Imidazoline receptors

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Imidazoline receptors are receptors for clonidine and other imidazolines.[1]

Contents

Classes

There are three classes of imidazoline receptors:[1]

  • I1 receptor – mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure, (NISCH or IRAS, imidazoline receptor antisera selected)
  • I2 receptor – an allosteric binding site of monoamine oxidase
  • I3 receptor – regulates insulin secretion from pancreatic beta cells

Activated I1-imidazoline receptors trigger the hydrolysis of phosphatidylcholine into DAG. Elevated DAG levels in turn trigger the synthesis of second messengers arachidonic acid and downstream eicosanoids.[2] In addition, the sodium-hydrogen antiporter is inhibited, and enzymes of catecholamine synthesis is induced. The I1-imidazoline receptor may belong to the neurocytokine receptor family, since its signaling pathways are similar to those of interleukins.[2]

Pharmacology

Agonists of these receptors include the antihypertensive moxonidine, while antagonists include idazoxan.

See also

References

  1. ^ a b Head GA, Mayorov DN (January 2006). "Imidazoline receptors, novel agents and therapeutic potential". Cardiovasc Hematol Agents Med Chem 4 (1): 17–32. PMID 16529547. 
  2. ^ a b Ernsberger P (June 1999). "The I1-imidazoline receptor and its cellular signaling pathways". Ann. N. Y. Acad. Sci. 881: 35–53. PMID 10415895. 

External links

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Antihypertensives (C02) and diuretics (C03)
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Wikipedia content modification information:

  • This page was last modified on 15 August 2008, at 11:08.

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