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Imidazoline Receptors(咪唑啉受体)

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.

  1. Cat.No. 产品名称 Information
  2. GC11588 2-BFI hydrochloride I2 ligand
  3. GC16831 Agmatine sulfate 硫酸胍丁胺对多个分子靶点发挥调节作用,例如神经递质系统、离子通道和一氧化氮合成。
  4. GC14934 AGN 192403 hydrochloride I1 imidazoline receptor
  5. GN10492 Allantoin 尿囊素是一种皮肤调理剂,可促进皮肤健康,刺激新的健康组织生长。
  6. GC15700 BU 224 hydrochloride BU 224 hydrochloride 是一种选择性和高亲和力的咪唑啉 I2 受体配体,Ki 为 2.1 nM。
  7. GC15202 BU 226 hydrochloride BU 226 hydrochloride 是一种选择性咪唑啉 2 (I2) 受体配体,对 I2 的 Ki 为 1.4 nM,对 I1 的 IC50 为 534.5 nM。
  8. GC11580 BU 239 hydrochloride Imidazoline receptors-selective antagonist
  9. GC31094 CR4056 CR4056是一个选择性的人重组MAO-A抑制剂,其IC50值为202.7nM。CR4056也是咪唑啉-2受体(I2R)的配体,其IC50值为596nM。
  10. GC15384 Harmane Harmane 是一种 β-咔啉生物碱 (BCA),是一种强效神经毒素,可导致严重的动作性震颤和精神症状。
  11. GC63754 Harmane-d1 Harmane-d1 是 Harmane 的氘代物。Harmane,一种 β-咔啉生物碱 (BCA),是有效的神经毒素,可引起严重的动作震颤和精神病学表现。Harmane 对 I1 咪唑啉受体 (I1-Imidazoline receptor, IC50=30 nM) 的选择性是对 α2-肾上腺素受体 (IC50=18 μM) 的 1000 倍。Harmane 还是有效和选择性的单胺氧化酶抑制剂 (对 MAO A/B 的 IC50 值分别为 0.5 μM 和 5 μM)。
  12. GC12629 Moxonidine Moxonidine(BDF5895) 是咪唑啉受体亚型 1 的选择性激动剂,用作抗高血压药。
  13. GC11198 Moxonidine hydrochloride Moxonidine Hydrochloride 是咪唑啉受体亚型 1 的选择性激动剂,用作抗高血压药。
  14. GC60325 Rilmenidine 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(I1imidazolinereceptor)激动剂。Rilmenidine是一种α2肾上腺素受体激动剂。Rilmenidine诱导自噬。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。
  15. GC13017 Rilmenidine Phosphate Rilmenidine phosphate 是一种创新的抗高血压药物,是一种具有口服活性的选择性 I1 咪唑啉受体激动剂。
  16. GC14958 RS 45041-190 hydrochloride Highly selective I2 imidazoline receptor ligand

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