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Merck
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重要文件

SML3513

Sigma-Aldrich

Lorcaserin hydrochloride

≥98% (HPLC)

同義詞:

(1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine hydrochloride, (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride, (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine hydrochloride, APD 356 hydrochloride, APD-356 hydrochloride, APD356 hydrochloride

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About This Item

經驗公式(希爾表示法):
C11H14ClN·HCl
CAS號碼:
分子量::
232.15
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.04

品質等級

化驗

≥98% (HPLC)

形狀

powder

藥物控制

USDEA Schedule IV

儲存條件

desiccated

顏色

white to beige

溶解度

H2O: 2 mg/mL, clear

儲存溫度

-10 to -25°C

生化/生理作用

Lorcaserin is an orally active, potent and selective 5-hydroxytryptamine receptor (5-HT2C) agonist (human/rat Ki = 15 /29 nM) with 18- and 104-fold higher potency than 5-HT2A and 5-HT2B by cellular inositol phosphate accumulation assay (EC50 = 9, 168, 943 nM, respectively) and good selectivity over 5-HT1A/3/4C/5A/6/7 and a panel of 67 other GPCRs and ion channels. Chronic daily treatment to rats (4.5-18 mg/kg p.o. b.i.d.) maintained on a high fat diet causes reductions in food intake and body weight gain.

注意

Hygroscopic

象形圖

Health hazardExclamation mark

訊號詞

Warning

危險聲明

危險分類

Acute Tox. 4 Oral - Carc. 2

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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The opioid epidemic continues despite the availability of medications, including buprenorphine, for opioid use disorder (OUD); identifying novel and effective treatments is critical for decreasing the prevalence of OUD and ending this crisis. Buprenorphine alone does not markedly attenuate abuse-related
Yang He et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 41(26), 5734-5746 (2021-05-26)
Obesity is a serious global health problem because of its increasing prevalence and comorbidities, but its treatments are limited. The serotonin 2C receptor (5-HT2CR), a G-protein-coupled receptor, activates proopiomelanocortin (POMC) neurons in the arcuate nucleus of hypothalamus (ARH) to reduce
William J Thomsen et al.
The Journal of pharmacology and experimental therapeutics, 325(2), 577-587 (2008-02-07)
5-Hydroxytryptamine (5-HT)(2C) receptor agonists hold promise for the treatment of obesity. In this study, we describe the in vitro and in vivo characteristics of lorcaserin [(1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3 benzazepine], a selective, high affinity 5-HT(2C) full agonist. Lorcaserin bound to human and rat
Muhan Jing et al.
Frontiers in pharmacology, 12, 761966-761966 (2021-11-23)
Lorcaserin is a serotonergic agonist specific to the 5-hydroxytryptamine 2c receptor (5-HT2CR) that is FDA approved for the long-term management of obesity with or without at least one weight-related comorbidity. Lorcaserin can restrain patients' appetite and improve insulin sensitivity and

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