Alpha2-adrenergic receptors

Eduardo Listik; Qin Wang

doi:10.1016/B978-0-323-85492-4.00075-2

Alpha₂-adrenergic receptors

Eduardo Listik, Qin Wang

Research output: Chapter in Book/Report/Conference proceeding › Chapter

Abstract

alpha₂-adrenergic receptors (α₂-ARs) consist of three subtypes, α₂A-, α_2B-, and α_2C-AR, which are encoded by three highly homologous genes. These receptors bind to endogenous ligands, epinephrine and norepinephrine, and are blocked by the antagonist yohimbine. All three subtypes of α₂-ARs share the same signaling pathways through the Gi/o subfamily of heterotrimeric G proteins, but display distinct trafficking profiles. Both the α₂A- and α₂C- ARs are involved in suppression of catecholamine release from neuronal terminals. Studies using genetically manipulated mice reveal that central effects of α₂-adrenergic ligands, such as the hypotensive, sedative, and antiepileptic effects, are primarily mediated by the α_2A- subtype. Conversely, the vascular hypertensive effect of these drugs is achieved through the α_2B- subtype. Genetic variations of α₂-ARs have been linked with a number of disease states in human populations including hypertension and diabetes.

Original language	English (US)
Title of host publication	Primer on the Autonomic Nervous System, Fourth Edition
Publisher	Elsevier
Pages	49-52
Number of pages	4
ISBN (Electronic)	9780323854924
ISBN (Print)	9780323854931
DOIs	https://doi.org/10.1016/B978-0-323-85492-4.00075-2
State	Published - Jan 1 2022
Externally published	Yes

Keywords

Adrenergic receptors
Catecholamine release
Epinephrine
Hypotensive effect
Norepinephrine
Sedation
Transgenic mice

ASJC Scopus subject areas

General Medicine
General Neuroscience

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/B978-0-323-85492-4.00075-2

Cite this

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title = "Alpha2-adrenergic receptors",

abstract = "alpha2-adrenergic receptors (α2-ARs) consist of three subtypes, α2A-, α2B-, and α2C-AR, which are encoded by three highly homologous genes. These receptors bind to endogenous ligands, epinephrine and norepinephrine, and are blocked by the antagonist yohimbine. All three subtypes of α2-ARs share the same signaling pathways through the Gi/o subfamily of heterotrimeric G proteins, but display distinct trafficking profiles. Both the α2A- and α2C- ARs are involved in suppression of catecholamine release from neuronal terminals. Studies using genetically manipulated mice reveal that central effects of α2-adrenergic ligands, such as the hypotensive, sedative, and antiepileptic effects, are primarily mediated by the α2A- subtype. Conversely, the vascular hypertensive effect of these drugs is achieved through the α2B- subtype. Genetic variations of α2-ARs have been linked with a number of disease states in human populations including hypertension and diabetes.",

keywords = "Adrenergic receptors, Catecholamine release, Epinephrine, Hypotensive effect, Norepinephrine, Sedation, Transgenic mice",

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N2 - alpha2-adrenergic receptors (α2-ARs) consist of three subtypes, α2A-, α2B-, and α2C-AR, which are encoded by three highly homologous genes. These receptors bind to endogenous ligands, epinephrine and norepinephrine, and are blocked by the antagonist yohimbine. All three subtypes of α2-ARs share the same signaling pathways through the Gi/o subfamily of heterotrimeric G proteins, but display distinct trafficking profiles. Both the α2A- and α2C- ARs are involved in suppression of catecholamine release from neuronal terminals. Studies using genetically manipulated mice reveal that central effects of α2-adrenergic ligands, such as the hypotensive, sedative, and antiepileptic effects, are primarily mediated by the α2A- subtype. Conversely, the vascular hypertensive effect of these drugs is achieved through the α2B- subtype. Genetic variations of α2-ARs have been linked with a number of disease states in human populations including hypertension and diabetes.

AB - alpha2-adrenergic receptors (α2-ARs) consist of three subtypes, α2A-, α2B-, and α2C-AR, which are encoded by three highly homologous genes. These receptors bind to endogenous ligands, epinephrine and norepinephrine, and are blocked by the antagonist yohimbine. All three subtypes of α2-ARs share the same signaling pathways through the Gi/o subfamily of heterotrimeric G proteins, but display distinct trafficking profiles. Both the α2A- and α2C- ARs are involved in suppression of catecholamine release from neuronal terminals. Studies using genetically manipulated mice reveal that central effects of α2-adrenergic ligands, such as the hypotensive, sedative, and antiepileptic effects, are primarily mediated by the α2A- subtype. Conversely, the vascular hypertensive effect of these drugs is achieved through the α2B- subtype. Genetic variations of α2-ARs have been linked with a number of disease states in human populations including hypertension and diabetes.

KW - Adrenergic receptors

KW - Catecholamine release

KW - Epinephrine

KW - Hypotensive effect

KW - Norepinephrine

KW - Sedation

KW - Transgenic mice

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