University of Hertfordshire

From the same journal

By the same authors

A New Pyridazine Series of GABAA α5 Ligands

Research output: Contribution to journalArticle

  • M.B. Van Niel
  • K. Wilson
  • C.H. Adkins
  • J.R. Atack
  • J.L. Castro
  • D.E. Clarke
  • S. Fletcher
  • U. Gerhard
  • M.M. Mackey
  • S. Malpas
  • K. Maubach
  • R. Newman
  • D. O'Connor
  • G.V. Pillai
  • P.B. Simpson
  • S.R. Thomas
  • A.M. MacLeod
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Original languageEnglish
Number of pages8
Pages (from-to)6004-6011
JournalJournal of Medicinal Chemistry
Journal publication date22 Sep 2005
Volume48
Issue19
DOIs
Publication statusPublished - 22 Sep 2005

Abstract

Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA α5 receptor subtypes.

ID: 940958