Novel non-peptide ligands for the somatostatin sst3 receptor

Bioorg Med Chem Lett. 2001 Apr 23;11(8):991-5. doi: 10.1016/s0960-894x(01)00107-x.

Abstract

A series of imidazole derivatives has been prepared using high throughput parallel synthesis. Several compounds showed high affinity (Ki in 10(-6)-10(-8) M range) and selectivity at recombinant human somatostatin receptor subtype 3 (hsst3).

MeSH terms

  • Amides / chemical synthesis
  • Amides / pharmacology*
  • Animals
  • Binding Sites / physiology
  • CHO Cells
  • Colforsin / pharmacology*
  • Cricetinae
  • Cyclic AMP / agonists*
  • Cyclic AMP / analysis
  • Cyclic AMP / biosynthesis
  • Dose-Response Relationship, Drug
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / pharmacology
  • Ligands
  • Nitrobenzenes / chemical synthesis
  • Nitrobenzenes / pharmacology*
  • Protein Binding / physiology
  • Receptors, Somatostatin / antagonists & inhibitors*
  • Recombinant Proteins / antagonists & inhibitors
  • Somatostatin / pharmacology*

Substances

  • Amides
  • Imidazoles
  • L796778
  • Ligands
  • Nitrobenzenes
  • Receptors, Somatostatin
  • Recombinant Proteins
  • somatostatin receptor 3
  • Colforsin
  • Somatostatin
  • Cyclic AMP