Design and synthesis of highly potent and specific dynorphin derivatives for affinity labeling of kappa opioid receptors

Chem Pharm Bull (Tokyo). 1993 Jul;41(7):1312-4. doi: 10.1248/cpb.41.1312.

Abstract

Dynorphin A derivatives containing S-(3-nitro-2-pyridinesulfenyl)-cysteine(Cys(Npys)) were designed and synthesized for affinity labeling of kappa opioid receptors. Derivatives with Cys(Npys) residue at the 8 position were highly potent and specific to kappa receptors and bound to receptors through disulfide bond formation.

MeSH terms

  • Affinity Labels / chemical synthesis*
  • Amino Acid Sequence
  • Animals
  • Drug Design
  • Dynorphins / analogs & derivatives*
  • Dynorphins / chemical synthesis*
  • Guinea Pigs
  • In Vitro Techniques
  • Molecular Sequence Data
  • Rabbits
  • Receptors, Opioid, kappa / drug effects*

Substances

  • Affinity Labels
  • Receptors, Opioid, kappa
  • Dynorphins