Subtypes of α1‐ and α2‐adrenergic receptors

@article{Bylund1992SubtypesO,
  title={Subtypes of $\alpha$1‐ and $\alpha$2‐adrenergic receptors},
  author={David B. Bylund},
  journal={The FASEB Journal},
  year={1992},
  volume={6},
  pages={832 - 839}
}
  • D. Bylund
  • Published 1 February 1992
  • Chemistry
  • The FASEB Journal
The adrenergic receptors are members of the superfamily of G protein‐coupled receptors. There are three major types of adrenergic receptors: α1, α2, and β. Each of these three major types can be divided into three subtypes. Within the α1‐adrenergic receptors, α1A and the subtypes have been defined pharmacologically on the basis of reversible antagonists, such as WB4101 and phentolamine, and the irreversible antagonist chloroethylclonidine. In at least some tissues the mechanism of action of the… Expand
Subtypes of alpha-1 and alpha-2 adrenergic receptors
  • D. Bylund
  • Medicine, Chemistry
  • European Neuropsychopharmacology
  • 1992
TLDR
The adrenergic receptors are members of the superfamily of G protein-coupled receptors and three pharmacological subtypes of the alpha 2-adrenergic receptor have been identified by molecular cloning in both the human and rat species. Expand
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Subtypes of functional α1- and α2-adrenoceptors, belonging to the seven transmembrane spanning G-protein-linked family of receptors, which respond to the physiological agonists noradrenaline and adrenaline are discussed. Expand
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Although no additional α-adrenoceptor subtypes have been cloned in the past several years, there is functional evidence to suggest that additional subtypes of both α1- and α2- adrenoceptors remain to be cloned. Expand
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  • A. Strosberg
  • Chemistry, Medicine
  • Protein science : a publication of the Protein Society
  • 1993
TLDR
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TLDR
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Pharmacological properties of the cloned α1A/D‐adrenoceptor subtype are consistent with the α1A‐adrenoceptor characterized in rat cerebral cortex and vas deferens
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Localization and trafficking of alpha2-adrenergic receptor subtypes in cells and tissues.
TLDR
The focus of this review is to compare the similarities and differences among the three alpha2AR subtypes in terms of specificity, signaling, and trafficking, and it is anticipated that a molecular understanding of receptor trafficking will lead to novel therapeutic strategies for diseases linked to aberrant adrenergic receptor function or localization. Expand
Pharmacological Characteristics of Alpha‐2 Adrenergic Receptor Subtypes
  • D. Bylund
  • Biology, Medicine
  • Annals of the New York Academy of Sciences
  • 1995
TLDR
The adrenergic receptor family has three main members: alpha-1, alpha-2, and beta receptor types, which contain three or more subtypes and little is currently known about the specific function mediated by the various subtypes. Expand
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TLDR
Functional data are consistent with the previous and more extensive binding data, and thus support the existence and definition ofalpha-2A and alpha-2B adrenergic receptor subtypes. Expand
The rat α2‐C4 adrenergic receptor gene encodes a novel pharmacological subtype
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RNA blots indicate that this gene is expressed in brain, heart and kidney but not in lung, liver or pancreas, and data suggest that the α2‐C4 gene product defines a previously undescribed pharmacological subtype α 2‐adrenergic receptor. Expand
Heterogeneity of alpha-2 adrenergic receptors
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  • Medicine, Chemistry
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TLDR
The ability to pharmacologically define putative alpha-2 adrenergic receptor subtypes should promote the development of additional subtype selective drugs which will increase the understanding of adrenergic pharmacology and may provide new therapeutic approaches. Expand
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It is concluded that the OK cell line and opossum kidney express a novel subtype of alpha-2 adrenergic receptor which is referred to as thealpha-2C subtype. Expand
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Two distinct pharmacological profiles for the two alpha-2 adrenergic receptor subtypes in several different tissues are demonstrated, further support the existence and definition of these subtypes. Expand
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TLDR
Data suggest that RG20 represents a fourth alpha 2-AR subtype distinct from the known alpha 2A-C receptor subtypes, which is also capable of mediating adenylylcyclase inhibition as determined following its stable expression in NIH-3T3 fibroblasts. Expand
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TLDR
Computer-assisted analysis of curvilinear Schild plots in a two-receptor system indicated that alpha 1-adrenoceptor populations responsible for the constrictive response are predominantly (approximately 80-90%) low affinity sites for the two antagonists and a small population (approximately 10-20%) are high affinity sites. Expand
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