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Details

Stereochemistry ABSOLUTE
Molecular Formula C11H14ClN.ClH
Molecular Weight 232.15
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LORCASERIN HYDROCHLORIDE ANHYDROUS

SMILES

Cl.C[C@H]1CNCCC2=CC=C(Cl)C=C12

InChI

InChIKey=ITIHHRMYZPNGRC-QRPNPIFTSA-N
InChI=1S/C11H14ClN.ClH/c1-8-7-13-5-4-9-2-3-10(12)6-11(8)9;/h2-3,6,8,13H,4-5,7H2,1H3;1H/t8-;/m0./s1

HIDE SMILES / InChI

Description

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
15.0 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Belviq
PubMed

PubMed

TitleDatePubMed
Nonincretin drugs in later-stage development.
2014 Jan
[Cutting-edge of medicine; the prospects of novel anti-obesity drugs].
2014 Mar 10
Patents

Sample Use Guides

In Vivo Use Guide
One tablet of 10 mg twice daily
Route of Administration: Oral
In Vitro Use Guide
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.
Name Type Language
LORCASERIN HYDROCHLORIDE ANHYDROUS
DASH  
Common Name English
LORCASERIN HYDROCHLORIDE
MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN  
Preferred Name English
1H-3-BENZAZEPINE, 8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-, HYDROCHLORIDE (1:1), (1R)-
Systematic Name English
APD-356
Code English
LORCASERIN HYDROCHLORIDE [VANDF]
Common Name English
LORCASERIN HYDROCHLORIDE [MI]
Common Name English
LORCASERIN HYDROCHLORIDE [WHO-DD]
Common Name English
LORCASERIN HYDROCHLORIDE [ORANGE BOOK]
Common Name English
LORCASERIN HYDROCHLORIDE [USAN]
Common Name English
APD356
Code English
LORQESS
Brand Name English
1H-3-BENZAZEPINE, 8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-, HYDROCHLORIDE, (1R)-
Systematic Name English
(1R)-8-CHLORO-1-METHYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE HYDROCHLORIDE
Systematic Name English
LORCASERIN HCL
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C47794
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
Code System Code Type Description
MERCK INDEX
M6908
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY Merck Index
NCI_THESAURUS
C76103
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY
RXCUI
1808546
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
ALTERNATIVE
RXCUI
1300700
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY RxNorm
EPA CompTox
846589-98-8
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY
EVMPD
SUB34927
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY
CAS
846589-98-8
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY
PUBCHEM
11673085
Created by admin on Tue Oct 22 01:50:22 UTC 2019 , Edited by admin on Tue Oct 22 01:50:22 UTC 2019
PRIMARY