首页 GPCR/G Protein Histamine Receptor ReN-1869 hydrochloride
ReN-1869 hydrochloride
编号 T12703     别名: NNC-05-1869 hydrochloride
CAS 170149-76-5     分子式 C24H28ClNO2     分子量 397.94
靶点: histamine H1 receptor(ki);
ReN 1869 hydrochloride is a novel, selective antagonist of histamine H1 receptor.
选择批次  
纯度 98.00%
规格 库存 单价 数量
100 mg 待询 待询
500 mg 待询 待询
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生物活性

产品描述

ReN 1869 hydrochloride is a novel, selective antagonist of histamine H1 receptor.

靶点活性

histamine H1 receptor(ki),ki:0.19±0.04 μM

体外活性

ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H1 receptor antagonism. 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.

体内活性

ReN 1869 is a novel, selective histamine H(1) receptor antagonist. It is orally available, well tolerated, easily enters the central nervous system (CNS) but no adverse effects are seen in mice at 300 mg/kg. ReN 1869 at 0.01-10 mg/kg is antinociceptive in tests of chemical nociception in rodents (formalin, capsaicin, phenyl quinone writhing) but not in thermal tests (hot plate and tail flick). ReN 1869 amplifies the analgesic action of morphine but does not show tolerance after chronic dosing. Moreover, the compound is effective against inflammation of neurogenic origin (antidromic nerve stimulation, histamine-evoked edema) but not in carrageenan-induced inflammation. We suggest that ReN 1869, via H(1) blockade, counteracts the effect of histamine liberated from activated mast cells and inhibits pain transmission in the dorsal spinal cord. ReN 1869 represents a new class of antihistamines with pain-relieving properties that probably is mediated centrally through histamine H(1) receptors but alternative mechanisms of action cannot be excluded.

化学信息

分子量

397.94

分子式

C24H28ClNO2

CAS

170149-76-5

溶解度

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.513 ml 12.565 ml 25.129 ml
5 mM 0.503 ml 2.513 ml 5.026 ml
10 mM 0.251 ml 1.256 ml 2.513 ml
50 mM 0.05 ml 0.251 ml 0.503 ml
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