Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics Aspects of Lorcaserin, a Selective Serotonin 5-HT2C Receptor Agonist: An Update

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Author(s): Sanjay Sharma *, Komal S. Aware, Ketan Hatware, Kiran Patil .

Journal Name: Mini-Reviews in Medicinal Chemistry

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Abstract:

This review refers to the all-inclusive details of Lorcaserin Hydrochloride, on comprehensive information about synthesis, analytical methods, pharmacodynamics, pharmacokinetics, drug interaction, and adverse effect. Lorcaserin Hydrochloride is (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride chemically. Lorcaserin HCl is a novel synthetic, centrally acting selective serotonin C (5-HT2c) receptor, l agonist, which results in increased satiety and decreased food consumption in patients. A headache, dizziness, nausea, is the most common side effects associated with this drug. Lorcaserin HCl has two major metabolites, one conjugated with glucuronide called N-carbamoyl glucuronide which is excreted in urine and the second Lorcaserin N-sulfamate which is circulated in the blood. Lorcaserin HCl is synthesized using four different schemes of which a six-step method that resulted in 92.3% yield with 99.8% of purity is employed for scale up production. It is analyzed quantitatively in plasma and brain tissue matrix of rat by Ultra Performance Liquid chromatographic (UPLC) method using MS-MS (Mass Spectrometric) detection.

Keywords: Lorcaserin Hydrochloride, Appetite suppressant, Chemistry, Analysis, Pharmacokinetics, Pharmacodynamics.

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(E-pub Ahead of Print)
DOI: 10.2174/1389557519666190408154443
Price: $95

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