BIBP3226 is a nonpeptide antagonist of neuropeptide Y (NPY) receptor Y (K = 1.1 nM). It is selective for Y over Y, Y, and Y receptors (Ks = >1,000 nM for all). It also binds to neuropeptide FF receptor 1 (NPFF1) and NPFF2 (Ks = 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. BIBP3226 inhibits NPY-induced increases in perfusion pressure in isolated rat kidney but not the NPY-induced twitch response in isolated rat vas deferens (ICs = 26 and >10,000 nM, respectively). BIBP3226 inhibits NPY-induced increases in blood pressure in pithed rats (ED = 0.11 mg/kg). It also inhibits NPFF-induced hypothermia in mice when administered intracerebroventricularly (i.c.v.) at a dose of 5 nmol.
BIBP3226 is a potent and selective neuropeptide Y Y1 and neuropeptide FF receptor antagonist, with Kis of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 displays anxiogenic-like effect.
体内研究
BIBP3226 (0.5, 5 μg; i.c.v.; male Wistar rats) induces an anxiogenic-like effect at the higher dose.