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.
Products for Imidazoline Receptors
- Cat.No. 产品名称 Information
- GC11588 2-BFI hydrochloride I2配体
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GC16831
Agmatine sulfate
胍基丁胺;硫酸胍基丁胺;硫酸鲱精胺;胍基丁胺硫酸盐
A polyamine metabolite - GC14934 AGN 192403 hydrochloride I1 imidazoline receptor
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GN10492
Allantoin
尿囊素; 5-Ureidohydantoin
A product of purine and uric acid metabolism - 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。
- 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。
- GC11580 BU 239 hydrochloride Imidazoline receptors-selective antagonist
- 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。
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GC15384
Harmane
哈尔满碱
A β-carboline with diverse biological activities -
GC69206
Harmane-d
哈尔满碱 d1
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)。 -
GC63754
Harmane-d1
哈尔满碱 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)。 -
GC12629
Moxonidine
莫索尼定; BDF5895
An imidazoline I1 and α2A-adrenergic receptor agonist -
GC11198
Moxonidine hydrochloride
盐酸莫索尼定; BDF5895 hydrochloride
An imidazoline I1 and α2A-adrenergic receptor agonist -
GC60325
Rilmenidine
利美尼啶
An antihypertensive agent -
GC13017
Rilmenidine Phosphate
磷酸利美尼定
An antihypertensive agent - GC14958 RS 45041-190 hydrochloride Highly selective I2 imidazoline receptor ligand