Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.

  title={Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.},
  author={Robert E Boyd and Jeffery B. Press and Caroline R. Rasmussen and Robert B Raffa and Ellen E. Codd and Caroline Connelly and Quan Sheng Li and Rebecca P Martinez and Mark A. Lewis and Harold R Almond and Allen B. Reitz},
  journal={Journal of medicinal chemistry},
  volume={44 6},
A series of imidazolylmethylthiophenes has been prepared and evaluated as ligands for the alpha(2) adrenoceptor. These compounds were tested in two animal models that are predictive of analgesic activity in humans. The 3-thienyl compounds were generally the most potent, particularly those with substitution in the 4-position. A subset of the most active compounds was further evaluated for adverse cardiovascular effects in the anesthetized rat model. In addition to excellent binding at the alpha… CONTINUE READING