产品
编 号:F243916
分子式:C17H23Cl2NO
分子量:328.28
产品类型
结构图
CAS No: 195875-84-4
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产品详情
生物活性:
Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.
体内研究:
Tesofensine (a single dose of 0.1-3? mg/kg, s.c.) induces hypophagia in the DIO rat. A single dose of Tesofensine (0. 1-3?mg/kg, s.c.) robustly and dose dependently inhibits food intake in DIO rats over the 12?h nocturnal observation period. Daily administration of a moderate dose of Tesofensine (2.0?mg/kg, s.c.) over 16 days triggers a significant reduction in body weight after 4 days of administration relative to vehicle-treated controls.Animal Model:Diet-induced obesity (DIO) rat
Dosage:0.1-3?mg/kg
Administration:Administered subcutaneously (s.c.); a single dose (acute treatment)
Result:The threshold dose for inhibition of total food intake was 1.0?mg/kg.The ED50 for inhibition of total food intake in DIO rats was estimated to be 1.3?mg/kg.
Animal Model:Diet-induced obesity (DIO) rat
Dosage:2.0?mg/kg
Administration:Administered subcutaneously (s.c.) daily for over 16 days (chronic treatment)
Result:The average relative decrease in the body weight of tesofensine-treated DIO rats over the entire treatment period was 8.6±1.4%. When comparing to vehicle controls, the relative weight loss with tesofensine was 13.8±1.4%.