranes(4) B2(NMe2)2Cl2, respectively. The products are formed by a nucleophilic attack of the CO oxygen atom at the boron centres with subsequent salt elimination. All compounds were characterized by IR and multinuclear NMR spectroscopy, and the structures of 1 and 2c in the solid state were determined by single-crystal X-ray diffraction studies.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 1998 (1998), S. 291-293 
    ISSN: 1434-1948
    Keywords: Boron ; Iron ; Boryl complexes ; η1-Coordinated borazine ; Chemistry ; General Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: A series of η1-borazine complexes were obtained by the reaction of trichloroborazine with Na[(η5-C5R5)Fe(CO)2]. The compounds [{(C5R5)(CO)2Fe}nCl3-nB3N3H3] (1a, n = 1, R = Me; 1b, n = 2, C5R5 = C5H4Me; 1c, n = 3, R = H) have one to three iron-boron σ bonds and Fe-B π-interactions can be ruled out from the spectroscopic and structural results. All new borazine complexes were isolated as orange crystalline solids and characterized by multinuclear NMR methods and IR spectroscopy. The structure of 1b in the crystalline state was also determined by a single-crystal X-ray study.
    Type of Medium: Electronic Resource
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