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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(2)
货号 产品名 Cas 产品描述
PL01217 Harmane-d Harmane-d 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)。
PL05333 Moxonidine-d4 1794811-52-1 Moxonidine-d4 是 Moxonidine 的氘代物。Moxonidine(BDF5895)是咪唑啉1型受体(I1-R)选择性激动剂,为降压剂。