Lorcaserin HCl 是一种选择性血清素激动剂，最近被批准为减肥药。

Lorcaserin is a selective serotonin agonist that has been recently approved as a weight loss agent.

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 decreases cumulative food intake at 2, 4, 6, and 22 h with a significant decrease continuing throughout the 22-h duration of the study at the highest dose (24 mg/kg) only. The reduction in food intake induced by lorcaserin (18 mg/kg, p.o.) is mediated by 5-HT2C and not 5-HT2A receptors. Lorcaserin significantly reduces active, and increased inactive counts, and increases the incidence of penile grooming, an effect mediated by the 5-HT2C receptor[1]. Lorcaserin (20 mg/kg) doses causes a significant linear dose-related reduction in responses on the active lever but has no significant effect on the response to the inactive lever. Lorcaserin (0.3125, 0.625, 1.25, and 2.5 mg/kg) also produces a significant reduction in nicotine self-administration[

For development of functional human and rat 5-HT2A,5-HT2B,and 5-HT2C inositol accumulation assays,recombinant 5-HT2 receptors are transiently expressed in HEK293 cells using the Lipofectamine method.Cells are incubated in 15-cm plates with DMEM,and they are grown to at least 60 to 80% confluence,rinsed with Opti-MEM I media,followed by addition of 2 mL of Opti-MEM I containing 60 μL of Lipofectamine and 16 μg of cDNA for human and rat 5-HT2A and 5-HT2B receptors or 15 μL of Lipofectamine and 16 μg of cDNA for human and rat 5-HT2C receptors.Cells are then incubated for 5 h at 37°C in a 5% CO2 incubator.Next,cells are aspirated,and 30 mL of DMEM is added.Cells are then used for assays 24 h after transfection.Under these conditions,cells expressing human 5-HT2C receptor display constitutive elevation of inositol phosphate accumulation that is reversed by the inverse agonist mianserin,whereas cells expressing human 5-HT2A and 5-HT2B receptors display considerably less constitutive activity.

On the day of the experiment, rats receives a single dose of lorcaserin in water via oral gavage. Dosing volume and dose are 5 mL/kg and 10 mg/kg, respectively.

846589-98-8

C11H15Cl2N

232.15

Ethanol:46 mg/mL (198.14 mM)
DMSO:46 mg/mL (198.14 mM)
DMSO:2.4 mg/mL (10.34 mM)
H2O:46 mg/mL (198.14 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years