• Publications
  • Influence
A selective inhibitor of serotonin uptake: Lilly 110140, 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine.
Abstract Lilly 110140 is a highly selective inhibitor of serotonin uptake into synaptosomes of rat brain, unlike previous monoamine uptake inhibitors that also inhibit the uptake of norepinephrine
A new selective inhibitor for uptake of serotonin into synaptosomes of rat brain: 3-(p-trifluoromethylphenoxy). N-methyl-3-phenylpropylamine.
Lilly 110140 is a potent and selective inhibitor for uptake of 5-HT into synaptosomes of rat brain and its primary amine derivative did not block the in vivo uptake of NE into rat heart.
Comparison of 4-chloro-, 4-bromo- and 4-fluoroamphetamine in rats: Drug levels in brain and effects on brain serotonin metabolism
The failure of 4-fluoroamphetamine to produce a long-lasting depletion of brain serotonin like that produced by 4-chloroamphetamine or 4-bromoamphetamine may reflect the inability of the fluoro-compound to be metabolized in the same way as the other haloamphetamines.
Effect of an uptake inhibitor on serotonin metabolism in rat brain: studies with 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine (Lilly 110140).
Lilly 110140 had no effect on brain levels of tryptophan, serotonin, dopamine, or norepinephrine, but it decreased 5-hydroxyindoleacetic acid (5HIAA) levels, and reduced turnover was indicated by a decreased rate of fall in brain serotonin levels after p-chlorophenylalamine was given to inhibit serotonin synthesis.
Regulation of phenylethanolamine N-methyl transferase.
Phenylethanolamine N-methyl transferase catalyzes the methylation of norepinephrine, forming epinephrine in the adrenal medulla, and is inhibited by phenethylamines and other compounds structurally similar to its substrates, as well as by agents that bind to sulfhydryl groups.
Reversible and irreversible phases of serotonin depletion by 4-chloroamphetamine.
Findings indicate that the depletion of brain serotonin by 4-chloroamphetamine is initially reversible but that there is a gradual transition into an irreversible effect between 24 and 48 hr after 4- chloroamphetamine injection.
Effect of 3-(p-trifluoromethylphenoxy). N. N. methyl-3-phenylpropylamine on the depletion of brain serotonin by 4-chloroamphetamine.
The data suggest that 110140 is a specific drug for inhibiting uptake into serotoninergic neurons in the brain in rats, and suggests that reserpine does not require the membrane pump for entry into the neuron.
Blockade of amine depletion by nisoxetine in comparison to other uptake inhibitors.
Nisxetine is one of the more potent and specific inhibitors of norepinephrine uptake, differing remarkably from fluoxetine to which it is related structurally.
Properties of 8,9-dichloro-2,3,4,5-tetrahydro-1H-2-benzazepine, an inhibitor of norepinephrine N-methyltransferase.
LY134046 seems to be more selective than other currently known inhibitors of NMT and may be useful for pharmacologic intervention in the function of epinephrine-forming neurons in brain.