The pharmacology of the piperidine dicarboxylates on the crustacean neuromuscular junction. 1984

A E McBain, and H V Wheal, and J F Collins

The effects of the four cis-piperidine dicarboxylate analogues (PDAs) on the neuromuscular junction of the hermit crab (Eupagurus bernhardus) were examined. Intracellular recordings of evoked excitatory junction potentials (EJPs) and the membrane potential were made. All four analogues were active as agonists and depolarized the fibre membrane. The dose-response curves for the 2,3 and 2,6-piperidine dicarboxylates were similar to that for L-glutamate but were one tenth as potent. The dose-response curves for the 2,4 and 2,5-piperidine dicarboxylates had shallower gradients and lower maxima indicating lower potencies. The piperidine dicarboxylates non-competitively antagonized and glutamate-induced potential and reversibly attenuated the amplitude of the junction potential, with no change in membrane input resistance. The decrease in amplitude of the glutamate-induced potentials produced by a train of ionophoretic pulses was reversibly blocked by incubation with any of the dicarboxylates. The results indicate that the piperidine dicarboxylates prevent the development of receptor desensitization. The significance of these findings is discussed.

UI MeSH Term Description Entries
D008564 Membrane Potentials The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization). Resting Potentials,Transmembrane Potentials,Delta Psi,Resting Membrane Potential,Transmembrane Electrical Potential Difference,Transmembrane Potential Difference,Difference, Transmembrane Potential,Differences, Transmembrane Potential,Membrane Potential,Membrane Potential, Resting,Membrane Potentials, Resting,Potential Difference, Transmembrane,Potential Differences, Transmembrane,Potential, Membrane,Potential, Resting,Potential, Transmembrane,Potentials, Membrane,Potentials, Resting,Potentials, Transmembrane,Resting Membrane Potentials,Resting Potential,Transmembrane Potential,Transmembrane Potential Differences
D009469 Neuromuscular Junction The synapse between a neuron and a muscle. Myoneural Junction,Nerve-Muscle Preparation,Junction, Myoneural,Junction, Neuromuscular,Junctions, Myoneural,Junctions, Neuromuscular,Myoneural Junctions,Nerve Muscle Preparation,Nerve-Muscle Preparations,Neuromuscular Junctions,Preparation, Nerve-Muscle,Preparations, Nerve-Muscle
D010875 Pipecolic Acids Acids, Pipecolic
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005071 Evoked Potentials Electrical responses recorded from nerve, muscle, SENSORY RECEPTOR, or area of the CENTRAL NERVOUS SYSTEM following stimulation. They range from less than a microvolt to several microvolts. The evoked potential can be auditory (EVOKED POTENTIALS, AUDITORY), somatosensory (EVOKED POTENTIALS, SOMATOSENSORY), visual (EVOKED POTENTIALS, VISUAL), or motor (EVOKED POTENTIALS, MOTOR), or other modalities that have been reported. Event Related Potential,Event-Related Potentials,Evoked Potential,N100 Evoked Potential,P50 Evoked Potential,N1 Wave,N100 Evoked Potentials,N2 Wave,N200 Evoked Potentials,N3 Wave,N300 Evoked Potentials,N4 Wave,N400 Evoked Potentials,P2 Wave,P200 Evoked Potentials,P50 Evoked Potentials,P50 Wave,P600 Evoked Potentials,Potentials, Event-Related,Event Related Potentials,Event-Related Potential,Evoked Potential, N100,Evoked Potential, N200,Evoked Potential, N300,Evoked Potential, N400,Evoked Potential, P200,Evoked Potential, P50,Evoked Potential, P600,Evoked Potentials, N100,Evoked Potentials, N200,Evoked Potentials, N300,Evoked Potentials, N400,Evoked Potentials, P200,Evoked Potentials, P50,Evoked Potentials, P600,N1 Waves,N2 Waves,N200 Evoked Potential,N3 Waves,N300 Evoked Potential,N4 Waves,N400 Evoked Potential,P2 Waves,P200 Evoked Potential,P50 Waves,P600 Evoked Potential,Potential, Event Related,Potential, Event-Related,Potential, Evoked,Potentials, Event Related,Potentials, Evoked,Potentials, N400 Evoked,Related Potential, Event,Related Potentials, Event,Wave, N1,Wave, N2,Wave, N3,Wave, N4,Wave, P2,Wave, P50,Waves, N1,Waves, N2,Waves, N3,Waves, N4,Waves, P2,Waves, P50
D005971 Glutamates Derivatives of GLUTAMIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the 2-aminopentanedioic acid structure. Glutamic Acid Derivatives,Glutamic Acids,Glutaminic Acids
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D018698 Glutamic Acid A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM. Aluminum L-Glutamate,Glutamate,Potassium Glutamate,D-Glutamate,Glutamic Acid, (D)-Isomer,L-Glutamate,L-Glutamic Acid,Aluminum L Glutamate,D Glutamate,Glutamate, Potassium,L Glutamate,L Glutamic Acid,L-Glutamate, Aluminum
D033381 Anomura An infraorder of CRUSTACEA, in the order DECAPODA comprising the hermit crabs and characterized by a small fifth pair of legs. Hermit Crab,Pagurus,Paralithodes,Hermit Crabs,Anomuras,Crab, Hermit,Crabs, Hermit,Paralithode
D066298 In Vitro Techniques Methods to study reactions or processes taking place in an artificial environment outside the living organism. In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In

Related Publications

A E McBain, and H V Wheal, and J F Collins
April 1950, The Journal of pharmacology and experimental therapeutics,
A E McBain, and H V Wheal, and J F Collins
January 1974, Acta anaesthesiologica Belgica,
A E McBain, and H V Wheal, and J F Collins
July 1969, Anesthesiology,
A E McBain, and H V Wheal, and J F Collins
January 1976, Comparative biochemistry and physiology. C: Comparative pharmacology,
A E McBain, and H V Wheal, and J F Collins
June 1961, [Seitai no kagaku] [Science of the living body],
A E McBain, and H V Wheal, and J F Collins
September 1975, Comparative biochemistry and physiology. B, Comparative biochemistry,
A E McBain, and H V Wheal, and J F Collins
May 1974, British journal of pharmacology,
A E McBain, and H V Wheal, and J F Collins
August 1984, Neuroscience letters,
Copied contents to your clipboard!