Synthesis and biological activity of NK1 substance P selective agonists by modifying the methionyl residue.

Abstract:

:A series of analogues of substance P, where the Met11 residue was replaced by Glu(OCH2CH3), Glu(OBzl) and Hse(CH3), were synthesized in order to investigate the effect on agonist activity of modifications at the C-terminal residue. The biological activities in the guinea-pig ileum assay (NK1 receptor) and rat [text says rabbit] pulmonary artery (NK2 receptor) indicate that replacement of the SCH3 group of Met11 of substance P by the COOBzl or OCH3 groups favour interaction with the NK1 receptor and increase selectivity towards this receptor subtype.

journal_name

Neuropeptides

journal_title

Neuropeptides

authors

Poulos C,Antoniou M,Patacchini R,Maggi CA,Pegoraro S,Rovero P

doi

10.1016/0143-4179(94)90013-2

subject

Has Abstract

pub_date

1994-07-01 00:00:00

pages

27-9

issue

1

eissn

0143-4179

issn

1532-2785

pii

0143-4179(94)90013-2

journal_volume

27

pub_type

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