115689-52-6Relevant articles and documents
Dopamine Autoreceptor Agonists as Potential Antipsychotics. 3. 6-Propyl-4,5,5a,6,7,8-hexahydrothiazoloquinolin-2-amine
Caprathe, Bradley W.,Jaen, Juan C.,Wise, Lawrence D.,Heffner, Thomas G.,Pugsley, Thomas A.,et al.
, p. 2736 - 2746 (2007/10/02)
A series of rigid tricyclic analogues of the dopamine (DA) agonist PD 118440 was synthesized and evaluated for dopaminergic activity and DA autoreceptor selectivity. (R)-(+)-6-Propyl-4,5,5a,6,7,8-hexahydrothiazoloquinolin-2-amine ((+)-6) was identified as the most selective DA autoreceptor agonist from this group of compounds.It inhibited spontaneous locomotor activity (LMA) in rodents, reversed the γ-butyrolactone (GBL) induced accumulation of rat striatal DOPA and inhibited brain DA neuronal firing, all suggestive of direct DA autoreceptor agonist activity.However, (+)-6 is not completely free of postsynaptic DA activity, as evidenced by its stimulation of LMA in rats at high doses and its ability to produce stereotypy.On the other hand, (-)-6 appears to be a weak partial DA agonist with some effects on brain DA synthesis only at high doses.Like other DA autoreceptor agonists and DA antagonists, (+)-6 inhibited Sidman conditioned avoidance in squirrel monkeys, a test predictive of clinical antipsychotic activity.However, unlike classical antipsychotics, (+)-6 did not induce dystonias in haloperidol-sensitized squirrel monkeys, suggesting a minimal propensity toward extrapyramidal side effects (EPS).
HETERO [F] FUSED CARBOCYCLIC PYRIDINES AS DOPAMINERGIC AGENTS
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, (2008/06/13)
Hetero f! fused carbocyclic pyridines are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as dopamine agonists with selectivity for the presynaptic dopamine receptor and are useful as dopaminergi
