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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...
Adrenergic Agonists: Therapeutic Uses01:30

Adrenergic Agonists: Therapeutic Uses

Adrenergic agonists have diverse therapeutic uses across various medical conditions and emergencies.
Emergency and Intensive Care Unit (ICU) applications: Pressor agents increase blood pressure, heart rate, and contractility in shock and organ failure situations. Dopamine can induce vasodilation and stimulate adrenoceptors. Endogenous catecholamines are effective in treating cardiogenic shock. α2-agonists like clonidine can reverse anesthesia-induced hypertension.
Allergies and anaphylaxis:...
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...
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase C—inositol-1,4,5-trisphosphate...

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Updated: May 26, 2026

HPLC-based Assay to Monitor Extracellular Nucleotide/Nucleoside Metabolism in Human Chronic Lymphocytic Leukemia Cells
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Emerging adenosine receptor agonists: an update.

Zhan-Guo Gao, Kenneth A Jacobson

    Expert Opinion on Emerging Drugs
    |December 14, 2011
    PubMed
    Summary
    This summary is machine-generated.

    Adenosine receptor agonists are in clinical trials for numerous conditions, including pain, cancer, and heart disease. Several drugs targeting these receptors are already approved for clinical use.

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    Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications

    Published on: January 27, 2014

    Area of Science:

    • Pharmacology
    • Drug Discovery
    • Medicinal Chemistry

    Background:

    • Adenosine receptors (ARs) are crucial drug targets, with four subtypes: A(1), A(2A), A(2B), and A(3).
    • Caffeine and theophylline are common antagonists of adenosine receptors.
    • ARs play significant roles in various physiological processes, making them attractive therapeutic targets.

    Discussion:

    • Over a dozen AR agonists are undergoing clinical trials for conditions such as cardiac arrhythmias, neuropathic pain, myocardial perfusion imaging, cardiac ischemia, inflammatory diseases, and cancer.
    • Approved drugs like adenosine (nonselective), regadenoson (A(2A)), and dipyridamole (indirect AR action) highlight the clinical relevance of targeting ARs.
    • This editorial provides an update on the clinical trial status of AR agonists.

    Key Insights:

    • Adenosine receptor agonists show therapeutic potential across a wide spectrum of diseases.
    • The development pipeline for AR agonists is robust, with numerous candidates in clinical investigation.
    • Existing approved therapies demonstrate the feasibility and efficacy of modulating adenosine receptor pathways.

    Outlook:

    • Continued research and clinical trials are expected to yield new AR-targeting therapies.
    • Further understanding of AR subtype selectivity will refine therapeutic strategies.
    • AR agonists hold promise for addressing unmet medical needs in cardiovascular, neurological, inflammatory, and oncological conditions.