Lorcaserin hydrochloride CAS 846589-98-8
Introduction:Basic information about Lorcaserin hydrochloride CAS 846589-98-8, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Lorcaserin hydrochloride Basic information
| Product Name: | Lorcaserin hydrochloride |
| Synonyms: | (R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDE;LORCASERIN HCL;Lorcaserin hydrochloride;(R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride;(1R)-8-chloro-1-Methyl-2,3,4,5-tetrahydro-1H-3-benzazepine;lorcaserin hydrochloride (APD-356);R Lorcaserin hydrochloride;Green Card mianserin hydrochloride |
| CAS: | 846589-98-8 |
| MF: | C11H15Cl2N |
| MW: | 232.15 |
| EINECS: | 1592732-453-0 |
| Product Categories: | APIs;5-HT 2c receptor agonist;Inhibitors;1 |
| Mol File: | 846589-98-8.mol |
Lorcaserin hydrochloride Chemical Properties
| solubility | Soluble in DMSO > 10 mM |
| form | Powder |
| color | white to beige |
| Stability: | Hygroscopic |
Safety Information
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
| Hazard Classifications | Acute Tox. 4 Oral Carc. 2 |
| Description | In June 2012, the US FDA approved lorcaserin for chronic weight managementin adult patients who are characterized as overweight or obese andhave at least one comorbid, weight-related condition.Lorcaserin (also known as APD356) is the first 5-HT2C agonistapproved for chronic weight management since the withdrawal of the5-HT2C agonist fenfluramine in 1997 due to rare cases of cardiac valvulopathy. The serotonin receptor 5-HT2C is found primarily in the hypothalamusand regulates appetite and feeding behavior. Safety issues withfenfluramine were associated with poor selectivity for 5-HT2C versus5HT2A and 5HT2B. Ring constraint afforded by the benzazepine inlorcaserin improved selectivity for 5HT2C by over 2 log units. |
| Description | Lorcaserin (hydrochloride) (CRM) (Item No. 19247) is a certified reference material categorized as an anorectic. It also decreases oxycodone intake and has positive effects on self-administration and relapse vulnerability in the rat. Lorcaserin is regulated as a Schedule IV compound in the United States. This product is intended for research and forensic applications. |
| Originator | Pharmaceuticals (United States) |
| Uses | Lorcaserin hydrochloride, a novel antiobesity drug, is a selective serotonin 5-HT2C receptor agonist, approved by FDA in 2012. |
| Definition | ChEBI: A hydrochloride obtained by reaction of lorcaserin with one equivalent of hydrochloric acid. Used as an anti-obesity drug. |
| Brand name | Belviq |
| Side effects | Lorcaserin hydrochloride (Belviq) is a serotonin 2C receptor agonist that causes weight loss by causing appetite suppression.It appears to have fewer adverse effects than orlistat,although long-term safety data are limited. The recommended dosage is 10mg twice daily. Lorcaserin should be discontinued if patients do not lose 5% of their body weight in 12 weeks. The efficacy of lorcaserin appears similar to that of orlistat (mean difference in weight loss between active and placebo-treated groups approximately 3-4 kg).Common side effects include nausea, headache,dizziness, nasopharyngitis, and fatigue. Lorcaserin may increasethe risk of symptomatic hypoglycemia in patients with type 2 diabetes on oral agents, necessitating a reduction in the dose of diabetes medications. Lorcaserin should not be used in individuals with creatinine clearance <30 mL/minute. It is contraindicated during pregnancy. In addition, lorcaserin should not be used with other serotonergic drugs (e.g., selective serotonin reuptake inhibitors,selective serotonin-norepinephrine reuptake inhibitors, bupropion[Wellbutrin], tricyclic antidepressants,and monamine oxidase inhibitors)because of the theoretical potential for serotonin syndrome. https://www.accessdata.fda.gov https://medlineplus.gov |
| Drug interactions | Belviq (lorcaserin hydrochloride) may interact with antidepressants, including selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors (MAOIs), triptans, bupropion, dextromethorphan, or St. John's Wort. |
| Precautions | The precautions of BELVIQ (lorcaserin hydrochloride) tablets: Serotonin Syndrome or Neuroleptic Malignant Syndrome (NMS)- like Reactions: The safety of coadministration with other serotonergic or antidopaminergic agents has not been established. Valvular heart disease: If signs or symptoms develop, consider BELVIQ discontinuation and evaluate the patient for possible valvulopathy. Cognitive Impairment: This may cause disturbances in attention or memory. Caution with the use of hazardous machinery when starting BELVIQ treatment. Psychiatric Disorders, including euphoria and dissociation: Do not exceed the recommended dose of 10 mg twice daily. Monitor for depression or suicidal thoughts. Discontinue if symptoms develop. Use of Antidiabetic Medications: Weight loss may cause hypoglycemia. Monitor blood glucose. BELVIQ has not been studied in patients taking insulin. Priapism: Patients should seek emergency treatment if an erection lasts >4 hours. Use BELVIQ with caution in patients predisposed to priapism. |
| References | [1] PAUL J. FLETCHER . Characterizing the effects of 5-HT2C receptor ligands on motor activity and feeding behaviour in 5-HT2C receptor knockout mice[J]. Neuropharmacology, 2009, 57 3: Pages 259-267. DOI: 10.1016/j.neuropharm.2009.05.011 [2] HARSHINI NEELAKANTAN. Lorcaserin Suppresses Oxycodone Self-Administration and Relapse Vulnerability in Rats[J]. ACS Chemical Neuroscience, 2017, 8 5: 1065-1073. DOI: 10.1021/acschemneuro.6b00413 |
Lorcaserin hydrochloride Preparation Products And Raw materials
| Raw materials | LorcaserinA-->1H-3-Benzazepine, 8-chloro-2,3,4,5-tetrahydro-1-Methyl-, (1S)- |
