Multifaceted actions of melanin-concentrating hormone on mammalian energy homeostasis

O Al-Massadi, C Dieguez, M Schneeberger… - Nature Reviews …, 2021 - nature.com
Melanin-concentrating hormone (MCH) is a small cyclic peptide expressed in all mammals,
mainly in the hypothalamus. MCH acts as a robust integrator of several physiological …

The melanin-concentrating hormone system as a target for the treatment of sleep disorders

LE Potter, CR Burgess - Frontiers in neuroscience, 2022 - frontiersin.org
Given the widespread prevalence of sleep disorders and their impacts on health, it is critical
that researchers continue to identify and evaluate novel avenues of treatment. Recently the …

Discovery of (3-(4-(2-oxa-6-azaspiro [3.3] heptan-6-ylmethyl) phenoxy) azetidin-1-yl)(5-(4-methoxyphenyl)-1, 3, 4-oxadiazol-2-yl) methanone (AZD1979), a melanin …

A Johansson, C Lofberg, M Antonsson… - Journal of Medicinal …, 2016 - ACS Publications
A novel series of melanin concentrating hormone receptor 1 (MCHr1) antagonists were the
starting point for a drug discovery program that culminated in the discovery of 103 …

Crosstalk between melanin concentrating hormone and endocrine factors: implications for obesity

E Prida, S Fernández-González, V Pena-León… - International journal of …, 2022 - mdpi.com
Melanin-concentrating hormone (MCH) is a 19aa cyclic peptide exclusively expressed in the
lateral hypothalamic area, which is an area of the brain involved in a large number of …

In vitro Radiopharmaceutical Evidence for MCHR1 Binding Sites in Murine Brown Adipocytes

T Balber, K Benčurová, FW Kiefer… - Frontiers in …, 2019 - frontiersin.org
[11C] SNAP-7941 and its radiofluorinated, fluoro-ethyl derivative [18F] FE@ SNAP have
been developed as the first positron emission tomography tracers for melanin-concentrating …

Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one …

S Ahmad, WN Washburn, AS Hernandez… - Journal of Medicinal …, 2016 - ACS Publications
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols
derived from compound 2b is described. Subsequent pharmacokinetic and …

Evolution of physicochemical properties of melanin concentrating hormone receptor 1 (MCHr1) antagonists

A Johansson - Bioorganic & Medicinal Chemistry Letters, 2016 - Elsevier
One pharmacological principle for the treatment of obesity is blockade of the melanin
concentrating hormone receptor 1 (MCHr1), which in rodents has been shown to be strongly …

Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup

P Devasthale, W Wang, AS Hernandez, F Moore… - Bioorganic & Medicinal …, 2015 - Elsevier
Our investigation of the structure–activity and structure–liability relationships for
dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics …

Melanin-concentrating hormone receptor 1 antagonists for treatment of obesity

AF Abdel-Magid - ACS Medicinal Chemistry Letters, 2015 - ACS Publications
Melanin-Concentrating Hormone Receptor 1 Antagonists for Treatment of Obesity | ACS
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