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



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]

Selective Ligands




See also


  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. doi:10.2174/187152506775268758. 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. doi:10.1111/j.1749-6632.1999.tb09339.x. PMID 10415895.  
  3. ^ [ I1 imidazoline receptors: From the pharmacological basis to the therapeutic application Journal für Hypertonie 2002; 6 (Sonderheft 4), 6-9]

External links


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