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Neurotoxicity of the psychedelic amphetamine, methylenedioxymethamphetamine.
  • C. J. Schmidt
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental…
  • 1987
The neurochemical effects of the unique psychedelic agent, methylenedioxymethamphetamine (MDMA), indicate it may be a serotonergic neurotoxin related to agents such as p-chloroamphetamine and could be partially blocked by the uptake inhibitor as long as 6 hr after drug administration. Expand
Phosphodiesterases in the CNS: targets for drug development
The current state of the art in the burgeoning field of phosphodiesterase pharmacology in the CNS is reviewed, with a focus on the treatment of psychiatric and neurodegenerative disorders. Expand
Immunohistochemical localization of PDE10A in the rat brain
Data suggest a role for PDE10A in regulating activity within both the striatonigral and striatopallidal pathways, and a second, distinct function for the enzyme in these regions. Expand
Inhibition of the striatum-enriched phosphodiesterase PDE10A: A novel approach to the treatment of psychosis
The results indicate that PDE10A regulates the activation of striatal medium spiny neurons through effects on cAMP- and cGMP-dependent signaling cascades and demonstrate that papaverine has efficacy in behavioral models predictive of antipsychotic activity. Expand
Genetic deletion of the striatum-enriched phosphodiesterase PDE10A: Evidence for altered striatal function
The findings suggest that PDE10A is involved in regulating striatal output, possibly by reducing the sensitivity of medium spiny neurons to glutamatergic excitation, and presents a novel treatment for psychosis. Expand
In vitro and in vivo neurochemical effects of methylenedioxymethamphetamine on striatal monoaminergic systems in the rat brain.
Comparisons of the stereoisomers of methylenedioxymethamphetamine and its n-desmethyl analog, methylenedioxyamphetamine, indicated two phases of serotonin depletion similar to those reported for p-chloroamphetamine, and the (+)-enantiomer of both drugs to be the more potent releasing agent. Expand
Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies.
The data indicate that MDL 100,907 has a clozapine-like profile of potential antipsychotic activity with low extrapyramidal sid-effect liability. Expand
5-HT2 receptors exert a state-dependent regulation of dopaminergic function: studies with MDL 100,907 and the amphetamine analogue, 3,4-methylenedioxymethamphetamine.
The results suggest a permissive role for 5-HT2 receptors in the activation of the dopamine system which occurs during states of high serotonergic activity or during conditions of elevated dopamine efflux with high D2 receptor occupancy. Expand
Methylenedioxymethamphetamine-induced hyperthermia and neurotoxicity are independently mediated by 5-HT2 receptors
Results demonstrate that the drugs tested do not antagonize MDMA-induced neurotoxicity by interfering with its effect on body temperature, and indicate that MDMA- induced hyperthermia may contribute to the development of the drug's long-term neurochemical effects. Expand
Guanine nucleotides are competitive inhibitors of N-methyl-D-aspartate at its receptor site both in vitro and in vivo.
Micromolar concentrations of guanine nucleotides and their analogs decreased both agonist and antagonist N-methyl-d-aspartate receptor-effector coupling by competitive antagonism at the glutamate binding site, rather than via interaction with an intracellularly located GTP-binding protein. Expand