Binding of an imidazopyridoindole at imidazoline I2 receptors

Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9. doi: 10.1016/j.bmcl.2003.09.092.

Abstract

3,5,6,11-Tetrahydro-2H-imidazo[1',2':1,2]pyrido[3,4-b]indole (10) might be viewed as a fusion structure of two classes of I(2) imidazoline receptor ligands: 2-(2-benzofuranyl)-2-imidazolines and beta-carbolines. Its high affinity (K(i)=7.3 nM) provides insight to how the two classes of agents might bind relative to one another at I(2) receptors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Imidazoles / chemistry
  • Imidazoles / metabolism*
  • Imidazoline Receptors
  • Indoles / chemistry
  • Indoles / metabolism*
  • Male
  • Protein Binding / physiology
  • Pyridones / chemistry
  • Pyridones / metabolism
  • Rats
  • Rats, Wistar
  • Receptors, Drug / metabolism*

Substances

  • Imidazoles
  • Imidazoline Receptors
  • Indoles
  • Pyridones
  • Receptors, Drug
  • imidazole