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Adrenergic Receptors: β Subtype

Adrenergic Receptors: β Subtype

β-adrenoceptors have varied sensitivities towards adrenaline, noradrenaline, and isoprenaline. The order of agonist potency is as follows:
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors have equal affinities for...

Adrenergic Receptors (Adrenoceptors): Classification

Adrenergic Receptors (Adrenoceptors): Classification

Adrenergic receptors, or adrenoceptors, respond to the autonomic neurotransmitter noradrenaline and other endogenous catecholamine agonists. They are classified into two main families, α and β, based on their pharmacological response and are further subdivided depending on their location, elicited response, and affinity to specific agonists or antagonists.
α-Adrenoceptors
α-Adrenoceptors are classified into two main subtypes: α1 and α2. The α1 adrenoceptors, which are found on postsynaptic...

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...

Adrenergic Receptors: ɑ Subtype

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...

Antihypertensive Drugs: Types of β-Blockers

Antihypertensive Drugs: Types of β-Blockers

β receptors are classified into three subclasses: β1, β2, and β3. β1 receptors are primarily located in the heart and kidneys. When they get activated, they increase heart rate, contractility, and renin release. This process enhances blood pressure and aids in stress management. In contrast, β2 receptors are situated mainly in the lungs, blood vessels, and skeletal muscles. Upon activation, they trigger smooth muscle relaxation, causing bronchodilation and vasodilation. This widens airways and...

Adrenergic Antagonists: ɑ and β-Receptor Blockers

Adrenergic Antagonists: ɑ and β-Receptor Blockers

Third-generation β-blockers, such as labetalol and carvedilol, represent a significant advancement in managing cardiovascular conditions. Unlike conventional β-blockers, which can induce peripheral vasoconstriction, third-generation drugs block α1 adrenoceptors. This promotes vasodilation through several mechanisms, such as increased nitric oxide production, inhibition of calcium ion entry, opening of potassium ion channels, and antioxidant action. Labetalol, for instance, is clinically...

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Updated: Jun 13, 2026

Measuring the Rate of Lipolysis in Ex Vivo Murine Adipose Tissue and Primary Preadipocytes Differentiated In Vitro

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Adrenergic-beta(2) receptor polymorphism and athletic performance.

Vishnu Sarpeshkar¹, David J Bentley

¹School of Health and Exercise Science, Faculty of Medicine, University of New South Wales, Sydney, Australia. v.sarpeshkar@unsw.edu.au

Journal of Human Genetics

|May 1, 2010

Summary

Genetic variations in the beta(2)-adrenergic receptor (ADRB2) influence physiological functions impacting athletic performance. However, ADRB2 gene polymorphism does not yet predict elite athlete potential.

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Measuring the Rate of Lipolysis in Ex Vivo Murine Adipose Tissue and Primary Preadipocytes Differentiated In Vitro

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Published on: March 17, 2023

Cardiac Response to β-Adrenergic Stimulation Determined by Pressure-Volume Loop Analysis

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Published on: May 19, 2021

Area of Science:

Exercise Physiology
Human Genetics
Pharmacogenomics

Background:

The beta(2)-adrenergic receptor (ADRB2) plays a crucial role in regulating physiological functions.
Genetic variations (polymorphisms) in ADRB2 may influence athletic capabilities.
Previous research suggests a link between athlete genetics and enhanced aerobic capacity.

Purpose of the Study:

To review the influence of beta(2)-adrenergic receptor (ADRB2) gene polymorphism on human physiological systems.
To evaluate the impact of ADRB2 polymorphism on athletic performance, particularly endurance.
To explore the potential of ADRB2 genotype for identifying elite athletes.

Main Methods:

A narrative review of existing literature.
Searches conducted in MedLine, Pubmed, and Cochrane Library databases.
Keywords included ADRB2, endurance, and polymorphism.

Main Results:

ADRB2 receptor location and function were documented.
The effects of genetic polymorphisms on cardiovascular, respiratory, metabolic, and musculoskeletal systems were examined.
The Gly16Glu27 haplotype is associated with positive aerobic phenotypes and lipolysis.
No definitive evidence supports ADRB2 genotype polymorphism for predicting elite athlete status.

Conclusions:

Understanding ADRB2 polymorphism aids in identifying altered phenotypes that may affect athletic performance.
The interplay between fatigue and athletic performance in genetically polymorphic individuals requires further investigation.
Current evidence is insufficient to use ADRB2 genotype polymorphism for elite athlete identification.