Zetidoline (ZTD), a compound chemically unrelated to any available antipsychotic, with selective dopamine receptor-blocking properties, was compared with haloperidol (HLP) in a double-blind study on 56 in-patients who had either first episodes or acute relapses of schizophrenia. ZTD was found to be safe, as effective as HLP, and to produce significantly fewer extrapyramidal side-effects (EPS).
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http://dx.doi.org/10.1192/bjp.145.3.294 | DOI Listing |
Boll Chim Farm
September 1992
MMDRI, Lepetit Research Center, Gerenzano (VA), Italy.
A specific and sensitive assay is described. Zetidoline is extracted with ethyl ether from 1 ml of plasma or saliva added with the internal standard. The extract is carefully purified and injected into a gas chromatography-mass spectrometry system equipped with a crosslinked capillary column and operated in single ion monitoring mode by electron impact.
View Article and Find Full Text PDFPharmacol Biochem Behav
June 1991
Department of Experimental Psychology, Faculty of Medicine, F.N.D.P. Namur, Belgium.
It has been found that dopaminergic transmission could be involved in some aspects of anxiety. The present study aims to explore this hypothesis further, using specific DA1 (SKF 38393) and DA2 (bromocriptine) agonists or DA1 (SCH 23390), and DA2 (zetidoline) antagonists in the open-field test. The results confirm previous studies indicating that DA1 and DA2 agonists predominantly increase locomotor activity, while DA1 and DA2 antagonists predominantly decrease it.
View Article and Find Full Text PDFAct Nerv Super (Praha)
December 1989
Dept. of Psychiatry, Hradec Králové.
Act Nerv Super (Praha)
June 1989
Dept. of Psychiatry, Medical Faculty, Bratislava.
J Comput Aided Mol Des
March 1989
Laboratoire de Chimie Moléculaire Structurale, Facultés Universitaires Notre-Dame de la Paix, Namur, Belgium.
Molecular graphic design coupled with PCILO and crystallographic results have been used to investigate the three-dimensional structure of Tropapride, Piquindone, Zetidoline, and Metoclopramide, four dopamine D-2 receptor antagonists showing Na+-dependent binding. Three putative pharmacophoric elements, a nitrogen lone pair, a phenyl ring and a carbonyl moiety, are similarly oriented in all the Na+-dependent drugs. Conversely, for Na+-independent analogs, the two latter pharmacophoric elements play a subordinate role, but two pi-electron regions are systematically localized on the other side of the molecule: the first is a phenyl group while the second is a carbonyl function as in butyrophenones, a cyano group as in R48455, or a phenyl ring as in diphenylbutylpiperidines or tricyclics.
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