J. Kornhuber, K. Schoppmeyer, Peter Riederer
Dec 12, 1993
Citations
1
Influential Citations
66
Citations
Quality indicators
Journal
Neuroscience Letters
Abstract
Abstract The 1-aminoadamantanes memantine (1-amino-3,5-dimethyl-adamantane) and amantadine (1-amino-adamantane) are clinically used as antiparkinsonian, anti-spasticity, anti-dementia and antiviral drugs. In the present investigation we have tested a series of 1-aminoadamantane derivatives including memantine and amantadine for their ability to compete with [ 3 H](+)-pentazocine in homogenates of post-mortem human frontal cortex. The K i values ranged from 0.237 ± 0.019 μ M for 1- N -dimethyl-amino-3,5-dimethyl-adamantane to 20.25 ± 16.48 μ M for amantadine. The K i value of memantine was 19.98 ± 3.08 μ M and was thus very similar to that of amantadine. Memantine, at therapeutic concentrations, probably does not interact with the σ binding site. Amantadine, at therapeutic concentrations, probably binds both to the σ site and to the phencyclidine (PCP) binding site of the N- methyl- d -aspartate (NMDA) receptor.