T3158
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Adrenergic Receptor
Monoamine Oxidase
Imidazoline Receptor
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Harmane (Loturine) 是一种在咖啡和烟草烟雾中发现的 β-咔啉生物碱,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。它还是选择性的单胺氧化酶抑制剂,具有致突变作用,对 MAO A/B 的 IC50值分别为 0.5 和 5 μM。 |
T21911
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Apoptosis
Imidazoline Receptor
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Rilmenidine hemifumarate (S-3341 hemifumarate) 是一种新型且具有口服活性和选择性 的 I1咪唑啉受体 (I1 imidazoline receptor) 和α2肾上腺素受体激动剂,可诱导自噬 ,调节白血病细胞增殖,刺激促凋亡蛋白 Bax,诱导人白血病 K562 细胞线粒体通路的紊乱和凋亡。 |
T6641
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Apoptosis
Adrenergic Receptor
Autophagy
Imidazoline Receptor
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Rilmenidine phosphate 是一种新型的抗高血压药物和口服活性选择性 I1 咪唑啉受体激动剂。它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。它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。 |
T22760
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Others
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α2 adrenoceptor antagonist and imidazoline I1 receptor ligand |
T27155
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Dexisometheptene is an antimigraine drug candidate. Dexisometheptene significantly increases the pain threshold of acute pain response, and potently and selectively binds to receptors in the central nervous system known as imidazoline type-1 (I1) receptor |
T40869
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Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.
Target: I1-R
Moxonidine Hydrochloride is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response curve of moxonidine (log EC50: -6.01 +/- 0.25). The hypotensive and bradycardic actions of moxonidine but not clonidine are mediated through imidazoline receptors and are dependent on intact noradrenergic pathways within the RVLM. Furthermore, the noradrenergic innervation may be associated with a 42 kDa imidazoline receptor protein. |