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Spiperone: Tritium labelling at high specific activity

Applied Radiation and Isotopes, 2019
An efficient method is described to tritiate spiperone at high specific activity.
Crist Filer
exaly   +3 more sources

3H-spiperone labels sigma receptors, not dopamine D2 receptors, in rat and human lymphocytes

open access: yesImmunopharmacology, 1991
3H-Spiperone binds to dopamine D2 receptors in striatum and, under the assumption that it labels the same receptors in lymphocytes, this binding site has been suggested as a biological marker for schizophrenia.
Teresa Coccini, Luigi Manzo, L Manzo
exaly   +1 more source

Taurine interferes with spiperone binding in the striatum

Neuroscience, 1986
The effects of taurine and its structural analogues and two new anticonvulsant derivatives, taltrimide and MY-103, on the function of brain dopaminergic systems were studied by assessing their interference with the binding of [3H]spiperone to synaptic membranes isolated from rat striata. Two populations of binding sites were detected.
P, Kontro, S S, Oja
openaire   +2 more sources

Methodology of 3H-spiperone binding to lymphocytes

Journal of Psychiatric Research, 1990
Alterations in lymphocyte binding capacity for the dopamine antagonist 3H-spiperone may be of great interest in psychiatric and neurological disorders: an increase in capacity noted in lymphocytes of schizophrenic patients and their families may well turn out to be a phenotypic vulnerability marker. Since the 3H-spiperone binding assay with lymphocytes
B, Bondy, M, Ackenheil, R R, Engel
openaire   +2 more sources

Uptake of 3H-spiperone by lymphocytes in schizophrenia

Journal of Psychiatric Research, 1989
Uptake of 3H-spiperone into lymphocytes obtained from control subjects (N = 22), chronic schizophrenics (N = 20), relatives with psychiatric disorder (N = 11) and unaffected relatives (N = 17) was studied. No differences were observed in spiperone uptake among any of the groups examined.
S, Itzchaky, B, Lerer, R P, Ebstein
openaire   +2 more sources

Effect of Chronic Sulpiride on Striatal Spiperone Binding

International Pharmacopsychiatry, 2017
Increased ^3 H-spiperone binding after chronic neuroleptic treatment has been proposed as a molecular model of tardive dyskinesia. Sulpiride has been claimed to be an atypical neuroleptic that might not produce tardive dyskinesia. The effect of chronic sulpiride was, therefore, compared to that of chronic haloperidol on striatal ^3 H-spiperone binding.
J, Bannet   +3 more
openaire   +2 more sources

A study of the kinetics of the interaction of spiperone with binding sites on human mononuclear cells: existence of a heterogeneous population of spiperone binding sites

Journal of Neuroimmunology, 1992
The kinetics and equilibrium of the interaction of [3H]spiperone with binding sites on human mononuclear cells were studied using a competitive displacement of spiperone by ketanserin, sulpiride, haloperidol, (+)- and (-)-butaclamol. [3H]Spiperone binding sites on human mononuclear cells were shown to be not of the D2, but most probably of the 5-HT2 ...
S V, Zaitsev   +3 more
openaire   +2 more sources

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
openaire   +2 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
openaire   +2 more sources

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