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An improved synthesis of (3-N-[11C]methyl)spiperone
International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes, 1986An improved radiochemical synthesis of (3-N-[11C]methyl) spiperone is reported. The radiotracer was prepared by N-alkylation of spiperone in dimethylformamide in the presence of equimolar aqueous tetrabutylammonium hydroxide and was purified by semi-preparative reversed phase high performance liquid chromatography (C-18 HPLC). The average radiochemical
Alan A. Wilson +3 more
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Effect of Lipophilicity on the in vivo localization of radiolabelled spiperone analogues
International Journal of Nuclear Medicine and Biology, 1985A series of N-alkylated and para-brominated analogues of spiperone were synthesized to ascertain the effect of lipophilicity on the in vivo localization of neuroleptics. While the IC50 for D2 receptor binding was within the same order of magnitude for these compounds, the calculated octanol-water partition coefficients varied 300-fold. When the in vivo
G. Stöcklin +2 more
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Spiperone: a receptor ligand and/or a granular uptake tracer?
International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology, 1991The accumulation of [3H]spiperone and [3H]dopamine was measured in striatum and pituitary gland slices of rat. Contrary to [3H]dopamine, [3H]spiperone storage was similar in striatum and pituitary gland. In addition, [3H]spiperone accumulation was not diminished by reserpine and tetrabenazine.
Sylvie Chalon +3 more
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125I-spiperone: A novel ligand for D2 dopamine receptors
Life Sciences, 1984125I-Spiperone binds with high affinity (KD 0.3 nM) to a single specific site (Bmax 34 pmol/g wet weight) in homogenates of rat corpus striatum. Specific binding is about 40-60 percent of total binding and is displaced stereo-specifically by butaclamol and clopenthixol.
Brian L. Largent +2 more
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Effects of spiperone on feeding performance in a food preference test
Psychopharmacology, 1979Spiperone reduced latency to feed and prolonged the total duration of feeding in a food-preference test in which novel and familiar foods were presented simultaneously to food-deprived rats. The increase in feeding duration could be accounted for in terms of an increase in time devoted to eating the novel foods, leaving the time devoted to eating the ...
Frederick Toates +2 more
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Uptake of 77Br-spiperone in the striata of schizophrenic patients and controls
Nuclear Medicine Communications, 1986Twelve patients with a diagnosis of schizophrenia and thirteen control subjects were injected with 77Br-bromospiperone and scanned using single photon emission tomography after 16 h. Although a statistically significant increase in patients by comparison with controls could be demonstrated, wide variations in specific activity of the ligand preclude a ...
Eve C. Johnstone +8 more
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Effect of mazindol on brain dopamine turnover in spiperone-treated rats
Journal of Neural Transmission, 1979Mazindol, an anorexic drug, caused a large increase in brain 3, 4-dihydroxyphenylacetic acid (DOPAC) concentration in spiperone-pretreated rats. The increase was dose-related over a 1--10 mg/kg dose range of mazindol and was maximum within 1 hour after maxzindol injection into rats pretreated 1 hour previously with spiperone.
H. D. Snoddy, R. W. Fuller
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[3H]spiperone binding in the nigrostriatal system in human brain
European Journal of Pharmacology, 1984The characteristics of [3H]spiperone binding in human brain were compared in three areas of the nigrostriatal pathway: areas containing the nerve terminals (caudate nucleus, putamen and pallidum); the area containing the cell bodies (substantia nigra pars compacta); the area containing the dendrites (pars reticulata).
Bokobza B +4 more
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Multistep solution-Phase parallel synthesis of spiperone analogues
Bioorganic & Medicinal Chemistry Letters, 2000A flexible, multistep parallel synthesis of spiperone analogues is described. A library of 4-substituted piperidines, assembled utilizing reductive amination and acylation protocols, was alkylated either homogeneously or heterogeneously, exploiting a product release only concept, to afford an oxa-series of spiperone analogues. Screening of the products
Glenn Croston +3 more
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Pharmacologic characterization of [3H]Dopamine and [3H]spiperone binding in mouse cerebellum
Neurochemistry International, 19921. [3H]Dopamine and [3H]spiperone binding to cerebellar homogenates was characterized utilizing dopaminergic agonists, antagonists and non-dopaminergic drugs. 2. The [3H]DA binding to low affinity binding sites reveals a heterogeneous population consisting of dopaminergic as well as serotonergic and noradrenergic sites.
N. Matsokis, N. Panagopoulos
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