ChemInform Abstract: Synthesis and Single Cell Pharmacology of Potential Heterocyclic Bioisosteres of the Excitatory Amino Acid Antagonist Glutamic Acid Diethyl Ester.

ChemInform ◽  
1990 ◽  
Vol 21 (16) ◽  
Author(s):  
U. MADSEN ◽  
E. O. NIELSEN ◽  
D. R. CURTIS ◽  
D. T. BEATTIE ◽  
P. KROGSGAARD-LARSEN
Keyword(s):  
Amino Acid ◽  
Glutamic Acid ◽  
Single Cell ◽  
Excitatory Amino Acid ◽  
Diethyl Ester ◽  
Acid Antagonist ◽  
Glutamic Acid Diethyl Ester

scholarly journals Synthesis and Single Cell Pharmacology of Potential Heterocyclic Bioisosteres of the Excitatory Amino Acid Antagonist Glutamic Acid Diethyl Ester.

1990 ◽  
Vol 44 ◽  
pp. 96-102 ◽  
Author(s):  
Ulf Madsen ◽  
Elsebet Ø. Nielsen ◽  
David R. Curtis ◽  
David T. Beattie ◽  
Povl Krogsgaard-Larsen ◽  
...  
Keyword(s):  
Amino Acid ◽  
Glutamic Acid ◽  
Single Cell ◽  
Excitatory Amino Acid ◽  
Diethyl Ester ◽  
Acid Antagonist ◽  
Glutamic Acid Diethyl Ester

Blockade of hyperbaric oxygen induced seizures by excitatory amino acid antagonists

1985 ◽  
Vol 63 (5) ◽  
pp. 519-521 ◽  
Author(s):  
Carol A. Colton ◽  
Joel S. Colton
Keyword(s):  
High Pressure ◽  
Amino Acid ◽  
Glutamic Acid ◽  
Hyperbaric Oxygen ◽  
Excitatory Amino Acid ◽  
Diethyl Ester ◽  
Amino Acid Antagonists ◽  
Excitatory Amino Acid Antagonists ◽  
Higher Doses ◽  
Glutamic Acid Diethyl Ester

The effectiveness of several excitatory amino acid antagonists to delay or block seizures induced by oxygen at high pressure was examined in mice. Of the antagonists tested, namely, L-proline, DL-α-aminoadipate, DL-2-amino-5-phosphonovalerate, and L-glutamic acid diethyl ester, DL-2-amino-5-phosphonovalerate was the most effective in delaying or preventing seizures. L-Glutamic acid diethylester was also effective but at significantly higher doses, which were also associated with marked sedation.

Inhibition of the early phase of free fatty liberation during cerebral ischemia by excitatory amino acid antagonist administered

1994 ◽  
Vol 635 (1-2) ◽  
pp. 331-334 ◽  
Author(s):  
Yoichi Katayawa ◽  
Tatsuro Kawata ◽  
Takeshi Maeda ◽  
Koichi Ishikawa ◽  
Takashi Tsubokawa
Keyword(s):  
Amino Acid ◽  
Cerebral Ischemia ◽  
Early Phase ◽  
Excitatory Amino Acid ◽  
Acid Antagonist

The excitatory amino acid antagonist d-CPP-ene (SDZ EAA-494) in patients with epilepsy

1993 ◽  
Vol 16 (2) ◽  
pp. 165-174 ◽  
Author(s):  
S. Sveinbjornsdottir ◽  
J.W.A.S. Sander ◽  
D. Upton ◽  
P.J. Thompson ◽  
P.N. Patsalos ◽  
...  
Keyword(s):  
Amino Acid ◽  
Excitatory Amino Acid ◽  
Acid Antagonist ◽  
Patients With Epilepsy

Excitatory amino acid receptors of guinea pig medial nucleus tractus solitarius neurons

1990 ◽  
Vol 259 (5) ◽  
pp. H1389-H1395 ◽  
Author(s):  
J. A. Drewe ◽  
R. Miles ◽  
D. L. Kunze
Keyword(s):  
Amino Acid ◽  
Glutamate Receptor ◽  
Nucleus Tractus Solitarius ◽  
Excitatory Amino Acid ◽  
Membrane Conductance ◽  
Diethyl Ester ◽  
Receptor Subtypes ◽  
Amino Acid Receptors ◽  
Medial Nucleus ◽  
Inward Currents

Neurons isolated from the medial subnuclei of nucleus tractus solitarius in adult guinea pigs were studied for responses to the excitatory amino acid glutamate and its analogues using the whole cell tight-seal voltage clamp technique. In 80% of the cells studied (n = 60) 100 microM glutamate produced inward currents at negative voltages. To further characterize the glutamate response, the agonists for three glutamate receptor subtypes, N-methyl-D-aspartate (NMDA), kainate, and quisqualate, were examined for their effects on membrane conductance. NMDA (25-250 microM) activated currents in 85% of the neurons tested (n = 30). NMDA currents were generally very small in amplitude. Of the neurons tested, 84% responded to kainate (10-30 microM, n = 19) and only 50% to quisqualate (25-50 microM, n = 26). The conductance activated by NMDA was outwardly rectifying. The conductance activated by kainate was voltage independent, while that activated by quisqualate showed varying degrees of outward rectification. Responses to NMDA were specifically antagonized by DL-2-amino-5-phosphonovaleric acid (AP-5, 50-100 microM). Kainate responses were blocked by kynurenate at concentrations (0.5-1.5 mM) ineffective on quisqualate-induced current. Glutamic acid diethyl ester (GDEE, 2-15 mM) was effective in reducing quisqualate responses at concentrations that had no effect on kainate responses. This characterization of the glutamate receptor subtypes and effective antagonists provides a basis for future determination of the specific receptor of glutamate responsible for mediation of the excitatory postsynaptic potentials produced by activation of the baroreceptor input.

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