Selective agonists of NK-2 binding sites highly active on rat portal vein (NK-3 bioassay).
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.
Chassaing
G
G
Laboratoire de Chimie Organique Biologique, CNRS URA 493, Université Paris VI, France.
Lavielle
S
S
Loeuillet
D
D
Robilliard
P
P
Carruette
A
A
Garret
C
C
Beaujouan
J C
JC
Saffroy
M
M
Petitet
F
F
Torrens
Y
Y
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
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)