title: Synthesis and biological activity of NK1 tachykinin antagonists not containing D-residues.
abstract: A series of analogues of the previously reported NK1 tachykinin antagonist [Orn6, Glu(OBzl)11]-SP6-11-OBzl has been synthesized and tested in order to investigate the effects on antagonistic activity of modifications at the C-terminal residue. The biological activity in the guinea-pig ileum assay (NK1 receptor) indicates that the two aromatic rings introduced in the C-terminal part of the peptide are both essential for the expression of antagonistic activity.
authors.affiliation: Department of Chemistry, University of Patras, Greece.
authors.forename: C
authors.initials: C
authors.lastname: Poulos
authors.forename: M
authors.initials: M
authors.lastname: Antoniou
authors.forename: R
authors.initials: R
authors.lastname: Patacchini
authors.forename: C A
authors.initials: CA
authors.lastname: Maggi
authors.forename: P
authors.initials: P
authors.lastname: Rovero
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D015195:Drug Design; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008969:Molecular Sequence Data; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011651:Pulmonary Artery / Q000187:drug effects; D011817:Rabbits; D018040:Receptors, Neurokinin-1 / Q000378:metabolism; D013329:Structure-Activity Relationship; D013373:Substance P / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D064729:Neurokinin-1 Receptor Antagonists; D010446:Peptide Fragments; D018040:Receptors, Neurokinin-1; C086814:substance P (6-11)-O-benzyl, Orn(6)-Glu(O-benzyl)(11)-; C079225:substance P (6-11), Orn(6)-; D013373:Substance P