D'Amico M, Berrino L, Maione S, Rossi F
Institute of Pharmacology and Toxicology, Faculty of Medicine and Surgery, 2nd University of Naples, Italy.
Life Sci. 1996;58(10):PL 177-80. doi: 10.1016/0024-3205(96)00023-9.
The injection of endothelin-1 (ET-1) (1 pmol/rat) into the dorsolateral periaqueductal gray (PAG) area of freely moving rats induced rotation along the long axis of the body (barrel-rolling). Preinjection (10 min before) of BQ-788 (an ETB receptor selective antagonist; 5 nmol) or bosentan (an ETA/ETB receptor non-selective antagonist; 10 nmol) to the PAG reduced the behavioral response to ET-1. In contrast, pretreatment with FR139317 (an ETA receptor selective antagonist; 5 nmol) did not affect the ET-1-induced barrel-rolling. These results suggest that barrel-rolling induced by microinjection of ET-1 into the PAG area is predominantly mediated via ETB-like receptors.
将内皮素-1（ET-1）（1皮摩尔/大鼠）注射到自由活动大鼠的背外侧导水管周围灰质（PAG）区域，会诱导大鼠沿身体长轴旋转（翻滚）。在向PAG区域注射ET-1之前（提前10分钟）注射BQ-788（一种ETB受体选择性拮抗剂；5纳摩尔）或波生坦（一种ETA/ETB受体非选择性拮抗剂；10纳摩尔），可降低对ET-1的行为反应。相比之下，用FR139317（一种ETA受体选择性拮抗剂；5纳摩尔）预处理并不影响ET-1诱导的翻滚。这些结果表明，向PAG区域微量注射ET-1所诱导的翻滚主要通过类ETB受体介导。
