Biological ActivityHS 014 is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central administration in vivo. Also inhibits IL-1β-induced Fos expression in the paraventricular hypothalamus.
(Modifications: Cys-1 = N-terminal Ac, X = D-2-Nal, Asp-12 = C-terminal amide, Disulfide bridge: 1-8)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test.
Bellasio et al.
Discovery of novel melanocortin4 receptor selective MSH analogues.
Schioth et al.
Central blockade of melanocortin receptors attenuates the metabolic and locomotor responses to peripheral interleukin-1β administration.
Whitaker and Reye
Citation for HS 014
The citations listed below are publications that use Tocris products. Selected citations for HS 014 include:
1 Citation: Showing 1 - 1
The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo.
Authors: Panaro Et al.
PLoS One 2014;20:1018
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