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Orally active, potent and selective melanin-concentrating hormone receptor 1 (MCH1) antagonist (IC50 = 15.7 nM) that displays > 96-fold selectivity over MCH2. Exhibits antidepressant and anxiolytic activity in vivo. Also displays affinity for 5-HT1A and 5-HT2B receptors (IC50 values are 62.9 and 266 nM respectively).
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Kanuma et al (2006) Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists. Bioorg.Med.Chem. 14 3307 PMID: 16434202
Chaki et al (2005) Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: Nonpeptide and orally active melanin-concentrating hormone receptor 1 antagonists. J.Pharmacol.Exp.Ther. 313 832
Dyck et al (2005) Small molecule melanin-concentrating hormone receptor 1 (MCH1R) antagonists as anxiolytic and antidepressive agents. Drug Dev.Res. 65 291
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Keywords: ATC 0065, ATC 0065 supplier, potent, selective, MCH, MCHR, MCH1R, MCHR1, antagonists, melanin, concentrating, hormone, receptors, serotonin, 5HT, ATC0065, Melanin-concentrating, Hormone, Receptors, 3359, Tocris Bioscience
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.