Dopamine autoreceptor agonists as potential antipsychotics. 3. 6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine was written by Caprathe, Bradley W.;Jaen, Juan C.;Wise, Lawrence D.;Heffner, Thomas G.;Pugsley, Thomas A.;Meltzer, Leonard T.;Parvez, Masood. And the article was included in Journal of Medicinal Chemistry in 1991.Synthetic Route of C9H10ClNO This article mentions the following:
A series of rigid tricyclic analogs of the dopamine (DA) agonist 4-(1,2,5,6-tetrahydro-1-propyl-3-pyridinyl)-2-thiazolamine was synthesized and evaluated for dopaminergic activity and DA autoreceptor selectivity. (R)-(+)-6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine [(+)-I] 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 induced accumulation of rat striatal DOPA and inhibited brain DA neuronal firing, all suggestive of direct DA autoreceptor agonist activity. However, (+)-I 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, (-)-I 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, (+)-I inhibited Sidman conditioned avoidance in squirrel monkeys, a test predictive of clin. antipsychotic activity. However, unlike classical antipsychotics, (+)-I did not induce dystonias in haloperidol-sensitized squirrel monkeys, suggesting a minimal propensity toward extrapyramidal side effects. In the experiment, the researchers used many compounds, for example, 6,7-Dihydroisoquinolin-8(5H)-one hydrochloride (cas: 135311-97-6Synthetic Route of C9H10ClNO).
6,7-Dihydroisoquinolin-8(5H)-one hydrochloride (cas: 135311-97-6) belongs to isoquinoline derivatives. The isoquinoline structure occurs in a considerable number of alkaloids in widely separated plant families. Most traditional methods of generating isoquinoline do so via oxidative aromatization of dihydro- or tetrahydro-isoquinolines, usually offering some environmental or economic advantage.Synthetic Route of C9H10ClNO
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem