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Related Concept Videos

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
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...
Antidepressant Drugs: MAOIs and Other Agents01:23

Antidepressant Drugs: MAOIs and Other Agents

Atypical antidepressants, including bupropion (Wellbutrin), mirtazapine (Remeron), nefazodone (Serzone), trazodone (Desyrel), and vilazodone (Viibryd), offer unique mechanisms of action. Bupropion weakly inhibits dopamine and norepinephrine reuptake, aiding depression treatment and smoking cessation, with a low risk of sexual dysfunction. Mirtazapine enhances serotonin and norepinephrine neurotransmission, leading to sedation, increased appetite, and weight gain. As a result, it helps treat...
Neurochemical Transmission: Sites of Drug Action01:26

Neurochemical Transmission: Sites of Drug Action

Neurochemical transmission, the conduction of electrical impulses between neurons mediated by neurotransmitters, plays a vital role in various physiological processes. Autonomic drugs exert their effects by modulating neurotransmission within the autonomic nervous system. For instance, drugs such as hemicholinium block the precursor uptake necessary for synthesizing acetylcholine, an essential autonomic neurotransmitter. Following synthesis, neurotransmitters are stored in vesicles. Metyrosine...
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...
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: Jul 3, 2026

Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome
08:49

Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome

Published on: September 23, 2015

Fine-tuning serotonin2c receptor function in the brain: molecular and functional implications.

Kelly A Berg1, William P Clarke, Kathryn A Cunningham

  • 1Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX 78229-3900, USA.

Neuropharmacology
|July 8, 2008
PubMed
Summary

The serotonin 2C receptor (5-HT2CR) regulates brain excitability and dopamine function. Targeting this receptor offers potential for treating neuropsychiatric disorders like depression and Parkinson's disease.

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A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices
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A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices

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Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome
08:49

Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome

Published on: September 23, 2015

A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices
07:56

A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices

Published on: August 11, 2021

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • The serotonin 2C receptor (5-HT2CR) is a 7-transmembrane-spanning receptor.
  • It exhibits unique properties including constitutive activity and RNA editing.
  • Widely expressed in the central nervous system, it regulates neuronal excitability.

Purpose of the Study:

  • To review the functional status of the central 5-HT2CR.
  • To highlight its regulatory properties, constitutive activity, and RNA editing.
  • To explore its therapeutic potential for neuropsychiatric disorders.

Main Methods:

  • Review of molecular, cellular, anatomical, biochemical, and behavioral studies.
  • Analysis of receptor function, including constitutive activity and RNA editing.
  • Evaluation of therapeutic strategies targeting 5-HT2CR.

Main Results:

  • 5-HT2CR modulates dopamine neuron function.
  • Constitutive activity and RNA editing significantly impact 5-HT2CR function in vivo.
  • Inverse agonism represents a promising therapeutic avenue.

Conclusions:

  • The 5-HT2CR is a key regulator of central nervous system function.
  • Its unique properties present novel therapeutic opportunities.
  • Targeting 5-HT2CR offers potential for treating depression, schizophrenia, Parkinson's disease, and addiction.