Domin was launched in Japan for Parkinson's disease. The compound is
readily accessible in two steps from I-allylhexahydro-4H-azepin4-one. Its
antiparkinson activity resides in the fact that talipexole is a selective agonist for
presynaptic dopamine D2 receptors with no D1 receptor activity. It is a clonidine-like α2-adrenoreptor agonist and has fewer GI side effects than bromocriptine the most
widely used dopamine angonist. Also it is 70 times more potent than bromocriptine
and has a more rapid onset of action. In addition to its anti-tremor activity there was
a sedative effect but no emesis. The latter probably a result of talipexole's 5-HT3
receptor antagonistic activity. Its metabolites have no biological activity, there was
no development of tolerence and its effect could be enhanced by L-dopa.
Boehringer Ingelheim (Germany)
ChEBI: 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine is an azepine.
