| 別包装 |
あり
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| 純度 |
>=98%
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| 分子量 |
266.55
|
| CAS RN® |
4205-91-8
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| 化合物の概要 |
Imidazoline and α2-adrenergic agonist, Nav1.7 Na+ channel blocker.
|
| 構造 |
C9H9Cl2N3 HCl
|
| 使用目的 |
Clonidine is an α2-adrenergic receptor agonist that also activate the imidazoline 1 receptor, increasing downstream catecholamine synthesis. Clonidine exhibits antihypertensive, neuromoduatory, cognition enhancing, antinociceptive, analgesic, and antipsychotic activities. In hypertensive rats, clonidine increases baroreceptor sensitivity and decreases blood pressure and heart rate. In other animal models, clonidine inhibits long term potentiation (synaptic plasticity) and decreases excitatory postsynaptic potentials (EPSPs) in the medial prefrontal cortex (mPFC), a potential mechanism behind clonidine’s ability to decrease glutamate release. Clonidine also improves spatial memory impairments in vivo. This compound is occasionally used clinically for its antipsychotic benefits and is most often used to treat attention deficit hyperactive disorder (ADHD) as a result of its actions that stem from binding postsynaptic α2-adrenergic receptors. In vitro, clonidine inhibits Nav1.7 Na+ channels. In vivo, clonidine decreases mechanical and thermal pain in a model of chronic constriction injury-induced neuropathy, likely due to its ability to downregulate expression of phosphorylated NMDA receptor subunit 1 (pNR1). Clonidine also displays some sedative activity and induces downstream activation of histamine H2 receptors.
|
| その他 |
[融点]130 C
|
| 参考文献 |
Li CJ, Zhou M, Li HG, et al. Clonidine suppresses the induction of long-term potentiation by inhibiting HCN channels at the schaffer collateral-CA1 synapse in anesthetized adult rats. Cell Mol Neurobiol. 2013 Nov;33(8):1075-86. PMID: 23975095.Maruta T, Nemoto T, Satoh S, et al. Dexmedetomidine and clonidine inhibit the function of Na(v)1.7 independent of α(2)-adrenoceptor in adrenal chromaffin cells. J Anesth. 2011 Aug;25(4):549-57. PMID: 21607767.Roh DH, Kim HW, Yoon SY, et al. Intrathecal clonidine suppresses phosphorylation of the N-methyl-D-aspartate receptor NR1 subunit in spinal dorsal horn neurons of rats with neuropathic pain. Anesth Analg. 2008 Aug;107(2):693-700. PMID: 18633054.Ji XH, Ji JZ, Zhang H, et al. Stimulation of alpha2-adrenoceptors suppresses excitatory synaptic transmission in the medial prefrontal cortex of rat. Neuropsychopharmacology. 2008 Aug;33(9):2263-71. PMID: 17957212.Bardgett ME, Points M, Ramsey-Faulkner C, et al. The effects of clonidine on discrete-trial delayed spatial alternation in two rat models of memory loss. Neuropsychopharmacology. 2008 Jul;33(8):1980-91. PMID: 17882233.Ma XJ, Shen FM, Liu AJ, et al. Clonidine, moxonidine, folic acid, and mecobalamin improve baroreflex function in stroke-prone, spontaneously hypertensive rats. Acta Pharmacol Sin. 2007 Oct;28(10):1550-8. PMID: 17883939.Li CG, Rand MJ. Rilmenidine differs from clonidine in that it lacks histamine-like activity. J Pharm Pharmacol. 1989 Jul;41(7):464-8. PMID: 2570851.Ernsberger P, Giuliano R, Willette RN, et al. Hypotensive action of clonidine analogues correlates with binding affinity at imidazole and not alpha-2-adrenergic receptors in the rostral ventrolateral medulla. J Hypertens Suppl. 1988 Dec;6(4):S554-7. PMID: 2853758.
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| メーカー |
品番 |
包装 |
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LKT
|
C4558
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250 MG
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※表示価格について
| 当社在庫 |
なし
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| 納期目安 |
1週間程度
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| 保存温度 |
常温
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