A peptidases-resistant glycosylated analogue of substance P-(5-11). Specificity towards substance P receptors.
Glycosylated analogues of the C-terminal heptapeptide of substance P either free or blocked on the N-terminal glutamine were synthesized in order to develop a metabolically stable peptide that would have an increased specificity for one type of receptor. Of the analogue described, (N-alpha-Boc-beta-D-Glc-p (1----5) Gln) -Gln-Phe-Phe-Gly-Leu-Met-NH2 is highly resistant to degradation on exposure to rat hypothalamic slices. This glycosylated peptide is about one third as potent as substance P in eliciting contractions of the guinea-pig ileum and is almost devoided of affinity for the 125I-Bolton Hunter-SP specific binding sites on rat brain synaptosomes.
D000818:Animals; D001681:Biological Assay; D001921:Brain / Q000378:metabolism*; D005769:Gastrointestinal Motility / Q000187:drug effects; D006168:Guinea Pigs; D007031:Hypothalamus / Q000378:metabolism; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D051381:Rats; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013373:Substance P / Q000031:analogs & derivatives*; D013574:Synaptosomes / Q000378:metabolism
D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter; D013373:Substance P