Imidazoline receptor

Imidazoline receptors are receptors for clonidine and other imidazolines.cite journal | author = Head GA, Mayorov DN | title = Imidazoline receptors, novel agents and therapeutic potential | journal = Cardiovasc Hematol Agents Med Chem | volume = 4 | issue = 1 | pages = 17–32 | year = 2006 | month = January | pmid = 16529547 | url = http://www.bentham-direct.org/pages/content.php?CHAMC/2006/00000004/00000001/003AE.SGM | issn = ]

Classes

There are three classes of imidazoline receptors:
* 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.cite journal | author = Ernsberger P | title = The I1-imidazoline receptor and its cellular signaling pathways | journal = Ann. N. Y. Acad. Sci. | volume = 881 | issue = | pages = 35–53 | year = 1999 | month = June | pmid = 10415895 | url = http://www.annalsnyas.org/cgi/content/abstract/881/1/35 | issn = ] 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.

Pharmacology

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

ee also

* imidazoline
* NISCH

References

External links

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