title: Selective agonists of NK-2 binding sites highly active on rat portal vein (NK-3 bioassay).
abstract: All the synthetized NKA and NKA (4-10) agonists have been found active in the rat portal vein bioassay. Even [Lys5, MeLeu9, Nle10] NKA(4-10), a highly potent competitor of NK-2 binding sites with very low binding potencies for NK-1 and NK-3 sites (IC50 greater than microM) is still active in contracting the rat portal vein. These results suggest that this tissue contains not only a fairly large population of NK-3 receptors but also a minor population of NK-2 receptors. Comparison of the activities of NKA C-terminal analogues on the guinea-pig ileum suggests that 1) only a small population of NK-2 receptors are present in this tissue and 2) beside NK-1, NK-2 and NK-3 receptors, another type of receptor sensitive to C-terminal sequences might be present in the guinea-pig tissue.
authors.affiliation: Laboratoire de Chimie Organique Biologique, CNRS URA 493, Université Paris VI, France.
authors.forename: G
authors.initials: G
authors.lastname: Chassaing
authors.forename: S
authors.initials: S
authors.lastname: Lavielle
authors.forename: D
authors.initials: D
authors.lastname: Loeuillet
authors.forename: P
authors.initials: P
authors.lastname: Robilliard
authors.forename: A
authors.initials: A
authors.lastname: Carruette
authors.forename: C
authors.initials: C
authors.lastname: Garret
authors.forename: J C
authors.initials: JC
authors.lastname: Beaujouan
authors.forename: M
authors.initials: M
authors.lastname: Saffroy
authors.forename: F
authors.initials: F
authors.lastname: Petitet
authors.forename: Y
authors.initials: Y
authors.lastname: Torrens
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D001681:Biological Assay; D006168:Guinea Pigs; D008969:Molecular Sequence Data; D015288:Neurokinin A / Q000378:metabolism*; D015287:Neurokinin B / Q000378:metabolism; D010446:Peptide Fragments / Q000378:metabolism*; D011169:Portal Vein / Q000737:chemistry* / Q000378:metabolism; D011817:Rabbits; D011863:Radioimmunoassay; D051381:Rats; D018041:Receptors, Neurokinin-2; D018042:Receptors, Neurokinin-3; D017981:Receptors, Neurotransmitter / Q000032:analysis* / Q000378:metabolism; D018039:Receptors, Tachykinin; D013329:Structure-Activity Relationship; D015320:Tachykinins / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D010446:Peptide Fragments; D018041:Receptors, Neurokinin-2; D018042:Receptors, Neurokinin-3; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D015320:Tachykinins; D015288:Neurokinin A; D015287:Neurokinin B; C056408:neurokinin A(4-10); C053213:neurokinin B (4-10)