Xylamine, a ligand for the catecholamine transporter
Thesis/Dissertation
·
OSTI ID:6990819
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 identifying the catecholamine transporter, particularly in conjunction with procedures for protein purification and reconstitution.
- Research Organization:
- California Univ., Los Angeles (USA)
- OSTI ID:
- 6990819
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
550201 -- Biochemistry-- Tracer Techniques
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMAL CELLS
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
BRAIN
CARDIOTONICS
CARDIOVASCULAR AGENTS
CATECHOLAMINES
CENTRAL NERVOUS SYSTEM
DOPAMINE
DRUGS
HYDROXY COMPOUNDS
INHIBITION
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
NERVE CELLS
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
PROTEINS
RADIORECEPTOR ASSAY
RATS
RECEPTORS
RODENTS
SOMATIC CELLS
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UPTAKE
VERTEBRATES
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AMINES
ANIMAL CELLS
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
BRAIN
CARDIOTONICS
CARDIOVASCULAR AGENTS
CATECHOLAMINES
CENTRAL NERVOUS SYSTEM
DOPAMINE
DRUGS
HYDROXY COMPOUNDS
INHIBITION
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
NERVE CELLS
NERVOUS SYSTEM
NEUROREGULATORS
ORGANIC COMPOUNDS
ORGANS
PHENOLS
POLYPHENOLS
PROTEINS
RADIORECEPTOR ASSAY
RATS
RECEPTORS
RODENTS
SOMATIC CELLS
SYMPATHOMIMETICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UPTAKE
VERTEBRATES