Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2035-7. doi: 10.1016/s0960-894x(02)00310-4.

Abstract

Structure-activity relationship studies on novel non-imidazole, D-amino acid containing ligands of histamine 3 receptors are presented. A-304121 is a D-alanine piperazine amide with high affinity at the rat H(3) receptor.

MeSH terms

  • Acylation
  • Amino Acid Motifs
  • Amino Acids / chemistry*
  • Amino Acids / metabolism
  • Animals
  • Binding, Competitive
  • Biological Availability
  • Cerebral Cortex / metabolism
  • Histamine Antagonists / chemistry*
  • Histamine Antagonists / metabolism*
  • Humans
  • Kinetics
  • Ligands
  • Piperazines / chemistry
  • Rats
  • Receptors, Histamine H1 / metabolism
  • Receptors, Histamine H2 / metabolism
  • Receptors, Histamine H3 / drug effects
  • Receptors, Histamine H3 / metabolism*
  • Structure-Activity Relationship

Substances

  • Amino Acids
  • Histamine Antagonists
  • Ligands
  • Piperazines
  • Receptors, Histamine H1
  • Receptors, Histamine H2
  • Receptors, Histamine H3