Imidazoline receptor

Imidazoline receptors are proteins and receptors in the brain .

properties

Imidazoline receptors bind clonidine and other imidazoline derivatives (such as tolazoline , guanfacine , moxonidine , rilmenidine, and tolonidine ) as agonists . There are three classes of imidazoline receptors: I ₁ , I ₂ , I ₃ . Agmatine has been found to be an endogenous agonist , which not only binds to I ₁ and I ₂ receptors but also to α ₂ adrenoceptors. Competitive inhibitors of clonidine are agmatine, harmane and imidazole acetic acid . Guanfacine and tetrahydrozoline bind to imidazoline receptors.

I ₁ receptor

The I ₁ receptor mediated sympatholytic effects, together with α ₂ -adrenoceptors the blood pressure regulate. In humans Nischarin the suspected I ₁ receptor.

I ₂ receptor

The I ₂ receptor is an important allosteric binding site for the monoamine oxidases A and B. The receptors are involved in the regulation of pain . There are at least four proteins involved. They bind [3H] - idazoxan , [3H] - 2-BFI , CR4056 and [18F] - FEBU with high affinity .

I ₃ receptor

The I ₃ receptor regulates insulin - secretion from the beta cells of the pancreas and above the homeostasis of glucose .

literature

Entry on imidazoline receptor. In: Römpp Online . Georg Thieme Verlag, accessed on June 13, 2014.
Geoffrey A. Head, Dmitri N. Mayorov: Imidazoline receptors, novel agents and therapeutic potential . In: Cardiovascular and Hematological Agents in Medicinal Chemistry , 4 (1) (2006), pp. 17-32. PMID 16529547 .
WHO: ATC / DDD Index: Imidazoline receptor agonists

Individual evidence

↑ ^a ^b ^c ^d ^e J. A. Lowry, JT Brown: Significance of the imidazoline receptors in toxicology. In: Clinical toxicology. Volume 52, number 5, June 2014, pp. 454-469, doi : 10.3109 / 15563650.2014.898770 , PMID 24666288 .
↑ ^a ^b ^c ^d J. X. Li: Imidazoline I2 receptors: An update. In: Pharmacology & therapeutics. Volume 178, October 2017, pp. 48–56, doi : 10.1016 / j.pharmthera.2017.03.009 , PMID 28322973 , PMC 5600648 (free full text).
^ Y. Qiu, XH He, Y. Zhang, JX Li: Discriminative stimulus effects of the novel imidazoline I₂ receptor ligand CR4056 in rats. In: Scientific reports. Volume 4, October 2014, p. 6605, doi : 10.1038 / srep06605 , PMID 25308382 , PMC 4194429 (free full text).
↑ Kazunori Kawamura, Yoko Shimoda, Katsushi Kumata, Masayuki Fujinaga, Joji Yui, Tomoteru Yamasaki, Lin Xie, Akiko Hatori, Hidekatsu Wakizaka, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Ming-Rong Zhang: In-vivo evaluation of a new labeled PET ligand, [18F] FEBU, for the imaging of I2-imidazoline receptors. In: Nuclear Medicine and Biology. 42, 2015, p. 406, doi : 10.1016 / j.nucmedbio.2014.12.014 .

[Lowry-1] J. A. Lowry, JT Brown: Significance of the imidazoline receptors in toxicology. In: Clinical toxicology. Volume 52, number 5, June 2014, pp. 454-469, doi : 10.3109 / 15563650.2014.898770 , PMID 24666288 .

[Li-2] J. X. Li: Imidazoline I2 receptors: An update. In: Pharmacology & therapeutics. Volume 178, October 2017, pp. 48–56, doi : 10.1016 / j.pharmthera.2017.03.009 , PMID 28322973 , PMC 5600648 (free full text).

[3] Y. Qiu, XH He, Y. Zhang, JX Li: Discriminative stimulus effects of the novel imidazoline I₂ receptor ligand CR4056 in rats. In: Scientific reports. Volume 4, October 2014, p. 6605, doi : 10.1038 / srep06605 , PMID 25308382 , PMC 4194429 (free full text).

[DOI10.1016/j.nucmedbio.2014.12.014-4] Kazunori Kawamura, Yoko Shimoda, Katsushi Kumata, Masayuki Fujinaga, Joji Yui, Tomoteru Yamasaki, Lin Xie, Akiko Hatori, Hidekatsu Wakizaka, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Ming-Rong Zhang: In-vivo evaluation of a new labeled PET ligand, [18F] FEBU, for the imaging of I2-imidazoline receptors. In: Nuclear Medicine and Biology. 42, 2015, p. 406, doi : 10.1016 / j.nucmedbio.2014.12.014 .