产品描述:
BIBP3226 is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y1 (Ki = 1.1 nM).{59929} It is selective for Y1 over Y2, Y4, and Y5 receptors (Kis = >1,000 nM for all). It also binds to neuropeptide FF receptor 1 (NPFF1) and NPFF2 (Kis = 108 and 79 nM, respectively) and reverses NPFF-induced inhibition of forskolin-induced cAMP accumulation in CHO cells expressing human NPFF2 in a concentration-dependent manner.{59929} BIBP3226 inhibits NPY-induced increases in perfusion pressure in isolated rat kidney but not the NPY-induced twitch response in isolated rat vas deferens (IC50s = 26 and >10,000 nM, respectively).{59930} BIBP3226 inhibits NPY-induced increases in blood pressure in pithed rats (ED50 = 0.11 mg/kg).{59930} It also inhibits NPFF-induced hypothermia in mice when administered intracerebroventricularly (i.c.v.) at a dose of 5 nmol.{59931}