A new pyridazine series of GABAA alpha5 ligands.

  title={A new pyridazine series of GABAA alpha5 ligands.},
  author={Monique B van Niel and Kevin A. Wilson and Charles H Adkins and John R. Atack and Jose L Alba Castro and Dawn E Clarke and Stephen D. Fletcher and Ute Gerhard and Mark M Mackey and Sallie Malpas and Karen Maubach and Robert Newman and Desmond O'connor and Gopalan V. Pillai and Peter B. Simpson and Steven R. Thomas and Angus M Macleod},
  journal={Journal of medicinal chemistry},
  volume={48 19},
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 alpha5 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 alpha5 receptor subtypes. 

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