Holographic quantitative structure-activity relationships of tryptamine derivatives at NMDA, 5HT(1A) and 5HT(2A) receptors.

Tryptamine derivatives (Ts) were found to inhibit the binding of [³H]MK-801, [³H]ketanserin and [³H]8-OH-DPAT to rat brain membranes. [³H]MK-801 labels the NMDA (N-methyl-D-aspartate) receptor, a ionotropic glutamate receptor which controls synaptic plasticity and memory function in the brain, whereas [³H]ketanserin and [³H]8-OH-DPAT label 5HT(2A) and 5HT(1A) receptors, respectively. The inhibitory potencies of 64 Ts (as given by IC₅₀ values) were correlated with their structural properties by using the Holographic QSAR procedure (HQSAR).