Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens.
Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens.
复制标题
Orphanin FQ对豚鼠回肠和小鼠输精管有抑制作用。
DOI：
10.1016/s0006-8993(97)00858-5
复制
发表时间：
1997
期刊：
影响因子：
2.9
通讯作者：
Grandy,DK
中科院分区：
文献类型：
--
作者：
Zhang,G;Murray,TF;Grandy,DK
The activity of the recently isolated endogenous opioid-like peptide orphanin FQ (OFQ) was measured in two classical bioassays of opioid action. OFQ potently and concentration-dependently suppressed the electrically stimulated contractions of the guinea pig ileum (GPI) and the mouse vas deferens (MVD) with EC50values of 1.82±0.16 and 2.97±0.01 nM, and Emaxvalues of 56±3% and 96±4%, respectively. This effect of OFQ, in both the GPI and MVD, was insensitive to the opioid receptor antagonist naloxone. OFQ competed with [3H]diprenorphine binding to μ-, δ- or κ-opioid receptors stably expressed in Chinese hamster ovary cell lines with IC50values of 2.1±0.4, 2.2±0.3, 0.75±0.3 μM, respectively. Low affinity for the classical opioid receptors together with the inability of naloxone to antagonize its effect suggest that the inhibitory action of OFQ is mediated via a distinct OFQ receptor in the GPI and MVD. Consequently, the MVD could serve as a valuable bioassay of potential OFQ receptor antagonists.
