Adenosine A2A receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
A receptor antagonist, adenosine technology, applied in the field of adenosine A2a receptor antagonists, can solve the problems of undiagnosed and rarely active treatment
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[0382] A population of seven capuchin monkeys previously sensitive to the chronic effects of haloperidol showed EPS when given haloperidol (0.3 mg / kg, p.o.) rapidly. Compound A was administered orally (p.o.) at a dose of 0.3 to 30 mg / kg in combination with haloperidol. Compound B was administered orally (p.o.) at a dose of 3 to 100 mg / kg in combination with haloperidol. These studies were conducted using a within-subjects design such that each monkey received all 6 treatments (vehicle and 5 doses of Compound A) in a crossover, balanced design. In all of these studies, the group of seven monkeys showed baseline levels of EPS when receiving haloperidol.
[0383] Compound A produced a dose-dependent reduction in the maximum EPS score ( Figure 1A ), and a dose-dependent delay in the onset of EPS ( Figure 1B ). Compound A at a dose of 1 mg / kg prevented EPS onset in one monkey and delayed EPS onset by 1 hour. Compound A at a dose of 3 mg / kg prevented the onset of EPS in two m...
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Application Information
- IPC
- A61K45/06
- CPC
- A61K31/519; A61K31/522; A61K31/551; A61K31/5513; A61K45/06; A61P21/02; A61P25/02; A61P25/16
- Inventors
- M·格兹拉克; J·杭特