Peer-reviewed veterinary case report
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2007
- Authors:
- Neustadt, Bernard R et al.
- Affiliation:
- Department of Chemical Research · United States
- Species:
- rodent
Abstract
Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A2A antagonist SCH 58261 as a starting point, we identified the potent and selective (vs. A1) antagonist 11h, orally active in the rat haloperidol-induced catalepsy model. We further optimized this lead to the methoxyethoxyethyl ether 12a (SCH 420814), which shows broad selectivity, good pharmacokinetic properties, and excellent in vivo activity.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/17236762/