Abstract
The ability of quisqualic acid (1) to sensitize neurons to depolarization by ω-phosphono α-amino acid analogues of excitatory amino acids is a highly specific phenomenon and is termed the QUIS effect. In an attempt to elucidate the structure-activity relationships for this sensitization, analogues 2-6 of quisqualic acid have been synthesized. Compounds 4, 5, and 6 showed no quisqualate sensitization with respect to l-2-amino-6-phosphonohexanoic acid (l-AP6), while compounds 2 and 3 were 1/10 and 1/1000, respectively, as active as quisqualic acid in sensitizing neurons toward l-AP6.
Original language | English (US) |
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Pages (from-to) | 3939-3946 |
Number of pages | 8 |
Journal | Journal of medicinal chemistry |
Volume | 37 |
Issue number | 23 |
DOIs | |
State | Published - Nov 1 1994 |