Characterization of tachykinin receptors in endothelial cells of porcine artery.
The binding of iodine-labeled Bolton-Hunter substance P (125I-BHSP) to porcine endothelial cell membranes was examined. The endothelial cells had a single high-affinity binding site with a dissociation constant of 0.10 nM, and a maximum number of binding sites of 52.2 fmol/mg protein. The relative potencies of various tachykinins to displace the binding of 47 pM 125I-BHSP suggested that endothelial cells of porcine aorta contain the NK-1 subtype of tachykinin receptor. A GTP analogue, guanyl-5'-yl imidodiphosphate, induced marked reduction in the number of 125I-BHSP binding sites suggesting that these binding sites are coupled with GTP-binding protein.
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Fukuoka University, Japan.
R
R
Saito
H
H
Konishi
Y
Y
Takano
S
S
Nonaka
K
K
Sakaguchi
Y
Y
Shimohigashi
H
H
Kamiya
D000818:Animals; D001011:Aorta / Q000378:metabolism*; D001667:Binding, Competitive; D004730:Endothelium, Vascular / Q000378:metabolism; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology; D066298:In Vitro Techniques; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism*; D018039:Receptors, Tachykinin; D013373:Substance P / Q000378:metabolism*; D013388:Succinimides / Q000378:metabolism*; D013552:Swine
C043194:Bolton Hunter reagent-substance P conjugate; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D013388:Succinimides; D013373:Substance P; D006165:Guanylyl Imidodiphosphate