title: Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor.
abstract: A series of cyclic pseudopeptides were synthesized containing the sequence -Trp-Phe-(D)-PhePsiCH2NH-, the terminal ends of which were bound to 2-carboxy succinate or enantiomerically enriched tricarballylic acid to give the final cyclic structures. These two molecules and their subsequent derivatives were screened for h-NK2 receptor binding and functional antagonist activity on the rabbit urinary bladder.
authors.affiliation: Menarini Ricerche S.p.A. Laboratori di Firenze, Via Rismondo 12/A, 50131 Firenze, Italy. chimfarm@menarini.ricerche.it
authors.forename: Nicholas J S
authors.initials: NJ
authors.lastname: Harmat
authors.forename: Danilo
authors.initials: D
authors.lastname: Giannotti
authors.forename: Rossano
authors.initials: R
authors.lastname: Nannicini
authors.forename: Enzo
authors.initials: E
authors.lastname: Perrotta
authors.forename: Marco
authors.initials: M
authors.lastname: Criscuoli
authors.forename: Riccardo
authors.initials: R
authors.lastname: Patacchini
authors.forename: Anna-Rita
authors.initials: AR
authors.lastname: Renzetti
authors.forename: Sandro
authors.initials: S
authors.lastname: Giuliani
authors.forename: Maria
authors.initials: M
authors.lastname: Altamura
authors.forename: Carlo A
authors.initials: CA
authors.lastname: Maggi
mesh_terms: D000818:Animals; D003500:Cyclization; D018716:Molecular Mimicry; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D011869:Radioligand Assay; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D019802:Succinic Acid / Q000737:chemistry; D014233:Tricarboxylic Acids / Q000737:chemistry; D001743:Urinary Bladder / Q000187:drug effects
chemical_list: D009842:Oligopeptides; D010456:Peptides, Cyclic; D018041:Receptors, Neurokinin-2; D014233:Tricarboxylic Acids; D019802:Succinic Acid; C028021:tricarballylic acid