Fink-Jensen A, Kristensen P, Shannon H E, Calligaro D O, Delapp N W, Whitesitt C, Ward J S, Thomsen C, Rasmusseen T, Sheardown M J, Jeppesen L, Sauerberg P, Bymaster F P
Health Care Discovery, Novo Nordisk A/S, Måløv, Denmark.
Neuroreport. 1998 Oct 26;9(15):3481-6. doi: 10.1097/00001756-199810260-00027.
(5R,6R) 6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]oc tane (PTAC) is a selective muscarinic ligand with high affinity for central muscarinic receptors, agonist mode of action at the muscarinic M2 and M4 receptor subtypes and substantially less or no affinity for central dopamine receptors. In the present study PTAC, as well as the muscarinic agonists oxotremorine, RS86 and pilocarpine, inhibited dopamine D1 and D2 receptor agonist induced contralateral rotation in unilaterally 6-OHDA lesioned rats. The dose of SKF 38393 used to induce contralateral rotation also caused an intense Fos protein immunoreactivity in the rat dorsolateral striatum on the lesioned site which was inhibited by PTAC indicating that the inhibition of rotation by PTAC was not due to non-specific peripheral side effects.
(5R,6R) 6-(3-丙硫基-1,2,5-噻二唑-4-基)-1-氮杂双环[3.2.1]辛烷(PTAC)是一种对中枢毒蕈碱受体具有高亲和力的选择性毒蕈碱配体,对毒蕈碱M2和M4受体亚型具有激动剂作用模式,对中枢多巴胺受体的亲和力显著降低或无亲和力。在本研究中,PTAC以及毒蕈碱激动剂氧化震颤素、RS86和毛果芸香碱,抑制了多巴胺D1和D2受体激动剂诱导的单侧6-OHDA损伤大鼠的对侧旋转。用于诱导对侧旋转的SKF 38393剂量也在损伤部位的大鼠背外侧纹状体中引起强烈的Fos蛋白免疫反应性,PTAC可抑制该反应,表明PTAC对旋转的抑制不是由于非特异性外周副作用。