Olanzapine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Olanzapine (LY170053) 是一种选择性的、具有口服活性的单胺能拮抗剂，高亲和力结合 5-羟色胺 H1，5HT2A/2C，5HT3，5HT6 (Ki 分别为 7、4、11、57 和 5 nM)，多巴胺 D1-4 (Ki=11-31 nM)，毒蕈碱 M1-5 (Ki=1.9-25 nM) 和肾上腺素 α1 受体 (Ki=19 nM)。

Olanzapine is an atypical antipsychotic, approved by the FDA in 1996. Olanzapine is manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper ends in 2011.(In Vitro):Olanzapine binds weakly to GABAA, Benzodiazepine (BZD), and β-adrenergic receptors (Ki>10 μM) .Olanzapine induces autophagy in human SH-SY5Y neuronal cell line.Olanzapine (1-100 μM for 144 h under serum starvation) results in a marked anti-proliferative effect in glioblastoma cell lines as well as glioma stem-like cells.Olanzapine also enhances Temozolomide’s anti-tumor activity in glioblastoma cell lines.Olanzapine induces apoptosis and necrosis in glioblastoma cell lines.(In Vivo):Olanzapine (0.75, 1.5 and 3 mg/kg) evaluates body weight and periuterine fat mass, as well as insulin, non-esterified fatty acids, triglycerides, and glucose levels in mice.

Cell Proliferation AssayCell Line:U87MG and A172 glioblastoma cell lines as well as SC38 and SC40 glioma stem-like cellsConcentration:1, 10, 100 μM Incubation Time:144 h; under serum starvation (1.5 % FBS) prior to performing MTT-assaysResult:Resulted in a marked antiproliferative effect with IC50 values ranging from 25 to 79.9 μM. In U87MG cells, anchorage-independent growth was dose-dependently inhibited. In A172 cells, migration was also shown to be inhibited in a dose-dependent manner. Western Blot Analysis Cell Line:U87MG and A172 cells Concentration:10, 25, 50, and 100 μM Incubation Time:7 h, 24 h, 48 h, 72 h Result:Led to a dose responsive decrease of pAMPK expression after 72 h of treatment.

Animal Model:Forty-two, 14, and 28 female CD-1 mice Dosage:0.75, 1.5 and 3 mg/kg Administration:Orally and chronically administered; 35 days Result:Increased body weight relative to vehicle on days 20-22, and from day 32 onwards there was a straightforward increase in body weight at 3 mg/kg.No differences were found between control and mice administered olanzapine at both 1.5 and 0.75 mg/kg.

LY170053

Endocrinology/Hormones

5-HT Receptor

5-HT| HT| mAChR| Adrenergic Receptor| Dopamine

Neurological Disease

——

132539-06-1

312.44

C17H20N4S

>98% (HPLC)

Ethanol: 9 mg/mL (28.8 mM); DMSO: 63 mg/mL (201.63 mM)

CN1CCN(C2=C(C=C(C)S3)C3=NC4=CC=CC=C4N2)CC1

2-methyl-4-(4-methylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine

(-20℃)

With Ice Pack

≥ 2 years