Demonstration of a neurokinin A receptor subtype in transfected fibroblasts.
In competitive radioligand binding assays, the NK2 receptor antagonists [Tyr5,D-Trp6,8,9,Arg10]NKA(4-10) (MEN 10207) and [Tyr5,D-Trp6,8,9,Arg10]NKA(3-10) (MEN 10208) had high and low affinity, respectively, in bovine stomach membranes and SKLKB82#3 cells, a murine fibroblast cell line transfected with a cDNA encoding for the bovine NK2 receptor. These antagonists also had different affinities when inhibiting neurokinin A-induced polyphosphoinositide hydrolysis in SKLKB82#3 murine fibroblasts. Thus, the de novo protein expressed by the SKLKB82#3 murine fibroblasts may represent a distinct NK2 receptor subtype.
Henderson
A K
AK
Department of Pharmacology, University of Arizona, College of Medicine, Tucson 85724.
Yamamura
H I
HI
Maggi
C A
CA
Buck
S H
SH
Van Giersbergen
P L
PL
Roeske
W R
WR
D000818:Animals; D002417:Cattle; D002478:Cells, Cultured; D005347:Fibroblasts / Q000378:metabolism; D007457:Iodine Radioisotopes; D015288:Neurokinin A / Q000031:analogs & derivatives / Q000378:metabolism* / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology; D010446:Peptide Fragments / Q000494:pharmacology; D011869:Radioligand Assay; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors / Q000302:isolation & purification*; D014162:Transfection
D007457:Iodine Radioisotopes; D009842:Oligopeptides; D010446:Peptide Fragments; D018041:Receptors, Neurokinin-2; D017981:Receptors, Neurotransmitter; C063615:neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-; C068553:MEN 10208; D015288:Neurokinin A