Selective agonists of NK-2 binding sites highly active on rat portal vein (NK-3 bioassay)

  • Neuropeptides. 1991 Jun;19(2):91-5. doi: 10.1016/0143-4179(91)90137-8.
G Chassaing  1 ,  S Lavielle ,  D Loeuillet ,  P Robilliard ,  A Carruette ,  C Garret ,  J C Beaujouan ,  M Saffroy ,  F Petitet ,  Y Torrens, et al.
Affiliations
  • 1. Laboratoire de Chimie Organique Biologique, CNRS URA 493, Université Paris VI, France.
PMID: 1658676 DOI: 10.1016/0143-4179(91)90137-8
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.

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