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Identification and Pharmacological Profile of a New Class of Selective Nicotinic Acetylcholine Receptor Potentiators
  • L. Broad, R. Zwart, E. Sher
  • Biology, Chemistry
    Journal of Pharmacology and Experimental…
  • 1 September 2006
Three novel (2-amino-5-keto)thiazole compounds that act as selective potentiators of nicotinic acetylcholine receptors are discovered, which should help in clarifying the potential therapeutic utility of selective nAChR modulation for the treatment of central nervous system disorders.
Recent progress in the development of subtype selective nicotinic acetylcholine receptor ligands.
The first 1000 fold selective low molecular weight ligands from the AstraZeneca group are described and the first subtype specific channel modulators are commented on.
LY290181, an Inhibitor of Diabetes-Induced Vascular Dysfunction, Blocks Protein Kinase C—Stimulated Transcriptional Activation Through Inhibition of Transcription Factor Binding to a Phorbol Response
The results suggest that LY290181 may inhibit diabetes-induced vascular dysfunction by inhibiting transcription factor binding to specific PKC-regulated genes involved in vascular function.
Inhibition of vascular smooth muscle cell proliferation and arterial intimal thickening by a novel antiproliferative naphthopyran.
It is demonstrated that naphthopyrans LY290181 and LY290293 are potent inhibitors of smooth muscle cell proliferation in vitro and that they produce substantial reduction in arterial intimal thickening in a balloon injury model when administered systemically.
Oxidative 5-endo cyclization of enamides mediated by ceric ammonium nitrate.
The methodology was used to synthesize the basic heterocyclic ring fragments of the natural products L-755,807, Quinolacticin C, and PI-091.