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Related Concept Videos

Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

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An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
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The combined effects of drugs can result in various interactions, of which an important type is antagonism. Antagonism is a mechanism where one drug inhibits or counteracts the effects of another drug. Antagonism can occur through various means, including receptor binding, allosteric modulation, functional interaction, chemical reactions, and pharmacokinetic processes.
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Antipsychotic drugs are classified into first-generation (typical) drugs including phenothiazines; and second-generation (atypical) drugs. Chlorpromazine hydrochloride (Thorazine), a phenothiazine derivative, broadly impacts the central, autonomic, and endocrine systems. This drug, along with typical agents like haloperidol (Haldol), primarily works by antagonizing D2 receptors, thus reducing dopaminergic neurotransmission. However, typical antipsychotics can cause side effects such as sedation...
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Drug-Receptor Interaction: Agonist01:25

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Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
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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...
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Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
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Related Experiment Video

Updated: May 6, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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D-Cycloserine: Agonist turned antagonist.

T H Lanthorn1

  • 1Lightning Neurotech, 537 Majestic Court, 60031-3228, Gurnee, Illinois, USA.

Amino Acids
|November 6, 2013
PubMed
Summary

D-Cycloserine enhances learning and memory by activating NMDA receptors. However, these benefits diminish with repeated use or high doses, potentially due to feedback inhibition.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Cognitive Science

Background:

  • D-Cycloserine modulates NMDA receptor activity.
  • NMDA receptor activation is crucial for synaptic plasticity, including long-term potentiation (LTP).
  • Learning and memory processes are associated with LTP.

Purpose of the Study:

  • To investigate the effects of D-Cycloserine on learning and memory.
  • To explore the dose-dependent and chronic administration effects of D-Cycloserine.
  • To understand the underlying mechanisms of D-Cycloserine's efficacy and limitations.

Main Methods:

  • Review of existing animal and human studies on D-Cycloserine.
  • Analysis of D-Cycloserine's impact on NMDA receptor complex activation and LTP induction.

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  • Examination of clinical trial data for D-Cycloserine in age-associated memory impairment (AAMI) and Alzheimer's disease.

    • Main Results:

    • D-Cycloserine enhances NMDA receptor activation and LTP induction, improving learning and memory in the short term.
    • Repeated administration or higher doses of D-Cycloserine lead to diminished or lost enhancing effects.
    • Antagonist-like effects and inhibition of second messenger pathways are observed at higher doses or with chronic use.

    Conclusions:

    • D-Cycloserine shows potential for enhancing learning and memory via NMDA receptor modulation.
    • The therapeutic window for D-Cycloserine is narrow, with efficacy dependent on dosage and administration frequency.
    • Chronic D-Cycloserine treatment may be limited by feedback inhibition mechanisms, impacting its effectiveness in conditions like Alzheimer's disease.