2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. ReN-1869 hydrochloride

ReN-1869 hydrochloride  (Synonyms: NNC-05-1869 hydrochloride)

目录号: HY-101724
产品使用指南

摩尔计算器

ReN 1869 hydrochloride 是一种新型的选择性组胺 H1 受体拮抗剂，高亲和力作用于组胺 H1 受体 (豚鼠脑) 和非选择性 σ 位点 (豚鼠脑)，Ki 值分别为 0.19±0.04 μM 和 0.45 μM。

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ReN-1869 hydrochloride Chemical Structure

ReN-1869 hydrochloride Chemical Structure

CAS No. : 170149-76-5

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Other Forms of ReN-1869 hydrochloride:

ReN-1869 hydrochloride 相关抗体

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.

IC50 & Target

Ki: 0.19±0.04 μM (histamine H1 receptor)[1]
体外研究
(In Vitro)

ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H1 receptor antagonism. Binding studies with radioactively labelled ReN 1869 reveals high affinity only for the histamine H1 receptor in addition to some affinity for a sigma site. ReN 1869 is profiled for activity at 10 μM at various receptors, transporters, enzymes and ion channels. ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain, [3H]pyrilamine) with a Ki of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [3H]1,3-di-tolylguanidine (DTG)] with a Ki of 0.45 μM. ReN 1869 dose-dependently reduces the responses with IC50 of 1.70±0.002 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ReN-1869 hydrochloride 相关抗体:
体内研究
(In Vivo)

The in vivo binding of [3H]Mepyramine to mouse spinal cord and cerebellar histamine H1 receptors is dose-dependently inhibited by ReN 1869. ReN 1869 (in doses as low as 10 μg/kg i.p.) significantly inhibits the histamine-evoked paw edema. The ED50 is approximately 300 μg/kg. Interestingly, even a high dose of Mepyramine (10 mg/kg) is unable to inhibit significantly this type of edema (0.29±0.06 versus 0.34±0.05 in controls, n=7).ReN 1869 (1 mg/kg s.c.) is administered 30 min before paw injection with carrageenan and has no effect on the development of the paw edema. Dexamethasone (1 mg/kg s.c.) is given 1 h before carrageenan and expectedly diminished the edema. This effect is not affected by the simultaneous administration of 1 mg/kg ReN 1869[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

397.94

Formula

C24H28ClNO2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Kinase Assay
[1]

ReN 1869 is labelled with 3H in the tricyclic ring system resulting in a specific activity of 40 Ci/mmol. Thawed membranes (1 mg protein/tube), test compounds and [3H]ReN 1869 are added to test tubes in a final volume of 0.5 mL. Unless otherwise indicated, the concentration of the radioligand is 5 nM and non-specific binding is defined as the binding in the presence of 10 μM ReN 1869. Samples are incubated for 120 min at 37 °C in a shaking water bath. Free and bound radioactivity is separated by filtration over Whatman GF/F filters that are washed with 25 mL of ice-cold buffer (20 mM Tris-HCl, pH 7.4). Radioligand bound to filters accounted for 5-700 dpm that is subtracted before calculating specific binding[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

ReN-1869 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ReN-1869170149-76-5NNC-05-1869ReN1869ReN 1869Histamine ReceptorInhibitorinhibitorinhibit

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