Melanocortin MC4 antagonists

Panic Away

Panic Away System

Get Instant Access

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].

Was this article helpful?

0 0
Eliminating Stress and Anxiety From Your Life

Eliminating Stress and Anxiety From Your Life

It seems like you hear it all the time from nearly every one you know I'm SO stressed out!? Pressures abound in this world today. Those pressures cause stress and anxiety, and often we are ill-equipped to deal with those stressors that trigger anxiety and other feelings that can make us sick. Literally, sick.

Get My Free Ebook

Post a comment