M40 (trifluoroacetate salt)

GAL1和GAL2受体调节剂（Kis分别为2.4和4.07nM）；对GAL1和GAL2具有选择性，优于GAL3（Ki=288nM）；诱导表达人类GAL2受体的CHO细胞中的肌醇磷酸积累（EC50=16.2nM）；在10或100nM时抑制福斯高林诱导的RIN-m5F细胞中的cAMP积累；在9.36nmol/只、icv时逆转甘丙肽诱导的对东莨菪碱诱导的海马ACh释放的抑制；减少甘丙肽诱导的大鼠食物摄入量增加；在30nmol/kg时改善心脏功能并减少持续冠状动脉结扎诱发的心力衰竭模型中的心脏纤维化；以20µg/只的剂量服用，可增加性欲低下的雄性小鼠的插入频率和射精潜伏期。A GAL1 and GAL2 receptor modulator (Kis = 2.4 and 4.07 nM, respectively); selective for GAL1 and GAL2 over GAL3 (Ki = 288 nM); induces inositol phosphate accumulation in CHO cells expressing the human GAL2 receptor (EC50 = 16.2 nM); inhibits forskolin-induced cAMP accumulation in RIN-m5F cells at 10 or 100 nM; reverses galanin-induced inhibition of scopolamine-induced hippocampal ACh release in conscious rats at 9.36 nmol/animal, i.c.v.; reduces galanin-induced increases in food intake in rats; improves cardiac function and decreases cardiac fibrosis in a rat model of heart failure induced by sustained coronary artery ligation at 30 nmol/kg; increases the intromission frequency and ejaculation latency in sexually sluggish male mice at 20 µg/animal.分子式C94H145N23O24 • XCF3COOH分子量1981.3[H]NCC(N[C@H](C(N[C@]([C@@H](C)O)([H])C(N[C@@H](CC(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H](CO)C(N[C@H](C(NCC(N[C@H](C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(NCC(N1CCC[C@H]1C(N2CCC[C@H]2C(N3CCC[C@H]3C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)C)=O)=O)C)=O)=O)C)=O)=O)=O)=O)=O)=O)=O)CC4=CC=C(O)C=C4)=O)=O)C)=O)=O)=O)=O)=O)CC5=CNC6=C5C=CC=C6)=O.O=C(O)C(F)(F)F