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  • 1
    ISSN: 1432-2072
    Keywords: Striatum ; Dopamine receptor ; Positron emission tomography ; Prolactin ; Neuroleptics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The percentage occupation of striatal dopamine D2 receptors has been evaluated in 25 patients using76Br-bromospiperone positron emission tomography (PET) and prolactin plasma levels (PRL) during oral neuroleptic treatment (11 studies), 1–90 days following discontinuation of such treatment (16 studies), and 1–120 days after last intramuscular administration of depot neuroleptics (nine studies). The PET-estimated occupation was highly significantly correlated in a sigmoîd-like fashion to the logarithm of the chlorpromazine-equivalent dose of oral neuroleptics (suggesting a strict dose-occupation relationship during oral neuroleptic treatment and supporting the D2-mediated hypothesis of neuroleptic action), while PRL was weakly related to daily dosage. Following withdrawal, return to normal receptor availability, as estimated by PET, occurred within 5–15 days (suggesting that protracted effects of neuroleptics after withdrawal are not due to sustained D2 receptor occupation), but PRL values fell even more rapidly. Efficient treatment with depot neuroleptics resulted in marked PET-estimated D2 receptor occupation, stable over the whole 4-week drug-administration interval, suggesting that longer intervals could be appropriate; PRL values bore no relationship to PET-estimated occupation, indicating variable intersubject tolerance to neuro-endocrine dopamine blockade. Overall, PET was much more sensitive than PRL to estimate striatal D2 receptor occupation in vivo.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of nuclear medicine 16 (1990), S. 817-835 
    ISSN: 1619-7089
    Keywords: Radioligand receptor binding ; PET ; SPET ; Emission computerized tomography ; Psychiatric illness ; Neurological illness
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In the past two decades, tritiated radioligand receptor binding, a tool commonly used to investigate the site of action of drugs in laboratory animals, has provided a vast body of information on neuropharmacology and neurobiology. Several neurological and psychiatric diseases have been related to neurotransmitter and receptor disorders. In order to study ligand interactions with receptors in vivo in humans, new tracers capable of carrying aγ-emitting radionuclide to the receptor have been designed. Emission computerized tomography (ECT) techniques such as positron (PET) or single photon emission tomography (SPET) allow monitoring of the time-course of regional tissue concentration of these radiolabelled ligands. PET and SPET each have their inherent advantages and drawbacks. The cyclotron-based technology of PET is a demanding and expensive technique that, to date, is still mainly reserved for research purposes. It is hoped that once the scientific basis of a physiopathological study is established using PET, diagnostic information might be provided by the more readily available SPET technology. The purpose of this article is to review the current state of receptor-bindingγ-emitting radioligands and to present the clinical potential of these new kinds of radiopharmaceuticals in clinical investigation.
    Type of Medium: Electronic Resource
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