Detail of "78944-89-5"

Reference

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

The actions of 'selective' excitatory amino acid antagonists on the crustacean neuromuscular junction. King, Anne E.; Wheal, H. V. (Dep. Neurophysiol., Univ. Southampton, Southampton S09 3TU, UK). Neurosci. Lett., 49(1-2), 217-22 (English) 1984. CODEN: NELED5. ISSN: 0304-3940. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Intracellular recordings of neurally-evoked excitatory junction potentials were made from the hermit crab neuromuscular junction, and the effects of a putative antagonists, including the phosphoric amino acids, were examd. The most potent antagonists were (±)2-amino-6-phosphonohexanoic acid [78944-89-5] and (±)2-amino-5-phosphonovaleric acid [76326-31-3], whereas glutamate diEt ester [16450-41-2], DL-a-aminoadipate [626-71-1], 2-amino-7-phosphonoheptanoic acid [85797-13-3], and g-D-glutamylglycine [6729-55-1] were less effective. None of the compds. produced a change in membrane input resistance, but pyridine-2,5-dicarboxylic acid [100-26-5] depolarized the muscle membrane, and this probably accounted for its apparent antagonist properties. All the compds. readily and reversibly, but not competitively, antagonized the iontophoretic L-glutamate [56-86-0]-induced depolarization. Since none of the compds. was capable of producing complete antagonism a more potent and competitive antagonist is required.

Binding of [3H]3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to rat brain membranes: a selective, high-affinity ligand for N-methyl-D-aspartate receptors

Binding of [3H]3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to rat brain membranes: a selective, high-affinity ligand for N-methyl-D-aspartate receptors. Murphy, Deborah E.; Schneider, Josef; Boehm, Charles; Lehmann, John; Williams, Michael (Drug Discovery Div., Ciba-Geigy Corp., Summit, NJ 07901, USA). 4741-41-7 and 499-83-2 are also occured in this study. J. Pharmacol. Exp. Ther., 240(3), 778-84 (English) 1987. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 3H-labeled racemic 3-(2-carboxypiperazin-4-yl)propyl-1-phosphoric acid (CPP) [100828-16-8] a rigid analog of 2-amino-7-phosphonoheptanoic acid, bound with relatively high affinity (Kd = 201 nM) to Triton-treated rat brain crude synaptic membranes using a centrifugation assay. Binding was saturable, reversible, heat sensitive and dependent on protein concn. Specific binding, which represented 75 to 85% of the total counts bound, was enriched synaptosomal and microsomal fractions of rab brtain, suggesting an involvement in events related to synaptic transmission. On a regional basis, binding was highest in hippocampus, followed by cortex > striatum > cerebellum = thalamus. No specific binding could be detected in pons medulla or in liver, kidney, heart, lung and adrenal tissue. [3H]CPP binding was stereoselectively responsive to the isomers of glutamate, 2-amino-5-phosphonopentanoic acid, homocysteic acid, a-aminoadipic acid and N-methylaspartate. The most potent compds. tested were L-glutamate [56-86-0] and CPP, which were equiactive in displacing [3H]CPP. The order of activity of other excitatory amino acid receptor ligands was D-2-amino-5-phosphonopentanoic acid [79055-68-8] > L-homocysteic acid [14857-77-3] 3 DL-2-amino-7-phosphonoheptanoic acid [78966-69-5] = D-aspartate [1783-96-6] = L-aspartate [56-84-8] > L-serine-O-sulfate [626-69-7] = D-a-aminoadipic acid [7620-28-2] = ibotenate [2552-55-8] > N-methyl-D-aspartate (NMDA) [6384-92-5] > DL-2-amino-6-phosphonohexanoic acid [78944-89-5] > quisqualate [52809-07-1] > N-methyl-L-aspartate [4226-18-0]. The quisqualate- and kainate-type receptor agonists DL-a-amino-3-hydroxy-5-methylisoxazole-4-propionate [74341-63-2] and kalinic acid [487-79-6], resp., had negligible activity at 100 mM. Binding was also unaffected by phencyclidine [77-10-1], dexoxadrol [4741-41-7], DL-2-amino-4-phosphonobutyric acid [20263-07-4] (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate [77086-21-6], g-D-glutamylaminomethylsulfonic acid [90237-02-8], g-aminobutyric acid [56-12-2] and baclofen [1134-47-0]. These results are consistent with [3H]CPP being a selective ligand for the N-methyl-D-aspartate excitatory amino acid receptor. The specificity and relatively high affinity of [3H]CPP, together with its high degree of specific binding, make this the current ligand of choice to evaluate NMDA receptors in vitro. .