イミダゾリン受容体、イミダゾリンレセプター
WordNet
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/10/06 23:53:38」(JST)
[Wiki en表示]
Imidazoline receptors are receptors for clonidine and other imidazolines.[1]
Contents
- 1 Classes
- 2 Selective Ligands
- 2.1 Agonists
- 2.2 Antagonists
- 3 See also
- 4 References
- 5 External links
Classes[edit]
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 and is involved in pain modulation and neuroprotection.
- 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 are induced. The I1-imidazoline receptor may belong to the neurocytokine receptor family, since its signaling pathways are similar to those of interleukins.[2]
imidazoline receptors are receptors for clonidine and other imidazolines.[1]
Selective Ligands[edit]
Agonists[edit]
- Agmatine (endogenous agonist, non-selective, also binds to NMDA, nicotinic, and 2 adrenoceptors)
- Apraclonidine (I1 selective)
- Moxonidine
- Rilmenidine
- Clonidine usually cited as an alpha2 agonist, its structure corroborates recent lab data showing it may be a Imidazole receptor (I1) agonist.[3]
- S-23515
- S-23757
- LNP-509
- 2-BFI (selective I2 receptor agonist)
- BU224 (selective I2 receptor agonist, low efficacy)
- LNP-911[4]
Antagonists[edit]
- Efaroxan (non-selective, binds to I1 receptor and α2 adrenoceptor)
- Idazoxan (non-selective, binds to I2 receptor and α2 adrenoceptor)
- BU99006 (alkylating agent, inactivates I2 receptors)
Imidazoline I2 receptor antagonists reversibly block NMDA receptor-mediated Ca2+ influx[5] and thus may inhibit excitotoxicity.
See also[edit]
References[edit]
- ^ a b c 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.
- ^ a b Ernsberger P (June 1999). "The I1-imidazoline receptor and its cellular signaling pathways". Ann. N. Y. Acad. Sci. 881 (1): 35–53. doi:10.1111/j.1749-6632.1999.tb09339.x. PMID 10415895.
- ^ Reis DJ, Piletz JE (November 1997). "The imidazoline receptor in control of blood pressure by clonidine and allied drugs" (pdf). Am. J. Physiol. 273 (5 Pt 2): R1569–71. PMID 9374795.
- ^ Bousquet P (2002). "I1 imidazoline receptors: From the pharmacological basis to the therapeutic application" (pdf). Journal für Hypertonie 6 (4): 6–9.
- ^ Jiang SX, Zheng RY, Zeng JQ, Li XL, Han Z, Hou ST (March 2010). "Reversible inhibition of intracellular calcium influx through NMDA receptors by imidazoline I(2) receptor antagonists". Eur. J. Pharmacol. 629 (1–3): 12–9. doi:10.1016/j.ejphar.2009.11.063. PMID 19958763.
External links[edit]
- Imidazoline Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
- imidazoline receptor 2 at the US National Library of Medicine Medical Subject Headings (MeSH)
- imidazoline I1 receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
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Sympatholytic (and closely related) antihypertensives (C02)
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Sympatholytics
(antagonize α-adrenergic
vasoconstriction) |
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Central
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α2 agonist
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- Clonidine
- Guanfacine
- Methyldopa #
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Adrenergic release inhibitors
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- Bethanidine
- Bretylium
- Debrisoquine
- Guanadrel
- Guanazodine
- Guanethidine
- Guanoclor
- Guanoxan
- Guanazodine
- Guanoxabenz
- Guanoxan
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Imidazoline receptor agonist
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Ganglion-blocking/nicotinic antagonist
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- Mecamylamine
- Pentolinium
- Trimethaphan
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Peripheral
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Indirect
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MAOI
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Adrenergic uptake inhibitor
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- Bietaserpine
- Deserpidine
- Methoserpidine
- Rescinnamine
- Reserpine
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Tyrosine hydroxylase inhibitor
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Direct
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α1 blockers
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- Prazosin
- Indoramin
- Trimazosin
- Doxazosin
- Urapidil
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Non-selective α blocker
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| Other antagonists |
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Serotonin antagonist
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Endothelin antagonist (for PH)
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- dual (Bosentan)
- selective (Ambrisentan, Sitaxentan)
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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anat (a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot
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noco/syva/cong/lyvd/tumr, sysi/epon, injr
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proc, drug (C2s+n/3/4/5/7/8/9)
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UpToDate Contents
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English Journal
- Dexmedetomidine protects against oxygen-glucose deprivation-induced injury through the I2 imidazoline receptor-PI3K/AKT pathway in rat C6 glioma cells.
- Zhang F, Ding T, Yu L, Zhong Y, Dai H, Yan M.SourceSecond Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China.
- The Journal of pharmacy and pharmacology.J Pharm Pharmacol.2012 Jan;64(1):120-7. doi: 10.1111/j.2042-7158.2011.01382.x. Epub 2011 Nov 24.
- Objectives To explore the protection and the mechanism of dexmedetomidine on the oxygen-glucose deprivation (OGD) insults in rat C6 glioma cells. Methods Cells were subjected to OGD then assessed by viability studies. After dexmedetomidine treatment, p-AKT, hypoxia-inducible factor (HIF)-1α,
- PMID 22150679
- Agmatinase, an inactivator of the putative endogenous antidepressant agmatine, is strongly upregulated in hippocampal interneurons of subjects with mood disorders.
- Bernstein HG, Stich C, Jäger K, Dobrowolny H, Wick M, Steiner J, Veh R, Bogerts B, Laube G.SourceDepartment of Psychiatry, University of Magdeburg, Leipziger Str. 44, D-39120 Magdeburg, Germany. hans-gert.bernstein@med.ovgu.de
- Neuropharmacology.Neuropharmacology.2012 Jan;62(1):237-46. Epub 2011 Jul 22.
- The diamine agmatine may serve as a precursor in polyamine synthesis. In addition, agmatine may also act as a neurotransmitter, binding to imidazoline receptors. Behaviorally, agmatine exerts antidepressant-like effects. The enzyme agmatinase degrades agmatine. The gene coding for human agmatinase i
- PMID 21803059
Japanese Journal
- Effect of moxonidine and amlodipine on serum YKL-40, plasma lipids and insulin sensitivity in insulin-resistant hypertensive patients-a randomized, crossover trial
- MASAJTIS-ZAGAJEWSKA Anna,MAJER Jacek,NOWICKI Michal
- Hypertension research : clinical and experimental : official journal of the Japanese Society of Hypertension 33(4), 348-353, 2010-04-01
- NAID 10026127764
- Involvement of Supraspinal Imidazoline Receptors and Descending Monoaminergic Pathways in Tizanidine-Induced Inhibition of Rat Spinal Reflexes
- Kino Yurika,Tanabe Mitsuo,Honda Motoko [他],ONO Hideki
- Journal of pharmacological sciences 99(1), 52-60, 2005-09-20
- … Supraspinal receptors were then studied using yohimbine- and some imidazoline-receptor ligands containing an imidazoline moiety. … Idazoxan (I1, I2, I3, and α2), efaroxan (I1, I3, and α2), and RX821002 (I3 and α2), but not yohimbine, an α2-adrenergic receptor antagonist with no affinity for I receptors, antagonized the inhibitory effects of tizanidine. …
- NAID 10025730341
Related Links
- forum Join the Word of the Day Mailing List For webmasters TheFreeDictionary Google Bing? Word / Article Starts with Ends with Text ... imidazoline receptor binding site for clonidine and other antihypertensive agents.
- a newly-discovered family of receptors ... Immunodetection and quantitation of imidazoline receptor proteins in platelets of patients with major depression and in brains of suicide victims
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- imidazoline receptor
- 関
- イミダゾリンレセプター
[★]
- 英
- imidazoline receptor
- 関
- イミダゾリン受容体
[★]
イミダゾリン
- C原子3つとN原子2つに二重結合1つをもつ五員環化合物