Results 101 to 110 of about 2,118 (153)

Effect of Lipophilicity on the in vivo localization of radiolabelled spiperone analogues

International Journal of Nuclear Medicine and Biology, 1985
A 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
S M, Moerlein, P, Laufer, G, Stöcklin
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Multistep solution-Phase parallel synthesis of spiperone analogues

Bioorganic & Medicinal Chemistry Letters, 2000
A 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
H C, Hansen, R, Olsson, G, Croston, C M, Andersson   +3 more
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Effects of spiperone on feeding performance in a food preference test

Psychopharmacology, 1979
Spiperone 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 ...
S J, Cooper, K F, Sweeney, F M, Toates
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[3H]Spiperone binding to lymphocyte in extrapyramidal disease and in aging

Brain, Behavior, and Immunity, 1987
[3H]Spiperone binding to lymphocytes in Parkinson's disease (PD), Wilson's disease (WD), and age-matched control groups was studied. In the untreated PD group, [3H]spiperone binding was lower than in young controls, but did not differ from elderly healthy persons. After treatment with levodopa, the number of [3H]spiperone binding sites increased. In WD,
A, Członkowska, J, Jachowicz-Jeszka, A, Członkowski   +2 more
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Uptake of 77Br-spiperone in the striata of schizophrenic patients and controls

Nuclear Medicine Communications, 1986
Twelve 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 ...
J C, Crawley, T J, Crow, E C, Johnstone, S R, Oldland, F, Owen, D G, Owens, T, Smith, N, Veall, G D, Zanelli   +8 more
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Binding of 3H-spiperone to human lymphocytes: A biological marker in schizophrenia?

Psychiatry Research, 1985
The specific binding of the dopamine antagonist 3H-spiperone to lymphocytes from a healthy control group (n = 40), a group of acute, unmedicated schizophrenic patients (n = 27), and a psychiatric control group (n = 16) was investigated. There were no differences in binding parameters between the healthy controls (Bmax 2.6 +/- 0.7 fmoles/10(6) cells; Kd
Brigitta Bondy, M Ackenheil
exaly   +3 more sources

125I-spiperone: A novel ligand for D2 dopamine receptors

Life Sciences, 1984
125I-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.
A L, Gundlach, B L, Largent, S H, Snyder
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N-(3-[18F]fluoropropyl)-spiperone: The preferred 18F labeled spiperone analog for positron emission tomographic studies of the dopamine receptor

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology, 1988
The ligands currently used for PET studies of the dopamine receptor are fluorine-18-labeled spiperone (FSp) and carbon-11 or fluorine-18-labeled N-methyl-spiperone. All three of these ligands have drawbacks in either their chemical preparation or their biological behavior.
M.J. Welch, J.A. Katzenellenbogen, C.J. Mathias, J.W. Brodack, K.E. Carlson, D.Y. Chi, C.S. Dence, M.R. Kilbourn, J.S. Perlmutter, M.E. Raichle, M.M. Ter-Pogossian   +10 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, 1991
The 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.
F, Huguet, S, Chalon, D, Guilloteau, J C, Besnard   +3 more
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Effect of mazindol on brain dopamine turnover in spiperone-treated rats

Journal of Neural Transmission, 1979
Mazindol, 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.
R W, Fuller, H D, Snoddy
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