A novel super-potent neurokinin A receptor antagonist containing dehydroalanine

Bioorg Med Chem Lett. 1998 May 19;8(10):1153-6. doi: 10.1016/s0960-894x(98)00178-4.

Abstract

We report here the synthesis and preliminary pharmacological characterization of a novel Neurokinin A receptor antagonist. This molecule contains a dehydroalanine residue. It displays a high conformational rigidity and possesses very high activity. Its pharmacological properties as a neurokinin A receptor antagonist were assessed in in vitro experiments on rat vas deferens and were compared to those of Neuronorm and MEN10627.

Publication types

  • Comparative Study

MeSH terms

  • Alanine / analogs & derivatives*
  • Amino Acid Sequence
  • Animals
  • Male
  • Models, Molecular
  • Molecular Structure
  • Peptides, Cyclic / chemical synthesis*
  • Peptides, Cyclic / chemistry
  • Peptides, Cyclic / pharmacology*
  • Protein Conformation
  • Rats
  • Receptors, Neurokinin-2 / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Vas Deferens / drug effects
  • Vas Deferens / physiology

Substances

  • Peptides, Cyclic
  • Receptors, Neurokinin-2
  • neuronorm
  • neuronorm, delta-Ala(1)-
  • MEN 10627
  • dehydroalanine
  • Alanine