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S8061

Sigma-Aldrich

SB 242084 dihydrochloride hydrate

≥98% (HPLC), powder

Synonyme(s) :

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

Formule empirique (notation de Hill):
C21H19ClN4O2 · 2HCl · xH2O
Numéro CAS:
181632-25-7
Poids moléculaire :
467.78 (anhydrous basis)
Numéro MDL:
MFCD12755727
Code UNSPSC :
12352200
ID de substance PubChem :
24899774
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to beige

Solubilité

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

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne SMILES 

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

Clé InChI

SUOZHMLTMKJQNG-UHFFFAOYSA-N

Application

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

Actions biochimiques/physiologiques

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

Caractéristiques et avantages

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

Attention

Hygroscopic

Informations légales

Manufactured and sold with the permission of GlaxoSmithKline Pharmaceuticals

Code de la classe de stockage

13 - Non Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

dust mask type N95 (US), Eyeshields, Gloves

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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
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
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)
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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