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Adrenergic Agonists: Direct-Acting Agents

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...

Antihypertensive Drugs: Angiotensin II Receptor Blockers

Antihypertensive Drugs: Angiotensin II Receptor Blockers

In the renin-angiotensin-aldosterone system, a hormone called angiotensin II plays a crucial role. It binds to the AT1 receptors in vascular smooth muscles coupled with Gq proteins. The activation of these receptors activates an enzyme called phospholipase C, which releases two molecules: inositol trisphosphate and diacylglycerol. These molecules cause a chain reaction that leads to the phosphorylation of myosin light chains and promotes interaction between actin and myosin, leading to smooth...

Adrenergic Agonists: Therapeutic Uses

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: Therapeutic Classification

Adrenergic Agonists: Therapeutic Classification

Adrenergic agonists can be classified based on their therapeutic uses and mechanisms of action. They serve various purposes in clinical applications.
Vasopressor or pressor agents: They increase blood pressure and function as cardiac stimulants. Examples include endogenous catecholamines (norepinephrine and dopamine) and synthetic agents (phenylephrine).
Bronchodilators: β2-agonists can relax bronchial muscles and widen airways. They are commonly used for treating obstructive pulmonary...

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

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 Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

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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Updated: Jun 5, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Published on: June 7, 2016

Non-peptide AT2-receptor agonists.

U Muscha Steckelings¹, Mats Larhed, Anders Hallberg

¹Center for Cardiovascular Research, Charité-Universitätsmedizin Berlin, Hessische Str. 3-4, 10115 Berlin, Germany. ulrike.steckelings@charite.de

Current Opinion in Pharmacology

|December 21, 2010

Summary

This summary is machine-generated.

A novel AT2-receptor agonist, compound 21 (C21), demonstrates significant tissue protection and functional improvement in cardiovascular disease models. This orally active drug targets anti-inflammatory mechanisms, with clinical trials anticipated.

Related Experiment Videos

Last Updated: Jun 5, 2026

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Published on: June 7, 2016

Area of Science:

Cardiovascular Pharmacology
Renal Physiology
Drug Discovery

Background:

The renin-angiotensin system (RAS) includes AT1 and AT2 receptors for angiotensin II.
AT1 receptor antagonists are established cardiovascular drugs.
AT2 receptor's therapeutic potential was largely unexplored until recently.

Purpose of the Study:

To introduce compound 21 (C21), the first non-peptide, orally active AT2 receptor agonist.
To evaluate the therapeutic effects of C21 in preclinical models of cardiovascular disease.

Main Methods:

Administration of C21 in models of myocardial infarction and hypertension-induced end-organ damage.
Assessment of tissue protection and functional recovery.
Investigation of underlying anti-inflammatory mechanisms.

Main Results:

C21 showed significant tissue protective effects and functional improvement post-myocardial infarction.
C21 demonstrated benefits in hypertension models, independent of blood pressure reduction.
AT2 receptor-mediated anti-inflammation was identified as a key mechanism.

Conclusions:

Compound 21 represents a promising new therapeutic agent targeting the AT2 receptor.
C21 exhibits potent anti-inflammatory and tissue-protective properties.
Further clinical investigation of C21 is warranted.