product name Lorcaserin HCl
Description: Lorcaserin HCl is a potent and selective full agonist of human 5-HT2C receptor with Ki of 15 nM. 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.
References: J Pharmacol Exp Ther. 2008 May;325(2):577-87; J Pharmacol Exp Ther. 2011 Sep;338(3):890-6.
232.15
Formula
C11H14ClN.HCl
CAS No.
846589-98-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 46 mg/mL (198.1 mM)
Water: 46 mg/mL (198.1 mM)
Ethanol: 46 mg/mL (198.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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 (100%, 100% 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. Kinase Assay: Cell Assay: |
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| In Vivo | 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2008 May;325(2):577-87; J Pharmacol Exp Ther. 2011 Sep;338(3):890-6. |
