Ketanserin and Spiperone as Templates for Novel Serotonin 5-HT2A Antagonists
Current Topics in Medicinal Chemistry, 2002The structures of ketanserin (1) and spiperone (2) were examined in detail to determine the role of various substituent groups on 5-HT(2A) receptor affinity and selectivity. It was found that the presence of the quinazoline ring of ketanserin detracts from selectivity and that various ring-opened analogs displayed ketanserin-like affinity and up to 30 ...
Richard A, Glennon +7 more
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Hyperprolactinaemia does not alter specific striatal 3H-spiperone binding in the rat
Biochemical Pharmacology, 1986We have investigated the effect of single injections (1 mg/animal i.v.) of prolactin or vehicle, and repeated depot (0.125-1.0 mg/animal/day) or bolus (1.0 mg/animal/day) administration of prolactin or vehicle for 6 days to adult male rats. The density (Bmax) and affinity (Kd) of specific striatal [3H]spiperone binding was not changed by any of the ...
M D, Simpson, P, Jenner, C D, Marsden
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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
S M, Moerlein, P, Laufer, G, Stöcklin
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Potentiation of spiperone-induced oral activity in rats after neonatal 6-hydroxydopamine
Pharmacology Biochemistry and Behavior, 1991The influence of central dopaminergic fibers on drug-induced oral activity in rats has not been well studied. Rats were treated 3 days after birth with bilateral intracerebroventricular 6-hydroxydopamine (6-OHDA; 134 micrograms total, base form) to destroy dopaminergic fibers in the brain. Control rats received vehicle by the same route.
Kostrzewa, Richard M., Hamdi, Anwar
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Estrogen increases both spiperone-induced catalepsy and brain levels of [3H]spiperone in the rat
Brain Research, 1979L A, Chiodo, A R, Caggiula, C F, Saller
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Why does 4′‐nitro‐spiperone fail as precursor for the preparation of [F‐18]‐spiperone?
Journal of Labelled Compounds and Radiopharmaceuticals, 1989M. Gvsemans, J. Mertens, W. Vanryckeghem
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Spiperone-labelled dopamine transporter in lymphocytes
European Neuropsychopharmacology, 1992B. Bondy +3 more
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Elevated lymphocyte spiperone binding: A vulnerability factor for affective psychosis?
Biological Psychiatry, 1997R, Fartaçek +4 more
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Spiperone: A ligand of choice for neuroleptic receptors
Biochemical Pharmacology, 1978Josée E. Leysen +2 more
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Spiperone Binding in Lymphocytes: Part of a Dopamine Uptake System?
Annals of the New York Academy of Sciences, 1992B, Bondy, M, Ackenheil, T, Ruppert
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