TALIPEXOLE

Description

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.

Originator

Boehringer Ingelheim (Germany)

Definition

ChEBI: 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine is an azepine.

brand name

Domin