Home
Resources
Publications
Structure/activity Relations of N-methyl-D-aspartate Receptor Ligands as Studied by Their Inhibition of [3H]D-2-amino-5-phosphonopentanoic Acid Binding in Rat Brain Membranes

Structure/activity Relations of N-methyl-D-aspartate Receptor Ligands as Studied by Their Inhibition of [3H]D-2-amino-5-phosphonopentanoic Acid Binding in Rat Brain Membranes

H J Olverman, A W Jones, K N Mewett, J C Watkins

Neuroscience. 1988 Jul;26(1):17-31.

PMID: 2901691

Abstract:

Structure/activity relations of agonists and antagonists for the N-methyl-D-aspartate receptor have been investigated by measuring the ability of a large range of substances to inhibit binding of [3H]2-amino-5-phosphonopentanoate to rat brain membranes. A major difference between optimum structures for agonist and antagonist activity lay in the differential effectiveness of sulphonic and phosphonic acid groups as the omega-acidic terminal in these two types of compound. The sulphonic acid moiety was an effective omega-acidic terminal in short chain agonists, but not in longer chain antagonists, while the phosphonic acid group was the most effective omega-acidic terminal in longer chain antagonists, but was only very weakly active in short chain agonists. It is proposed that the binding site of the omega-acidic terminal of antagonists is different from that for the omega-acidic group of agonists. Other structural features conducive to effective interaction of ligands with the receptor are discussed.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP79055688-A	D(−)-2-Amino-5-phosphonopentanoic acid		79055-68-8	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: