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Related Concept Videos

Adrenergic Neurons: Neurotransmission01:27

Adrenergic Neurons: Neurotransmission

Postganglionic sympathetic fibers (except those supplying the sweat glands) releasing noradrenaline or norepinephrine are called noradrenergic or adrenergic neurons. Noradrenaline, dopamine, adrenaline, or epinephrine are collectively called "catecholamines" as they contain a catechol moiety and an amine side chain. The five stages of neurotransmitter release involve their synthesis, storage, release, reuptake and metabolism.
Synthesis: Catecholamine synthesis requires tyrosine, which is taken...
Drugs Affecting Neurotransmitter Synthesis01:29

Drugs Affecting Neurotransmitter Synthesis

Drugs affecting neurotransmitter synthesis can impact the adrenergic neuron and the synthesis of neurotransmitters. For example, α-methyltyrosine and carbidopa target specific enzymes involved in catecholamine synthesis. α-methyltyrosine inhibits the enzyme tyrosine hydroxylase, which converts tyrosine into dopamine. By blocking this enzyme, α-methyltyrosine reduces dopamine production and other catecholamines. Carbidopa, on the other hand, inhibits the enzyme dopa decarboxylase, which converts...
Drugs Affecting Neurotransmitter Release or Uptake01:21

Drugs Affecting Neurotransmitter Release or Uptake

Certain drugs can affect how neurotransmitters called catecholamines, are released or taken back up in the adrenergic neuron. They can have different effects on the body's sympathetic transmission. Reserpine, a natural compound found in the Rauwolfia shrub, blocks a transporter called vesicular monoamine transporter (VMAT), which leads to a buildup of catecholamines in the cell and reduces sympathetic transmission. Another drug called guanethidine works in multiple ways, including blocking...
Adrenergic Agonists: Indirect-Acting Agents01:25

Adrenergic Agonists: Indirect-Acting Agents

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...

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Related Experiment Video

Updated: Jun 29, 2026

Comprehensive Profiling of Dopamine Regulation in Substantia Nigra and Ventral Tegmental Area
09:54

Comprehensive Profiling of Dopamine Regulation in Substantia Nigra and Ventral Tegmental Area

Published on: August 10, 2012

Hydroxytyrosol increases norepinephrine transporter function in pheochromocytoma cells.

Berta Luzón-Toro1, Arjan Geerlings, Sabine Hilfiker

  • 1Institute of Parasitology and Biomedicine "López-Neyra", Spanish National Research Council (CSIC), 18100 Granada, Spain.

Nuclear Medicine and Biology
|October 14, 2008
PubMed
Summary

Hydroxytyrosol enhances norepinephrine transporter activity in pheochromocytoma cells. This suggests hydroxytyrosol may improve the effectiveness of (131)I-MIBG for diagnosing and treating tumors like pheochromocytomas.

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A Convenient Method for Extraction and Analysis with High-Pressure Liquid Chromatography of Catecholamine Neurotransmitters and Their Metabolites
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A Convenient Method for Extraction and Analysis with High-Pressure Liquid Chromatography of Catecholamine Neurotransmitters and Their Metabolites

Published on: March 1, 2018

Human Neural Organoids for Studying Brain Cancer and Neurodegenerative Diseases
09:36

Human Neural Organoids for Studying Brain Cancer and Neurodegenerative Diseases

Published on: June 28, 2019

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Last Updated: Jun 29, 2026

Comprehensive Profiling of Dopamine Regulation in Substantia Nigra and Ventral Tegmental Area
09:54

Comprehensive Profiling of Dopamine Regulation in Substantia Nigra and Ventral Tegmental Area

Published on: August 10, 2012

A Convenient Method for Extraction and Analysis with High-Pressure Liquid Chromatography of Catecholamine Neurotransmitters and Their Metabolites
13:35

A Convenient Method for Extraction and Analysis with High-Pressure Liquid Chromatography of Catecholamine Neurotransmitters and Their Metabolites

Published on: March 1, 2018

Human Neural Organoids for Studying Brain Cancer and Neurodegenerative Diseases
09:36

Human Neural Organoids for Studying Brain Cancer and Neurodegenerative Diseases

Published on: June 28, 2019

Area of Science:

  • Pharmacology
  • Oncology
  • Neuroscience

Background:

  • The norepinephrine transporter (NET) is crucial for the uptake of (131)I-MIBG, a radiopharmaceutical used for diagnosing and treating neuroendocrine tumors.
  • Limited therapeutic strategies exist to enhance NET activity for improved (131)I-MIBG delivery into tumor cells.

Purpose of the Study:

  • To investigate the potential of hydroxytyrosol, a natural antioxidant, to enhance NET function.
  • To explore the implications of hydroxytyrosol for combined therapy with (131)I-MIBG in pheochromocytoma treatment.

Main Methods:

  • Rat pheochromocytoma PC12 cells were utilized to assess NET activity.
  • Cells were incubated with radiolabeled norepinephrine in the presence of varying hydroxytyrosol concentrations.
  • Uptake and release of radiolabeled norepinephrine were measured to quantify NET function.

Main Results:

  • Hydroxytyrosol significantly increased norepinephrine transporter activity with rapid onset, independent of transporter expression levels.
  • Hydroxytyrosol reduced both spontaneous and evoked norepinephrine release.
  • Findings suggest hydroxytyrosol modulates pre-existing plasma membrane-associated NETs.

Conclusions:

  • Hydroxytyrosol demonstrates potent enhancement of norepinephrine transporter activity in pheochromocytoma cells.
  • Combinatorial therapy with hydroxytyrosol and (131)I-MIBG may offer improved diagnostic and therapeutic outcomes for pheochromocytomas.