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Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM. Preladenant also completely antagonizes cAMP in cells expressing the recombinant human A2A receptor.
Preladenant (1 mg/kg) inhibits L-Dopa-induced behavioral sensitization after repeated daily administration, which suggests a reduced risk of the development of dyskinesias. Preladenant exhibits antidepressant-like profiles in models of behavioral despair, namely the mouse tail suspension test and the mouse and rat forced swim test. Preladenant produces a dose-dependent reduction in parkinsonian scores at doses of 1 mg/kg (min score: 9.0) and 3 mg/kg (min score: 6.5). A subthreshold dose of Preladenant reduces minimum and mean parkinsonian scores in animals treated with 3 mg kg of L-Dopa to 5.25 and 6.88 respectively. A Wilcoxin test is used to compare individual treatments against vehicle. Preladenant (3 mg/kg), L-Dopa (3, 6, and 12 mg/kg), and the combination of Preladenant and L-Dopa (1 or 3 mg/kg+3 mg/kg) are all significantly improved on the minimum parkinsonian score. In addition, both the 12 mg/kg L-Dopa and L-Dopa+Preladenant groups are significantly improved on both minimum and mean parkinsonian scores relative to the 3 mg/kg L-Dopa group.
| Molecular Weight | 503.56 |
| Formula | C25H29N9O3 |
| CAS Number | 377727-87-2 |
| Solubility (25°C) | DMSO 2.5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Adenosine Receptor Products |
|---|
| CV1808
CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively. |
| FK 453
FK 453 is a potent and selective adenosine A1 receptor antagonist with an IC50 value of 17.2 nM. |
| GS-9667
GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). |
| PD81723
PD81723 is an adenosine receptor binding enhancer. |
| PSB-0788
PSB-0788 is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. |
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