Structural requirements for uptake into serotoninergic neurones.
Experiments were performed to examine whether non-hydroxylated tryptamines and 4-chloroamphetamine utilize the membrane 5-hydroxytryptamine carrier to pass into serotoninergic neurones. The accumulation and deamination of 14C-tryptamine by mouse brain slices or homogenates of rat hypothalamus were not inhibited by cocaine or norzimelidine, a selective inhibitor of the neuronal 5-HT uptake. The prevention by alpha-methyltryptamine (10 mg/kg, intraperitoneally), alpha-ethyltryptamine (20 mg/kg intraperitoneally) and 4-chloroamphetamine (20 mg/kg intraperitoneally) of the irreversible inhibtion of monoamine oxidase by pheniprazine (2.5 mg/kg intraperitoneally) and clorgyline (5 mg/kg intraperitoneally) in serotoninergic synaptosomes from mouse brain was not antagonized by pretreatment of the animals with norzimelidine (20 mg/kg intraperitoneally). The partial preventing effect of alpha-ethyl-4-methyl-m-tyramine (H 75/12)(2 X 50 mg/kg intraperitoneally) was, on the other hand, antagonized by norzimelidine. These results do not support the hypothesis that non-hydroxylated tryptamines and 4-chloroamphetamine are transported by the 5-HT carrier.
D000818:Animals; D001692:Biological Transport; D001921:Brain / Q000378:metabolism*; D001969:Bromobenzenes / Q000494:pharmacology; D003042:Cocaine / Q000494:pharmacology; D007031:Hypothalamus / Q000378:metabolism; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology; D009474:Neurons / Q000378:metabolism; D011725:Pyridines / Q000494:pharmacology; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000494:pharmacology; D014363:Tryptamines / Q000037:antagonists & inhibitors / Q000378:metabolism*; D015031:Zimeldine / Q000031:analogs & derivatives*; D010133:p-Chloroamphetamine / Q000378:metabolism
D001969:Bromobenzenes; D008996:Monoamine Oxidase Inhibitors; D011725:Pyridines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines; D012701:Serotonin; D015031:Zimeldine; C017578:norzimelidine; D010133:p-Chloroamphetamine; D003042:Cocaine