The NK1 receptor is involved in the neurokinin‐induced shape change of rabbit platelets

FEBS Letters

Savi, P.¹  Emonds-Alt, X.¹  Herbert, J.M.¹  Laplace, M.Cl.¹  Le Fur, G.¹ 

[1] Sanofi Recherche, Toulouse, France

关键词: Substance P;    Neurokinin;    Neurokinin receptor agonist;    Rabbit platelet;    Shape change in rabbit platelet;   

DOI  :  10.1016/0014-5793(92)80935-A

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Substance P and selective neurokinin receptor agonists have been tested for their ability to induce shape change in rabbit platelets. Substance P and the NK₁ receptor agonist Ac [Arg⁶,Sar⁹,Met(O₂)¹¹]-substance P (6–11) induced shape change (EC₅₀ = 3 and 6 nM, respectively), whereas the selective NK₂ agonist [Nle¹⁰]-Neurokinin A (4–10) and the selective NK₃ agonist [MePhe⁷]-Neurokinin B did not show any effect. Moreover, the specific NK₁ receptor antagonist CP-96,345 selectively and dose-dependently counteracted the effect of substance P or of the NK₁ receptor agonist (IC₅₀ = 2 and 0.8 nM, respectively), whereas the selective NK₂ receptor antagonist, SR 48968, had no effect. Unlike for serotonin or low doses of ADP, epinephrine did not allow substance P or the NK₁ receptor agonist to become a proaggregating substance. These data therefore show that the NK₁ receptor is solely involved in the neurokinin-induced shape change of rabbit platelets.

【 授权许可】

Unknown