Henderson A K, Yamamura H I, Maggi C A, Buck S H, Van Giersbergen P L, Roeske W R
Department of Pharmacology, University of Arizona, College of Medicine, Tucson 85724.
Eur J Pharmacol. 1992 Feb 13;225(2):175-8. doi: 10.1016/0922-4106(92)90099-h.
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.
在竞争性放射性配体结合试验中，NK2受体拮抗剂[Tyr5，D-Trp6,8,9,Arg10]NKA(4-10)（MEN 10207）和[Tyr5，D-Trp6,8,9,Arg10]NKA(3-10)（MEN 10208）在牛胃膜和SKLKB82#3细胞（一种转染了编码牛NK2受体cDNA的鼠成纤维细胞系）中分别具有高亲和力和低亲和力。当在SKLKB82#3鼠成纤维细胞中抑制神经激肽A诱导的多磷酸肌醇水解时，这些拮抗剂也具有不同的亲和力。因此，SKLKB82#3鼠成纤维细胞表达的新生蛋白可能代表一种独特的NK2受体亚型。
