SYNTHESIS OF AZABICYCLIC PYRAZINE DERIVATIVES AS MUSCARINIC AGONISTS AND THE PREPARATION OF A CHLOROPYRAZINE ANALOG WITH FUNCTIONAL SELECTIVITY AT SUBTYPES OF THE MUSCARINIC RECEPTOR

被引:23
作者
BAKER, R
STREET, LJ
REEVE, AJ
SAUNDERS, J
机构
关键词
D O I
10.1039/c39910000760
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The synthesis of quinuclidine and azanorbornyl pyrazine derivatives has yielded highly potent and efficacious muscarinic agonists; chloro-substitution in the pyrazine ring of the quinuclidine analogue resulted in the formation of a derivative with both enantiomers displaying partial agonist character but, more importantly, functional selectivity at the M1, M2 and M3 sub-types of the muscarinic receptor.
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页码:760 / 762
页数:3
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