BIBP3226

NPYY1的非肽拮抗剂(Ki=1.1nM)；对Y1受体具有选择性，优于Y2、Y4和Y5受体（所有受体的Kis=>1,000nM）；与NPFF1和NPFF2结合（Kis分别为108和79nM）并逆转NPFF诱导的对表达人NPFF2的CHO细胞中福斯高林诱导的环磷酸腺苷积累的抑制作用；抑制NPY诱导的大鼠离体肾脏灌注压升高(IC50s=26nM)；抑制NPY诱导的大鼠血压升高(ED50=0.11mg/kg)；在5nmol、icv浓度下抑制小鼠NPFF诱导的低温。A nonpeptide antagonist of NPY Y1 (Ki = 1.1 nM); selective for Y1 over Y2, Y4, and Y5 receptors (Kis = >1,000 nM for all); binds to NPFF1 and NPFF2 (Kis = 108 and 79 nM, respectively) and reverses NPFF-induced inhibition of forskolin-induced cyclic AMP accumulation in CHO cells expressing human NPFF2; inhibits NPY-induced perfusion pressure increases in isolated rat kidney (IC50s = 26 nM); inhibits NPY-induced increases in blood pressure in pithed rats (ED50 = 0.11 mg/kg); inhibits NPFF-induced hypothermia in mice at 5 nmol, i.c.v.分子式C27H31N5O3分子量473.6OC(C=C1)=CC=C1CNC([C@@H](CCCNC(N)=N)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O