Tecle H, Lauffer D J, Mirzadegan T, Moos W H, Moreland D W, Pavia M R, Schwarz R D, Davis R E
Parke-Davis Pharm. Res. Div., Warner-Lambert Co. Ann Arbor, MI 48105.
Life Sci. 1993;52(5-6):505-11. doi: 10.1016/0024-3205(93)90308-p.
The synthesis of a series of potent and efficacious 1-azabicyclo[2.2.1]heptan-3-one oxime muscarinic agonists is described. The oximes have extended appendages designed to span the cavity defined by the seven transmembrane helices of the muscarinic receptor. Some members of the series are selective for receptors of the m1 subtype. One such oxime, 31, shows affinity and functional selectivity for m1 over m2, m3, and m4 muscarinic receptor types.
本文描述了一系列强效且有效的1-氮杂双环[2.2.1]庚-3-酮肟类毒蕈碱激动剂的合成。这些肟类化合物具有延伸的基团，设计用于跨越毒蕈碱受体七个跨膜螺旋所界定的腔隙。该系列中的一些成员对m1亚型受体具有选择性。其中一种肟类化合物31，对m1受体的亲和力和功能选择性高于m2、m3和m4毒蕈碱受体类型。
