| Id |
Subject |
Object |
Predicate |
Lexical cue |
| T1 |
0-112 |
Sentence |
denotes |
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease. |
| T2 |
113-254 |
Sentence |
denotes |
The in vivo characterization of a dual adenosine A(2A)/A(1) receptor antagonist in several animal models of Parkinson's disease is described. |
| T3 |
255-417 |
Sentence |
denotes |
Discovery and scale-up syntheses of compound 1 are described in detail, highlighting optimization steps that increased the overall yield of 1 from 10.0% to 30.5%. |
| T4 |
418-855 |
Sentence |
denotes |
Compound 1 is a potent A(2A)/A(1) receptor antagonist in vitro (A(2A) K(i) = 4.1 nM; A(1) K(i) = 17.0 nM) that has excellent activity, after oral administration, across a number of animal models of Parkinson's disease including mouse and rat models of haloperidol-induced catalepsy, mouse model of reserpine-induced akinesia, rat 6-hydroxydopamine (6-OHDA) lesion model of drug-induced rotation, and MPTP-treated non-human primate model. |
