|
|||||
|
|
E-2078, a potent, selective and stable dynorphin analog with preferential activity for the kappa-opioid receptor subtype on the mouse vas deferens neuroeffector junction |
|
| Authors: | Raú l Valenzuela Shinro Tachibana J. Pablo Huidobro-Toro |
| Affiliation: | a Neurohumoral Regulation Unit, Department of Physiology, Faculty of Biological Sciences P. Catholic University of Chile, P.O. Box 114-D, Santiago 1, Chile * EISAI Chemical Co., Tsukuba Research Laboratories, 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-26, Japan |
| Abstract: | The profile of opioid activity of E-2078, a synthetic stable dynorphin analog, was examined in the mouse vas deferens bioassay and compared to that of methionine enkephalin and nonpeptide kappa agonists in the absence and in the presence of selective antagonists for the mu-, kappa- and delta-opioid receptor subtypes. The inhibitory action of E-2078 and related kappa agonists was specifically and potently antagonized only by norbinaltorphimine, revealing the presence of kappa receptors in this tissue and the predominant kappa activity of E-2078. |
| Keywords: | Dynorphin stable analog E-2078 Mouse vas deferens neurotransmission Kappa-opioid receptor Norbinaltorphimine antagonism Kappa-opioid agonist |
| 本文献已被 ScienceDirect 等数据库收录！ | |