Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C11H14ClN |
Molecular Weight | 195.689 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1CNCCC2=C1C=C(Cl)C=C2
InChI
InChIKey=XTTZERNUQAFMOF-QMMMGPOBSA-N
InChI=1S/C11H14ClN/c1-8-7-13-5-4-9-2-3-10(12)6-11(8)9/h2-3,6,8,13H,4-5,7H2,1H3/t8-/m0/s1
DescriptionCurator's Comment: description was created based on several sources, including:
http://www.eisai.com/news/news201464.html
Curator's Comment: description was created based on several sources, including:
http://www.eisai.com/news/news201464.html
Lorcaserin, currently marketed under the trade name Belviq and previously Lorqess during development, is a weight-loss drug developed by Arena Pharmaceuticals. Lorcaserin is a selective 5-HT2C receptor agonist, and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets. 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion, the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor
CNS Activity
Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3828930/
Curator's Comment: Lorcaserin acts at 5-HT2C receptors in the central nervous system (CNS), particularly the hypothalamus, to reduce appetite
Originator
Sources: http://www.eisai.com/news/news201464.html
Curator's Comment: Discovered and developed by Arena Pharmaceuticals, Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL225 |
15.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | Belviq Approved UseIndicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight
management in adults with an initial body mass index (BMI) of 30 kg/m^2 or greater (obese) or 27 kg/m^2 or greater (overweight) in the presence of at least one weight-related comorbid condition, (e.g., hypertension, dyslipidemia, type 2 diabetes) Launch Date2012 |
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18252809
Curator's Comment: Radioligand binding assays for human and rat 5-HT2A, 5-HT2B, and 5-HT2C receptors were developed using the 5-HT2 agonist [125I] DOI asadioligand.
Lorcaserin was evaluated for its ability to inhibit neurotransmitter uptake into rat
brain synaptosomes. Lorcaserin weakly inhibited norepinephrine (EC50 = 2500 nM), serotonin (EC50 = 1400 nM), and dopamine (EC50 = 12,000 nM) uptake.
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FDA ORPHAN DRUG |
828021
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WHO-ATC |
A08AA11
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FDA ORPHAN DRUG |
758920
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LIVERTOX |
NBK548834
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NCI_THESAURUS |
C47794
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WHO-VATC |
QA08AA11
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NDF-RT |
N0000185010
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FDA ORPHAN DRUG |
565816
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DEA NO. |
1625
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N0000185009
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CHEMBL360328
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8128
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C506658
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N0000182137
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PRIMARY | Cytochrome P450 2D6 Inhibitors [MoA] | ||
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65353
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100000128165
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LORCASERIN
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8765
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C76102
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4374
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1300701
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m6908
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2941
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DB04871
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