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Merck
모든 사진(1)

주요 문서

S8061

Sigma-Aldrich

SB 242084 dihydrochloride hydrate

≥98% (HPLC), powder

동의어(들):

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

실험식(Hill 표기법):
C21H19ClN4O2 · 2HCl · xH2O
CAS Number:
Molecular Weight:
467.78 (anhydrous basis)
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

분석

≥98% (HPLC)

양식

powder

저장 조건

desiccated

색상

white to beige

solubility

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

주관자

GlaxoSmithKline

저장 온도

2-8°C

SMILES string

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 key

SUOZHMLTMKJQNG-UHFFFAOYSA-N

애플리케이션

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

생화학적/생리학적 작용

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

특징 및 장점

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

주의사항

Hygroscopic

법적 정보

Manufactured and sold with the permission of GlaxoSmithKline Pharmaceuticals

Storage Class Code

13 - Non Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

개인 보호 장비

dust mask type N95 (US), Eyeshields, Gloves


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문서 라이브러리 방문

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
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)
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
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
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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