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Related Concept Videos

Antiasthma Drugs: β2-Adrenoceptor Agonists01:25

Antiasthma Drugs: β2-Adrenoceptor Agonists

Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce relaxation in these...
Adrenergic Receptors: β Subtype01:26

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...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

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 (Adrenoceptors): Classification01:27

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...
Antihypertensive Drugs: Types of β-Blockers01:28

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 Blockers01:31

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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β2-Adrenoreceptor Polymorphisms in Asthmatic Patients.

Saeed Binaei1, Sahar M Rashed, Michael L Christensen

  • 1Department of Pharmacy, The University of Tennessee Health Science Center, and LeBonheur Children's Medical Center, Memphis, Tennessee.

The Journal of Pediatric Pharmacology and Therapeutics : JPPT : the Official Journal of PPAG
|January 10, 2013
PubMed
Summary

Genetic variations in beta2-adrenergic receptors (β2AR) influence asthma patient responses to common inhaled medications. Understanding these beta2-adrenergic receptor polymorphisms can personalize asthma treatment strategies.

Keywords:
asthmapolymorphismsβ2-Adrenoreceptorβ2-agonist

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Area of Science:

  • Pharmacogenetics
  • Molecular Biology
  • Respiratory Medicine

Background:

  • Beta2-adrenergic receptors (β2AR) are key targets for inhaled bronchodilators used in asthma.
  • Genetic variations (polymorphisms) in the β2AR gene may alter drug responsiveness and asthma phenotypes.

Purpose of the Study:

  • To review the impact of β2AR gene polymorphisms on asthma pathophysiology and therapeutic responses.
  • To explore the association between specific β2AR genetic variants and clinical outcomes in asthma patients.

Main Methods:

  • Analysis of single nucleotide polymorphisms (SNPs) in coding and 5' upstream regions of the β2AR gene.
  • Investigation of common variants like Arg16Gly and Gln27Glu, and 5' leader cistron (5'LC) polymorphisms.
  • Examination of haplotype combinations and their functional implications.

Main Results:

  • Certain β2AR polymorphisms (Gly16, Gln27) are linked to receptor down-regulation.
  • Homozygosity for Arg16 and/or Glu 27 may increase susceptibility to tachyphylaxis.
  • No direct relation between β2AR polymorphism and asthma severity, but Gly16 is more frequent in nocturnal asthma.
  • The Cys19 polymorphism in 5'LC is associated with higher β2AR expression.

Conclusions:

  • β2AR gene polymorphisms significantly influence asthma pathophysiology and patient response to β2-agonist therapy.
  • Haplotypes of multiple SNPs may dictate β2AR function and lead to diverse asthma phenotypes.
  • Understanding β2AR genetic variations is crucial for personalized asthma management.