title: Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor.
abstract: Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is preferentially adopted to rationalize the obtained results.
authors.affiliation: Menarini Ricerche S.p.A., Via dei Sette Santi 3, Florence, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Altamura
authors.forename: Franca
authors.initials: F
authors.lastname: Canfarini
authors.forename: Rose-Marie
authors.initials: RM
authors.lastname: Catalioto
authors.forename: Antonio
authors.initials: A
authors.lastname: Guidi
authors.forename: Franco
authors.initials: F
authors.lastname: Pasqui
authors.forename: Anna R
authors.initials: AR
authors.lastname: Renzetti
authors.forename: Antonio
authors.initials: A
authors.lastname: Triolo
authors.forename: Carlo A
authors.initials: CA
authors.lastname: Maggi
mesh_terms: D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008024:Ligands; D013058:Mass Spectrometry; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D010456:Peptides, Cyclic / Q000494:pharmacology; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D013237:Stereoisomerism
chemical_list: D008024:Ligands; C463499:MEN 11558; D010455:Peptides; D010456:Peptides, Cyclic; D018041:Receptors, Neurokinin-2