The neurokinins are indisputably essential neurotransmitters in numerous pathoand
physiological events. Being widely distributed in the Central Nervous System (CNS) and …

A screening of conformationally constrained aromatic amino acids as base cores for the
preparation of new NK1 receptor antagonists resulted in the discovery of three new NK1 …

Neurokinins (or tachykinins) are peptides that modulate a wide variety of human physiology
through the neurokinin G protein-coupled receptor family, implicated in a diverse array of …

Publisher Summary This chapter focuses on the progress in the development of neurokinin
(NK) antagonists. The neurokinins substance P (SP), neurokinin A (NKA), and neurokinin B …

The area of neurokinin (NK) research has seen an explosion of interest following the
identification of the first non-peptide antagonists. Since then nearly every major …

The mammalian tachykinins, substance P (SP, l), neurokinin A (NKA, 2) and neurokinin B
(NKB, 3) are the preferred endogenous agonists at three distinct neurokinin (NK) receptors …

A thorough SAR study of the oxime region of the dual NK1/NK2 antagonist 1 revealed
several modifications that result in potent dual antagonists. Follow up SAR studies on a …

Substance P (SP), the first isolated neuropeptide, belongs to the family of tachykinin
peptides and is the natural ligand of neurokinin-1 receptors (NK-1R), also named SP …

The pharmacological profiles of two novel neurokinin agonists have been investigated. δAva
[L-Pro 9, N-MeLeu 10] SP (7–11)(GR73632) and [Lys 3, Gly 8-R-γ-lactam-Leu 9] NKA (3 …

A reported mixed opioid agonist–neurokinin 1 receptor (NK1R) antagonist 4 (Dmt-D-Arg-
Aba-Gly-(3′, 5′-(CF 3) 2) NMe-benzyl) was modified to identify important features in both …