Synthesis of azabicyclic pyrazine derivatives as muscarinic agonists and the preparation of a chloropyrazine analogue with functional selectivity at sub-types of the muscarinic receptor

1991; Royal Society of Chemistry; Issue: 11 Linguagem: Inglês

10.1039/c39910000760

ISSN

2050-5639

Autores

Raymond Baker, Leslie J. Street, Austin J. Reeve, John Saunders,

Tópico(s)

Nicotinic Acetylcholine Receptors Study

Resumo

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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