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Related Concept Videos

Adrenergic Agonists: Direct-Acting Agents01:30

Adrenergic Agonists: Direct-Acting Agents

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
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...
Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

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.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
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...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...

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Related Experiment Video

Updated: May 16, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Small molecule amides as potent ROR-γ selective modulators.

Pasha M Khan1, Bahaa El-Dien M El-Gendy, Naresh Kumar

  • 1Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.

Bioorganic & Medicinal Chemistry Letters
|December 13, 2012
PubMed
Summary

Researchers studied diphenylpropanamide compounds that modulate ROR-γ (Retinoic acid receptor-related Orphan Receptor gamma). The lead compound showed promise as an in vivo probe for studying ROR-γ functions in disease models.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

Area of Science:

  • Medicinal Chemistry
  • Molecular Pharmacology
  • Endocrinology

Background:

  • Retinoic acid receptor-related Orphan Receptor gamma (ROR-γ) is a nuclear receptor with critical roles in immune regulation and metabolism.
  • Dysregulation of ROR-γ activity is implicated in various diseases, making it a therapeutic target.

Purpose of the Study:

  • To investigate the structure-activity relationship (SAR) of a novel series of diphenylpropanamide compounds as selective ROR-γ modulators.
  • To identify potent and selective ROR-γ modulators with suitable pharmacokinetic properties for in vivo studies.

Main Methods:

  • Synthesis and chemical modification of a diphenylpropanamide scaffold targeting three distinct regions.
  • Screening of synthesized compounds using a Gal4-DBD-NR ligand binding domain cotransfection assay to assess ROR-γ transcriptional activity.
  • Evaluation of in vitro and in vivo pharmacokinetic profiles of lead compounds.

Main Results:

  • Several diphenylpropanamide derivatives demonstrated potent repression of ROR-γ transcriptional activity.
  • Structural modifications influenced compound potency and selectivity.
  • Lead compound 1 exhibited modest mouse pharmacokinetics and an acceptable in vitro profile.

Conclusions:

  • The study successfully identified diphenylpropanamide derivatives as effective ROR-γ modulators.
  • Lead compound 1 serves as a valuable in vivo probe for further investigation of ROR-γ functions in disease pathogenesis.
  • This work provides a foundation for developing ROR-γ-targeted therapeutics.