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ReN-1869 hydrochloride

CAS No. : 170149-76-5

MCE 站：ReN-1869 hydrochloride

产品活性：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)，K_i 值分别为 0.19±0.04 μM 和 0.45 μM。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

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 K_i of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [³H]1,3-di-tolylguanidine (DTG)] with a K_i of 0.45 μM. ReN 1869 dose-dependently reduces the responses with IC₅₀ of 1.70±0.002 μM.

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.

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