Lorcaserin HCl846589-98-8赫澎生物說明書
發(fā)布時(shí)間：2016-09-13瀏覽次數(shù)：1160返回列表
| Lorcaserin HCl 分子式：C11H14ClN.HCl 分子量：232.15 產(chǎn)品描述 Lorcaserin HCl是一種選擇性的人源5-HT2C受體完激動(dòng)劑，Ki值為15 nM 靶點(diǎn) Human 5-HT2C Rat 5-HT2C IC50 15 nM (Ki) 29 nM (Ki) 體外研究 Lorcaserin exhibits higher affinity for human 5-HT2C than to 5-HT 5-HT2A (7.5-fold selective, Ki=112 nM) and 5-HT2B (11.6-fold selective, Ki=174 nM). Lorcaserin possesses agonist activity at all three human 5-HT2 receptors. Lorcaserin is 18-fold more potent at human 5-HT2C (EC50= 9 nM) than at human 5-HT2A (EC50= 168 nM), and it is 104-fold more potent at human 5-HT2C than human 5-HT2B (EC50= 943 nM). Lorcaserin shows full agonist activity at the human 5-HT2C and 5-HT2B receptors and partial agonist activity at the human 5-HT2A receptor (, and 75% of the maximal response elicited by serotonin, respectively). Lorcaserin does not compete for binding of ligands to serotonin, dopamine, and norepinephrine transporters. Lorcaserin does not stimulate norepinephrine, dopamine, or serotonin release from rat synaptosomes at submicromolar concentrations. Lorcaserin weakly inhibits norepinephrine (EC50= 2500 nM), serotonin (EC50= 1400 nM), and dopamine (EC50= 12,000 nM) uptake. 體內(nèi)研究 Lorcaserin is potent in inhibiting rat acute food intake upon oral administration with ED50 of 18 mg/kg at 6 hr. Lorcaserin chronic administration to rats maintained on a high fat diet also produces dose-dependent reductions in food intake and body weight gain during the 4-week study. Lorcaserin (18 mg/kg) significantly increases resting and penile grooming, and has no effects on wet dog shakes, and back muscle contractions of rats. Lorcaserin short-term administration (0.3125-20 mg/kg) significantly reduces nicotine self-administration in female rats. Long-term Lorcaserin (0.625 mg/kg) also significantly reduces nicotine self-administration over a 2-week period of repeated injections. 溶解性 DMSO 46 mg/mL，水 46 mg/mL，乙醇 46 mg/mL 穩(wěn)定性 2年 -20°C粉狀，6月-80°C溶于DMSO |
