The actions of 'selective' excitatory amino acid antagonists on the crustacean neuromuscular junction

Neurosci Lett. 1984 Aug 24;49(1-2):217-22. doi: 10.1016/0304-3940(84)90163-0.

Abstract

Intracellular recordings of neurally evoked excitatory junction potentials were made from the hermit crab neuromuscular junction and the effects of a series of putative antagonists, including the phosphonic amino acids, were examined for their effectiveness. The most potent antagonists were (+/-)2-amino-5-phosphonohexanoic acid and (+/-) 2-amino-5-phosphonovaleric acid while glutamate diethyl ester, DL-alpha-aminoadipate, 2-amino-7-phosphonoheptanoic acid and gamma-D-glutamylglycine were less effective. None of the compounds produced a change in membrane input resistance, but pyridine-2,5-dicarboxylic acid depolarized the muscle membrane and this probably accounted for its apparent antagonist properties. All the compounds readily and reversibly, but not competitively, antagonized the ionophoretic L-glutamate-induced depolarization. Since none of the compounds was capable of producing complete antagonism it is concluded that a more potent and competitive antagonist is required.

Publication types

  • Comparative Study

MeSH terms

  • 2-Amino-5-phosphonovalerate
  • 2-Aminoadipic Acid / pharmacology
  • Amino Acids / pharmacology
  • Animals
  • Anomura
  • Dipeptides / pharmacology
  • Excitatory Amino Acid Antagonists*
  • Glutamates / pharmacology
  • Glutamic Acid
  • Neuromuscular Junction / drug effects*
  • Norleucine / analogs & derivatives
  • Norleucine / pharmacology
  • Pyridines / pharmacology
  • Synaptic Transmission / drug effects*
  • Valine / analogs & derivatives
  • Valine / pharmacology

Substances

  • Amino Acids
  • Dipeptides
  • Excitatory Amino Acid Antagonists
  • Glutamates
  • Pyridines
  • glutamic acid diethyl ester
  • gamma-glutamylglycine
  • 2-Aminoadipic Acid
  • Glutamic Acid
  • 2,5-Pyridinedicarboxylic acid
  • 2-Amino-5-phosphonovalerate
  • 2-amino-6-phosphonohexanoic acid
  • Norleucine
  • Valine
  • 2-amino-7-phosphonoheptanoic acid