Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0026838 (spasticity)
 6,471 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The adamantane derivative memantine (1-amino-3,5-dimethylaminoadamantane, D-145, Akatinol) is clinically used as well in the therapy of neurogenic motor diseases (e.g. spasticity) as in the treatment of cerebral disorders like coma, cerebrovascular and geronto-psychiatric disturbances. The aim of the paper is to summarize experimental evidences that may help to explain the clinical observations. Biochemical, pharmacological, and electrophysiological studies show that memantine interferes with the metabolism of the transmitters dopamine, noradrenaline (norepinephrine), and serotonin and modulates synaptic transMission. In order to explain the antispastic activity of memantine, a spinal action must be assumed in addition to the supraspinal effect on transmitter systems. Since memantine reduces the membrane resistance as well as the membrane conductance of sodium, potassium, and chloride ions, it is very likely that memantine Is directly involved in the generation of action potentials.
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PMID:[Pharmacodynamics and pharmacokinetics of memantine]. 635 2

The 1-aminoadamantanes memantine (1-amino-3,5-dimethyl-adamantane) and amantadine (1-amino-adamantane) are clinically used as anti-parkinsonian, 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 [3H](+)-pentazocine in homogenates of post-mortem human frontal cortex. The Ki values ranged from 0.237 +/- 0.019 microM for 1-N-dimethyl-amino-3,5-dimethyl-adamantane to 20.25 +/- 16.48 microM for amantadine. The Ki value of memantine was 19.98 +/- 3.08 microM and was thus very similar to that of amantadine. Memantine, at therapeutic concentrations, probably does not interact with the sigma binding site. Amantadine, at therapeutic concentrations, probably binds both to the sigma site and to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA) receptor.
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PMID:Affinity of 1-aminoadamantanes for the sigma binding site in post-mortem human frontal cortex. 830 17