Pavia Jillian M, Schiöth Helgi B, Morris Margaret J
Department of Neuroscience, Division of Pharmacology, Uppsala University, Sweden.
Neuroreport. 2003 Apr 15;14(5):703-7. doi: 10.1097/00001756-200304150-00009.
The receptor subtype(s) responsible for the cardiovascular actions of the melanocortins remains to be elucidated. This study investigated the cardiovascular effects of central injection of alpha-MSH and a potent cyclic MC3/4 receptor agonist, MTII, in the presence and absence of the newly developed MC4 receptor selective antagonist, HS014. Both alpha-MSH (250 pmol) and MTII (20-500 pmol) produced a rapid decrease in blood pressure and heart rate after injection into the nucleus tractus solitarii (NTS) of urethane-anaesthetised male Sprague-Dawley rats. These responses were attenuated in a dose-dependent manner by prior local NTS blockade with HS014 (20 or 100 pmol), providing evidence for the role of the MC4 receptor in the cardiovascular changes following NTS injection of melanocortins in the rat.
负责黑皮质素心血管作用的受体亚型仍有待阐明。本研究在存在和不存在新开发的MC4受体选择性拮抗剂HS014的情况下,研究了向中枢注射α-MSH和强效环状MC3/4受体激动剂MTII的心血管效应。在向乌拉坦麻醉的雄性Sprague-Dawley大鼠的孤束核(NTS)注射后,α-MSH(250 pmol)和MTII(20-500 pmol)均使血压和心率迅速下降。预先用HS014(20或100 pmol)进行局部NTS阻断,这些反应以剂量依赖性方式减弱,这为MC4受体在大鼠NTS注射黑皮质素后心血管变化中的作用提供了证据。