Cutler, David L. published the artcileEvaluation of the effects of a high-fat meal on the oral bioavailability of a single dose of preladenant in healthy subjects, Name: 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, the publication is Journal of Clinical Pharmacology (2012), 52(11), 1698-1703, database is CAplus and MEDLINE.
The aim of this study was to evaluate the effect of food on the oral bioavailability of preladenant, a novel adenosine A2A receptor antagonist. This open-label, randomized, single-dose, 2-way crossover study evaluated the effects of a high-fat, high-calorie meal on the pharmacokinetics of preladenant and its metabolite (SCH434748) following oral administration of a single 25-mg preladenant capsule to 24 healthy subjects. When administered with food, the time of maximum concentration (Tmax) of preladenant was prolonged compared with administration in the fasting state. Whereas Tmax was increased from 0.9 h to 2.6 h and maximum concentration (Cmax) was decreased (from 212 ng/mL to 128 ng/mL), the extent of absorption (area under the plasma concentration-time curve from time 0 to time of final quantifiable sample, or AUC[tf]) was unaffected by the meal. Similarly, SCH434748 Tmax was prolonged in the fed state, and Cmax decreased from 43.7 ng/mL to 28.6 ng/mL. The assessment of AUC[tf] and area under the plasma concentration-time curve from time 0 to infinity [AUC[I]] together suggests that the AUC for the metabolite remained unchanged. No serious, significant, or unexpected adverse events occurred. In summary, food delays absorption and reduces peak exposure (Cmax) but does not alter the extent of preladenant exposure (AUC). These small changes are unlikely to be of clin. importance. A single 25-mg dose of preladenant is safe and well tolerated in healthy subjects under both fed and fasting conditions.
Journal of Clinical Pharmacology published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, Name: 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics