Neuropeptide approaches

6.03.7.1.2.1 NK1 receptor antagonists

SP is an 11 amino acid peptide belonging to the tachykinin family; it mediates its biological actions through G tachykinin (NK1) receptors. Evidence to support a major role of the NK1 receptor system in stress-related behaviors has guided the clinical development of several NK1 receptor antagonists, including aprepitant (MK-869; 72), lanepitant (73), dapitant (74), vestiptant (75), PD-174424 (76), and NBI 127914 (77). The antidepressant efficacy of the first NK1 receptor antagonist MK-0869 (Aprepitant; 72) was demonstrated in patients with major depression and high anxiety, and has recently been replicated with a second compound, L759274. Aprepitant improved depression and anxiety symptoms in a quantitatively similar manner to SSRIs. However, it failed to show efficacy in Phase III clinical trials for depression.11,57 NK2 receptor ligands (e.g., NKP 608 (78), GR159897 (79)) are also under investigation for their potential role in depression and anxiety disorders.

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