1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Imidazoline Receptor

Imidazoline Receptor

Imidazoline receptors are the primary receptors on which clonidine and other imidazolines act. 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 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 downstreameicosanoids. In addition, the sodium-hydrogen antiporter is inhibited, and enzymes of catecholamine synthesis are induced. The I1-imidazoline receptor may belong to the neurocytokine receptorfamily, since its signaling pathways are similar to those of interleukins.

Imidazoline Receptor 相关产品 (10):

Cat. No. Product Name Effect Purity
  • HY-N0543
    Allantoin Agonist 99.85%
  • HY-101238
    Agmatine sulfate Agonist >98.0%
    Agmatine sulfate在多个靶点上发挥调节作用,如神经递质系统,离子通道,一氧化氮合成。它是 imidazoline receptor 的内源性激动剂和 NO synthase 抑制剂。
  • HY-100490A
    Rilmenidine hemifumarate Inhibitor >98.0%
    Rilmenidine hemifumarate 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体 (I1 imidazoline receptor) 激动剂。Rilmenidine hemifumarate 也是一种 α2 肾上腺素受体激动剂。Rilmenidine phosphate 诱导自噬 (autophagy)。Rilmenidine hemifumarate 可通过减少交感神经过度活跃而发挥中枢作用,并通过抑制 Na+/H+ 反向转运而在肾脏中发挥作用。Rilmenidine hemifumarate可调节白血病细胞增殖,刺激促凋亡蛋白 Bax,从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。
  • HY-100179
    CR4056 Agonist 98.32%
    CR4056 是一个选择性的人重组 MAO-A 抑制剂,其 IC50 值为 202.7 nM。 CR4056 也是咪唑啉-2 受体 (I2R) 的配体,其 IC50 值为 596 nM。
  • HY-B0374
    Moxonidine Agonist 99.91%
  • HY-100490B
    Rilmenidine phosphate Agonist >98.0%
    Rilmenidine phosphate 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体 (I1 imidazoline receptor) 激动剂。Rilmenidine phosphate 也是一种 α2 肾上腺素受体激动剂。Rilmenidine phosphate 诱导自噬 (autophagy)。Rilmenidine phosphate 可通过减少交感神经过度活跃而发挥中枢作用,并通过抑制 Na+/H+ 反向转运而在肾脏中发挥作用。Rilmenidine phosphate 可调节白血病细胞增殖,刺激促凋亡蛋白 Bax,从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。
  • HY-B1416A
    Efaroxan hydrochloride Antagonist
    Efaroxan hydrochloride 是一种有效的选择性性的 α2 肾上腺素受体 (α2-adrenoceptor) 拮抗剂,具有抗糖尿病的活性。Efaroxan hydrochloride 是一种选择性的 I1 咪唑啉受体 (I1-Imidazoline receptor) 的拮抗剂,可用于心血管疾病的研究。
  • HY-100490
    Rilmenidine Agonist
    Rilmenidine 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体 (I1 imidazoline receptor) 激动剂。Rilmenidine 是一种 α2 肾上腺素受体激动剂。Rilmenidine 诱导自噬 (autophagy)。Rilmenidine 可通过减少交感神经过度活跃而发挥中枢作用,并通过抑制 Na+/H+ 反向转运而在肾脏中发挥作用。Rilmenidine 可调节白血病细胞增殖,刺激促凋亡蛋白 Bax,从而诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。
  • HY-14561A
    Idazoxan hydrochloride Antagonist
    Idazoxan hydrochloride (RX 781094 hydrochloride) 是一种 α2-肾上腺素受体拮抗剂,也是咪唑啉受体 (IRs) 拮抗剂,可竞争性拮抗唑啉样药物 (IMs) 的中枢性降压作用。Idazoxan hydrochloride 还可改善帕金森氏病,L-DOPA 引起的运动障碍和实验性帕金森病的运动症状。
  • HY-B0374A
    Moxonidine hydrochloride Agonist
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