Abstract | RATIONALE: OBJECTIVES: The aim of this study was to test, using single photon emission computed tomography (SPECT) and [(123)I]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: RESULTS: A high occupancy of striatal D(2)-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.
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Authors | G Gründer, M J Müller, J Andreas, N Heydari, H Wetzel, R Schlösser, S Schlegel, O Nickel, D Eissner, O Benkert |
Journal | Psychopharmacology
(Psychopharmacology (Berl))
Vol. 146
Issue 1
Pg. 81-6
(Sep 01 1999)
ISSN: 0033-3158 [Print] Germany |
PMID | 10485968
(Publication Type: Journal Article)
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Chemical References |
- Antipsychotic Agents
- Benzamides
- Oxazoles
- Piperidines
- Pyrimidines
- Pyrrolidines
- Receptors, Dopamine D2
- Receptors, sigma
- panamesine
- alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol
- 3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide
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Topics |
- Adult
- Antipsychotic Agents
(metabolism)
- Benzamides
(metabolism)
- Blood-Brain Barrier
- Corpus Striatum
(metabolism)
- Female
- Humans
- Male
- Middle Aged
- Oxazoles
(metabolism, pharmacology)
- Piperidines
(metabolism, pharmacology)
- Pyrimidines
(pharmacology)
- Pyrrolidines
(metabolism)
- Receptors, Dopamine D2
(metabolism)
- Receptors, sigma
(metabolism)
- Schizophrenia
(drug therapy)
- Tomography, Emission-Computed, Single-Photon
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