Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28.

Abstract

Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs have been prepared and evaluated for their GPR88 agonist activity and pharmacokinetic (PK) properties.

Keywords: Agonist; GPR88; Phenyl amine; Phenylglycinol; Schizophrenia.

MeSH terms

  • Amines / chemical synthesis
  • Amines / chemistry
  • Amines / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Ethanolamines / chemical synthesis
  • Ethanolamines / chemistry
  • Ethanolamines / pharmacology*
  • HEK293 Cells
  • Humans
  • Molecular Structure
  • Receptors, G-Protein-Coupled / agonists*
  • Structure-Activity Relationship

Substances

  • Amines
  • Ethanolamines
  • GPR88 protein, human
  • Receptors, G-Protein-Coupled
  • N-phenylethanolamine