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Propionylpiperazines as human melanocortin-4 receptor ligands
Bioorganic and Medicinal Chemistry Letters, 2006A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice.
Caroline W Chen +2 more
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Melanocortin 4 receptor mutations become common
Cell Metabolism, 2021In a new paper, Wade et al. (2021) analyzed the frequency of MC4R loss-of-function (LoF) mutations in a population-based Avon Longitudinal Study of Parents and Children. The frequency was 1 in 337 and the authors showed that MC4R LoF variants significantly correlated with increased body weight and fat mass in children and adults (cumulating in ...
Peter, Kühnen +2 more
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Characterisation of the Melanocortin 4 Receptor by Radioligand Binding
Pharmacology & Toxicology, 1996Abstract: The DNA encoding the human melanocortin 4 receptor was expressed in COS (CV‐1 origin, SV 40) cells and its radioligand binding properties was tested by using the [125I][Nle4, D‐Phe7]α‐melanocyte stimulating hormone (MSH). The radioligand was found to bind to a single saturable site with a Kd of 3.84±0.57 nmol/1 in the MC4 receptor expressing
H B, Schiöth +2 more
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Melanocortin - 4 Receptor Agonists for the Treatment of Obesity
Current Topics in Medicinal Chemistry, 2007The melanocortin family of receptors (MC 1-5R) and their endogenous peptide ligands (alpha, beta, gamma- MSH and ACTH) have been implicated in the control of a wide variety of behavioral and physiological functions including the homeostatic control of food intake and body weight.
Paul J, Emmerson +3 more
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