Remerin

一种具有多种生物活性的阿朴啡类生物碱；选择性地与5-HT2A受体结合，而非与5-HT1A和多巴胺D1和D2受体结合（Kis分别为0.0621、1.17、1.4和22.6µM）；对白色念珠菌以及氯喹抗性和氯喹敏感的恶性疟原虫菌株均有活性（IC50s分别为4.5、0.4和0.2µg/ml）；增强多药耐药KB-V1细胞中长春花碱诱导的细胞毒性；在20mg/kg剂量下可提高MRSA诱发的败血症小鼠模型的存活率。An aporphine alkaloid with diverse biological activities; selectively binds to the 5-HT2A receptor over 5-HT1A and dopamine D1 and D2 receptors (Kis = 0.0621, 1.17, 1.4, and 22.6 µM, respectively); active against C. albicans as well as chloroquine-resistant and -sensitive strains of P. falciparum (IC50s = 4.5, 0.4, and 0.2 µg/ml, respectively); enhances vinblastine-induced cytotoxicity in multidrug-resistant KB-V1 cells; improves survival in a mouse model of MRSA-induced sepsis at 20 mg/kg.分子式C18H17NO2分子量279.3CN1[C@@]2([H])C3=C(CC1)C=C(OCO4)C4=C3C5=CC=CC=C5C2