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Merck
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文件

S8061

Sigma-Aldrich

SB 242084 dihydrochloride hydrate

≥98% (HPLC), powder

别名:

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride hydrate, 6-Chloro-5-methyl-1-[[2-(2-methylpyrid-3-yloxy)pyrid-5-yl]carbamoyl]indoline dihydrochloride hydrate

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About This Item

经验公式（希尔记法）:
C21H19ClN4O2 · 2HCl · xH2O
CAS号:
181632-25-7
分子量:
467.78 (anhydrous basis)
MDL號碼:
MFCD12755727
分類程式碼代碼:
12352200
PubChem物質ID:
24899774
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

DMSO: 15 mg/mL, clear
H2O: 5 mg/mL, clear

起源

GlaxoSmithKline

儲存溫度

2-8°C

SMILES 字串

O.Cl.Cl.Cc1cc2CCN(C(=O)Nc3ccc(Oc4cccnc4C)nc3)c2cc1Cl

InChI

1S/C21H19ClN4O2.2ClH.H2O/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2;;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27);2*1H;1H2

InChI 密鑰

SUOZHMLTMKJQNG-UHFFFAOYSA-N

應用

SB 242084 dihydrochloride hydrate was used to study the role of 5-HT2C on food intake behavior of rats.4,5

生化／生理作用

SB 242084 is a potent and selective antagonist of 5-HT2C receptor. It increases the basal activity of dopaminergic neurons and affects the behavioral responses mediated by 5-HT2C such as mesolimbic neuron activity and food intake.3,4,5

特點和優勢

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

注意

吸湿

法律資訊

Manufactured and sold with the permission of GlaxoSmithKline Pharmaceuticals

儲存類別代碼

13 - Non Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves

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G A Kennett et al.
Neuropharmacology, 36(4-5), 609-620 (1997-04-01)
SB 242084 has a high affinity (pKi 9.0) for the cloned human 5-HT2C receptor and 100- and 158-fold selectivity over the closely related cloned human 5-HT2B and 5-HT2A subtypes respectively. SB 242084 had over 100-fold selectivity over a range of
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
S M Bromidge et al.
Journal of medicinal chemistry, 40(22), 3494-3496 (1997-11-14)
Claudia von Meyenburg et al.
Pharmacology, biochemistry, and behavior, 74(2), 505-512 (2002-12-14)
Rats consistently reduce their food intake following injections of bacterial lipopolysaccharides (LPS). Because inhibition of serotonergic (5-HT) activity by 8-OH-DPAT (5-HT(1A) activation) attenuates LPS-induced anorexia, we conducted a series of studies to examine whether other 5-HT-receptors are involved in the
V Di Matteo et al.
Neuropharmacology, 38(8), 1195-1205 (1999-08-26)
Electrophysiological techniques and in vivo microdialysis were used to investigate the effect of SB 242084, a potent and selective 5-HT2C receptor antagonist in the control of nigro-striatal and mesolimbic dopaminergic function. Thus, extracellular single unit recordings were performed from neurochemically-identified
Brigitte S Kopf et al.
Brain research, 1306, 77-84 (2009-09-29)
LPS, a potent activator of the innate immune system, is commonly used to investigate the acute phase response to infection, including anorexia. Serotonin 2C-receptor signaling has been shown to be involved in the mediation of LPS anorexia. Here we used

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