多巴胺刚性角状三环类似物的多巴胺能活性及立体化学考量：苯并喹喔啉和萘并噻嗪。
Dopaminergic activity and stereochemical considerations for rigid angular tricyclic congeners of dopamine: benzoquinoxalines and naphthothiazines.
作者信息
Perrone R, Berardi F, Tortorella V, Racagni G, Rovescalli A
机构信息
Dipartimento Farmaco-Chimico, Università di Bari, Italy.
出版信息
Farmaco. 1990 May;45(5):479-88.
Replacement of the oxygen atom at 1-position in the hexahydronaphthoxazines (4, PHNO) with a sulfur or nitrogen atom leads to the hexahydronaphthiazines (6, PHNT) and octahydro-benzoquinoxalines (5, POBQ) respectively and the 9-OH-PHNT shows to have a high affinity towards D-2 dopamine receptors in the binding assays; the racemic 9-OH-PHNT was then resolved and its absolute configuration was determined by CD. Inactivity on D-2 receptors of (+)-9-OCH3-PHNT 12 confirms the validity of the McDermed receptor model.
在六氢萘并恶嗪（4，PHNO）的1-位用硫原子或氮原子取代氧原子，分别得到六氢萘并噻嗪（6，PHNT）和八氢苯并喹喔啉（5，POBQ），并且在结合试验中9-OH-PHNT显示出对D-2多巴胺受体具有高亲和力；然后拆分了外消旋的9-OH-PHNT，并通过圆二色光谱确定了其绝对构型。（+）-9-OCH3-PHNT 12对D-2受体无活性，证实了麦克德姆受体模型的有效性。
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