TY - JOUR
T1 - Binding of a iodinated substance P analog to a NK-1 receptor on isolated cell membranes from rat anterior pituitary
AU - Larsen, P J
AU - Mikkelsen, J D
AU - Saermark, T
PY - 1989/5
Y1 - 1989/5
N2 - The characteristics of binding sites for substance-P (SP) on rat anterior pituitary membranes were studied, using 125I-labeled Bolton-Hunter SP as a ligand. The binding of [125I]Bolton-Hunter SP was saturable and reversible, and reached a plateau of maximal binding after approximately 12 min of incubation. Scatchard and Hill analyses of specific binding revealed a single class of noninteracting binding sites with a high affinity (Kd = 0.72 nM) and a moderate density (binding capacity = 32.16 fmol/mg protein). The biologically active tachykinins, which, in addition to SP, consist of physalaemin, eledoisin, kassinin, neurokinin-A, and neurokinin-B, could inhibit the binding in a concentration-dependent manner. Based on titration curves, the IC50 values of the tachykinins were measured, and the receptor was classified as a NK-1 receptor. These results demonstrate that a population of specific SP-binding sites is present in rat anterior pituitary and further support evidence that this peptide has an influence on pituitary function.
AB - The characteristics of binding sites for substance-P (SP) on rat anterior pituitary membranes were studied, using 125I-labeled Bolton-Hunter SP as a ligand. The binding of [125I]Bolton-Hunter SP was saturable and reversible, and reached a plateau of maximal binding after approximately 12 min of incubation. Scatchard and Hill analyses of specific binding revealed a single class of noninteracting binding sites with a high affinity (Kd = 0.72 nM) and a moderate density (binding capacity = 32.16 fmol/mg protein). The biologically active tachykinins, which, in addition to SP, consist of physalaemin, eledoisin, kassinin, neurokinin-A, and neurokinin-B, could inhibit the binding in a concentration-dependent manner. Based on titration curves, the IC50 values of the tachykinins were measured, and the receptor was classified as a NK-1 receptor. These results demonstrate that a population of specific SP-binding sites is present in rat anterior pituitary and further support evidence that this peptide has an influence on pituitary function.
KW - Animals
KW - Binding Sites
KW - Cell Membrane/metabolism
KW - Male
KW - Pituitary Gland, Anterior/metabolism
KW - Polyethyleneimine/pharmacology
KW - Rats
KW - Rats, Inbred Strains
KW - Receptors, Neurotransmitter/classification
KW - Receptors, Tachykinin
KW - Substance P/analogs & derivatives
KW - Succinimides/metabolism
U2 - 10.1210/endo-124-5-2548
DO - 10.1210/endo-124-5-2548
M3 - Journal article
C2 - 2468475
SN - 0013-7227
VL - 124
SP - 2548
EP - 2557
JO - Endocrinology
JF - Endocrinology
IS - 5
ER -