Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2067-70. doi: 10.1016/s0960-894x(01)00414-0.

Abstract

The synthesis and structure-activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. L-Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC(50) 0.63 microM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat formalin-induced pain model by intrathecal and oral administration.

MeSH terms

  • Amino Acids / chemical synthesis
  • Amino Acids / chemistry
  • Amino Acids / pharmacology*
  • Amino Acids / therapeutic use
  • Analgesics / chemical synthesis
  • Analgesics / chemistry
  • Analgesics / pharmacology*
  • Analgesics / therapeutic use
  • Animals
  • Calcium Channel Blockers / chemical synthesis
  • Calcium Channel Blockers / chemistry
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channel Blockers / therapeutic use
  • Calcium Channels, N-Type / drug effects
  • Calcium Channels, N-Type / metabolism*
  • Disease Models, Animal
  • Formaldehyde
  • Pain / chemically induced
  • Pain / drug therapy
  • Rats
  • Structure-Activity Relationship

Substances

  • Amino Acids
  • Analgesics
  • Calcium Channel Blockers
  • Calcium Channels, N-Type
  • Formaldehyde