Mechanisms involved in α1B-adrenoceptor desensitization

IUBMB Life. 2011 Oct;63(10):811-5. doi: 10.1002/iub.519. Epub 2011 Aug 3.


α(1B)-Adrenergic receptors mediate many of the actions of the natural catecholamines, adrenaline and noradrenaline. They belong to the seven transmembrane domains G protein-coupled receptor superfamily and exert their actions mainly through activation of Gq proteins and phosphoinositide turnover/calcium signaling. Many hormones and neurotransmitters are capable of inducing α(1B)-adrenergic receptor phosphorylation and desensitization; among them: adrenaline and noradrenaline, phorbol esters, endothelin-I, bradykinin, lysophosphatidic acid, insulin, EGF, PDGF, IGF-I, TGF-β, and estrogens. Key protein kinases for these effects are G protein coupled receptor kinases and protein kinase C. The lipid/protein kinase, phosphoinositide-3 kinase also appears to play a key role, acting upstream of protein kinase C. In addition to the agents employed for cells stimulation, we observed that paracrine/autocrine mediators also participate; these processes include EGF transactivation and sphingosine-1-phosphate production and action. The complex regulation of these receptors unlocks opportunities for therapeutic intervention.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Epidermal Growth Factor / metabolism
  • G-Protein-Coupled Receptor Kinases / metabolism
  • Hormones / metabolism*
  • Lysophospholipids / metabolism
  • Models, Biological*
  • Neurotransmitter Agents / metabolism*
  • Paracrine Communication / physiology*
  • Phosphorylation
  • Protein Kinase C / metabolism
  • Receptors, Adrenergic, alpha-1 / physiology*
  • Sphingosine / analogs & derivatives
  • Sphingosine / metabolism
  • Transcriptional Activation / physiology*


  • Hormones
  • Lysophospholipids
  • Neurotransmitter Agents
  • Receptors, Adrenergic, alpha-1
  • sphingosine 1-phosphate
  • Epidermal Growth Factor
  • Protein Kinase C
  • G-Protein-Coupled Receptor Kinases
  • Sphingosine