46415-29-6Relevant academic research and scientific papers
Potent, selective, and orally active adenosine A2A receptor antagonists: Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines
Neustadt, Bernard R.,Hao, Jinsong,Lindo, Neil,Greenlee, William J.,Stamford, Andrew W.,Tulshian, Deen,Ongini, Ennio,Hunter, John,Monopoli, Angela,Bertorelli, Rosalia,Foster, Carolyn,Arik, Leyla,Lachowicz, Jean,Ng, Kwokei,Feng, Kung-I
, p. 1376 - 1380 (2008/02/05)
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 11 h, 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.
Pyrrolo-pyridine derivatives
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, (2008/06/13)
A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D 4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia while manifesting fewer side-effects than those associated with classical neuroleptic drugs.
