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Title: Xylamine, a ligand for the catecholamine transporter

Previous studies have established xylamine (N-2'-chloro-ethyl-N-ethyl-2-methylbenzylamine) irreversibly inhibits neuronal norepinephrine uptake with no concomitant effect on other neurotransmitter systems. Since xylamine is thought to alkylate transport-associated sites in the plasma membrane of noradrenergic neurons, so the loss of endogenous norepinephrine may be a consequence of neuronal membrane damage resulting from the alkylation of membrane components. In these studies, xylamine, under in vitro conditions, irreversibly inhibited both neuronal norepinephrine and dopamine uptake in the rat cortex and striatum, respectively. The efficacy of xylamine as a neuronal dopamine uptake inhibitor appeared to depend on its ability to access dopaminergic neurons during tissue exposure to the drug. In sympathetically innervated peripheral tissues, (/sup 3/H)xylamine was accumulated in noradrenergic neurons in a carrier-dependent manner. Although the data suggested that xylamine was interacting with the norepinephrine uptake carrier, (/sup 3/H)xylamine exposure to isolated synaptic membranes from superior cervical ganglia revealed a large proportion of (/sup 3/H)xylamine binding that was not associated with the noradrenergic transporter. For a closer characterization of xylamine binding in synaptic membranes, brain tissue was chosen as a more practical source of these membranes. While these experiments did not meet with great success, xylamine remains potentially useful as a ligand for identifyingmore » the catecholamine transporter, particularly in conjunction with procedures for protein purification and reconstitution.« less
Authors:
Publication Date:
OSTI Identifier:
6990819
Resource Type:
Thesis/Dissertation
Resource Relation:
Other Information: Thesis (Ph. D.)
Publisher:
Univ. of California,Los Angeles, CA
Research Org:
California Univ., Los Angeles (USA)
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; 59 BASIC BIOLOGICAL SCIENCES; CATECHOLAMINES; RADIORECEPTOR ASSAY; DOPAMINE; UPTAKE; TRITIUM COMPOUNDS; AMINES; BRAIN; INHIBITION; LIGANDS; NERVE CELLS; RATS; RECEPTORS; ANIMAL CELLS; ANIMALS; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; BODY; CARDIOTONICS; CARDIOVASCULAR AGENTS; CENTRAL NERVOUS SYSTEM; DRUGS; HYDROXY COMPOUNDS; ISOTOPE APPLICATIONS; LABELLED COMPOUNDS; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; NEUROREGULATORS; ORGANIC COMPOUNDS; ORGANS; PHENOLS; POLYPHENOLS; PROTEINS; RODENTS; SOMATIC CELLS; SYMPATHOMIMETICS; TRACER TECHNIQUES; VERTEBRATES 550601* -- Medicine-- Unsealed Radionuclides in Diagnostics; 550201 -- Biochemistry-- Tracer Techniques