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In synaptic plasma membranes of rat striatum, activation of dopamine receptors stimulates a high affinity GTPase activity. The rank order of potency of various dopamine receptor agonists in increasing GTP hydrolysis is the following: (-)-propylnorapomorphine greater than (-)-apomorphine = (+/-)-2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene [(+/-)-A-6,7-DTN] greater than dopamine = LY 171555 greater than noradrenaline. The selective D-1 dopamine receptor agonist, SKF 38393, does not produce a significant increase in GTP hydrolysis.
View Article and Find Full Text PDFZetidoline blocks dopamine autoreceptors in the rat substantia nigra.
Neuropharmacology
January 1985
Zetidoline, applied microiontophoretically onto neurones in the substantia nigra, zona compacta of anaesthetized rats, reversibly blocked the depressant effect of iontophoretically-applied dopamine. The inhibitory actions of gamma-aminobutyric acid (GABA) and glycine and the excitatory action of glutamate were unaffected by the antagonist. Zetidoline applied by bath perfusion, was similarly an antagonist of the inhibitory effect of bath applications of dopamine on neurones in the zona compacta of slices of substantia nigra; the pA2 for zetidoline in this preparation was 7.
View Article and Find Full Text PDFZetidoline, a new antipsychotic. First controlled trial in acute schizophrenia.
Br J Psychiatry
September 1984
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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