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Occupancy of striatal D2-like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic (1999)

Gründer, G. ; Müller, Matthias J. ; Andreas, Jörg ; [et al.]

Springer

Psychopharmacology 146 (1999), S. 81-86

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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

URL: http://dx.doi.org/10.1007/s002130051091

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Protolysis of Tri-tert-butylazadiboriridine: Formation of a B-H-B Bridge in Unusual Coordination (1995)

Müller, Matthias ; Eversheim, Ellen ; Englert, Ulli ; [et al.]

Weinheim : Wiley-Blackwell

Berichte der deutschen chemischen Gesellschaft 128 (1995), S. 99-103

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ISSN: 0009-2940

Keywords: Tri-tert-butylazadiboriridine ; (Hydroboryl)(methoxyboryl)amine ; 2,3-μ-Hydro-1,2,3-azoniadiborata-l-cyclopropenes ; Chemistry ; Inorganic Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The B—B bond of tri-tert-butylazadiboriridine [—NR—BR—BR—] (R = tBu; 1) is oxidized by MeOH to give the (hydroboryl)(methoxyboryl)amine H—BR=NR-BR(OMe) (2a). μ-2,3-Hydroazoniadiborata-1-cyclopropenes [=NR—BR(X)—μH—BR=] (3a, 3c-e) are formed by the action of the acids HX upon 1. A similar hydrogen bridge as in 3a-e is formed during the hydroboration of 1 by catecholborane, yielding 3f. A B atom is identified in the products 3a-f to be planarly coordinated by four atoms, two of which are forming a BHB three-center bond with that B atom. This is a novel bonding situation in boron chemistry. The structures of the products are deduced from 1H-, 11B-, and 13C-NMR spectra and are confirmed by X-ray structural analyses of 2a, 3a, and 3c.

Additional Material: 2 Tab.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1002/cber.19951280203

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Synthesis and Structure of Trinuclear Boryloxycarbyne Complexes (1999)

Braunschweig, Holger ; Kollann, Carsten ; Koster, Margot ; [et al.]

Weinheim : Wiley-Blackwell

Berichte der deutschen chemischen Gesellschaft 1999 (1999), S. 2277-2281

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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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Synthesis and Structure of the First η1-Borazine Complexes (1998)

Braunschweig, Holger ; Kollann, Carsten ; Müller, Matthias

Weinheim : Wiley-Blackwell

Berichte der deutschen chemischen Gesellschaft 1998 (1998), S. 291-293

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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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Einbau eines Elements der ersten Achterperiode in die Brücke eines gespannten Metallocenophans: Synthese eines borverbrückten [1]FerrocenophansH. B. dankt der Deutschen Forschungsgemeinschaft (DFG) und dem Fonds der Chemischen Industrie für finanzielle Unterstützung. M. M. dankt der DFG für ein Stipendium und Prof. K. Prout für Unterstützung. I. M. dankt dem von der American Chemical Society verwalteten Petroleum Research Fund (PRF) für finanzielle Unterstützung, dem kanadischen Natural Sciences and Engineering Research Council (NSERC) für Stipendien (D. P. G. und P. N.) sowie der Alfred-P.-Sloan Foundation, der NSERC und der Universität Toronto für Stipendien (1997). (1997)

Braunschweig, Holger ; Dirk, Regina ; Müller, Matthias ; [et al.]

Weinheim : Wiley-Blackwell

Zeitschrift für die chemische Industrie 109 (1997), S. 2433-2435

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ISSN: 0044-8249

Keywords: Bor ; Eisen ; Metallocenophane ; Ringöffnungspolymerisation ; Sandwichkomplexe ; Chemistry ; General Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Additional Material: 2 Ill.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1002/ange.19971092114

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Incorporation of a First Row Element into the Bridge of a Strained Metallocenophane: Synthesis of a Boron-Bridged [1]FerrocenophaneH. B. thanks the Deutsche Forschungsgemeinschaft (DFG) and the Fonds der Chemischen Industrie for financial support of this work. M. M. gratefully acknowledges a scholarship from the DFG and thanks Prof. K. Prout for his support. I. M. thanks the donors of the Petroleum Research Fund (PRF), administered by the American Chemical Society, for financial support of this work, the Natural Sciences and Engineering Research Council of Canada (NSERC) for a Graduate Student Fellowship for D. P. G. and a Postdoctoral Fellowship for P. N. the Alfred P. Sloan Foundation for a Research Fellowship (1994-1998), NSERC for an E. W. R. Steacie Fellowship (1997-98), and the University of Toronto for a McLean Fellowship (1997). (1997)

Braunschweig, Holger ; Dirk, Regain ; Müller, Matthias ; [et al.]

Weinheim : Wiley-Blackwell

Angewandte Chemie International Edition in English 36 (1997), S. 2338-2340

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ISSN: 0570-0833

Keywords: boron ; iron ; metallocenophanes ; ring-opening polymerization ; sandwich complexes ; Chemistry ; General Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Additional Material: 2 Ill.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1002/anie.199723381

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