SML0230
GW-803430
≥98% (HPLC)
别名:
6-(4-chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one, GW-3430, GW-803430A
SMILES string
[s]1c2c(nc[n]([c]2=O)c4cc(c(cc4)OCCN5CCCC5)OC)cc1c3ccc(cc3)Cl
InChI
1S/C25H24ClN3O3S/c1-31-22-14-19(8-9-21(22)32-13-12-28-10-2-3-11-28)29-16-27-20-15-23(33-24(20)25(29)30)17-4-6-18(26)7-5-17/h4-9,14-16H,2-3,10-13H2,1H3
InChI key
MWULMTACIBZPGN-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: ≥4 mg/mL at warmed to 60 °C
originator
GlaxoSmithKline
storage temp.
2-8°C
Quality Level
Application
GW-803430 may be used in MCHR1-mediated cell signaling studies.
Biochem/physiol Actions
GW-803430 antagonizes central MCHR1 and produces anxiolytic, anti-depressant and anti-obesity effects in rats and mice. It also controls the alcohol-seeking behavior in rats and is a promising treatment for alcohol use-related disorders.
GW-803430 is a centraly active and selective melanin-concentrating hormone receptor (MCHR) 1 antagonist
Features and Benefits
This compound is featured on the Melanin-Concentrating Hormone Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Eye Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Donald R Gehlert et al.
The Journal of pharmacology and experimental therapeutics, 329(2), 429-438 (2009-02-03)
The mammalian neuropeptide, melanin-concentrating hormone, interacts with two G protein-coupled receptors, melanin-concentrating hormone receptor (MCHR) 1 and MCHR2; however, only MCHR1 is expressed in rats and mice. In the present study, we evaluated MCHR1 antagonism in preclinical models believed to
Andrea Cippitelli et al.
Psychopharmacology, 211(4), 367-375 (2010-07-16)
Melanin-concentrating hormone (MCH) is involved in regulation of appetitive behaviors as well as emotional reactivity and reward, behavioral domains relevant to alcohol addiction. We evaluated the effects of the non-peptide MCH1 receptor antagonist, GW803430 [6-(4-chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one; 3-30 mg/kg, i.p.] on alcohol-related
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