2. Academic Validation
  3. (-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor

(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor

  • J Med Chem. 2000 Nov 2;43(22):4045-50. doi: 10.1021/jm000249r.
G Mullen 1,  J Napier,  M Balestra,  T DeCory,  G Hale,  J Macor,  R Mack,  J Loch 3rd,  E Wu,  A Kover,  P Verhoest,  A Sampognaro,  E Phillips,  Y Zhu,  R Murray,  R Griffith,  J Blosser,  D Gurley,  A Machulskis,  J Zongrone,  A Rosen,  J Gordon
Affiliations

Affiliation

  • 1 Department of Chemistry, AstraZeneca R&D Boston, 3 Biotech, One Innovation Drive, Worcester, Massachusetts 01605, USA. george.mullen@astrazeneca.com
PMID: 11063601 DOI: 10.1021/jm000249r
Abstract

Neuronal nicotinic acetylcholine receptors are members of the ligand-gated ion channel receptor superfamily and may play important roles in modulating neurotransmission, cognition, sensory gating, and anxiety. Because of its distribution and abundance in the CNS, the alpha 7 nicotinic receptor is a strong candidate to be involved in some of these functions. In this paper we describe the synthesis and in vitro profile of AR-R17779, (-)-spiro[1-azabicyclo[2.2. 2]octane-3,5'-oxazolidin-2'-one] (4a), a potent full agonist at the rat alpha 7 nicotinic receptor, which is highly selective for the rat alpha 7 nicotinic receptor over the alpha 4 beta 2 subtype. Preliminary SAR of AR-R17779 presented here indicate that there is little scope for modification of this rigid molecule as even minor changes result in significant loss of the alpha 7 nicotinic receptor affinity.

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