Melanocortin MC4 antagonists

Melanocortins participate in the HPA axis response to stress, at least partly through the release of CRF. The MC4 receptor has been identified as the receptor of particular interest in relationship to stress-related disorders including anxiety and depression [45]. The non-peptide MC4 antagonist MCL0129, 24, (K = 7.9 nM) demonstrated antidepressant effects in the forced swim and learned helplessness models, and also showed anxiolytic activity after oral administration [46]. Interestingly, the same series of compounds led to the serendipitous discovery of MCL0042 (25), a dual SSRI-MC4 antagonist (MC4: IC50 = 124nM; SERT: IC50 = 42) that was active in the olfactory bulbectomized rat model of depression [45].

Anxiety and Depression 101

Anxiety and Depression 101

Everything you ever wanted to know about. We have been discussing depression and anxiety and how different information that is out on the market only seems to target one particular cure for these two common conditions that seem to walk hand in hand.

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