586368-06-1
Olcegepant (hydrochloride)(Olcegepant (hydrochloride))
CAS: 586368-06-1
化学式: C38H48Br2ClN9O5
<"" ="xl" "">| 中文名 | Olcegepant (hydrochloride) |
| 英文名 | Olcegepant (hydrochloride) |
| 别名 | 化合物 T12293 |
| 英文别名 | BIBN-4096 HYDROCHLORIDE BIBN-4096 hydrochloride BIBN4096BS hydrochloride BIBN-4096BS hydrochloride BIBN4096BS HYDROCHLORIDE BIBN 4096BS hydrochloride BIBN 4096BS HYDROCHLORIDE BIBN-4096BS HYDROCHLORIDE Olcegepant (hydrochloride) |
| CAS | 586368-06-1 |
| 化学式 | C38H48Br2ClN9O5 |
| 分子量 | 906.12 |
| 溶解度 | H2O: ≥ 66.66 mg/mL |
| 存储条件 | -20℃ |
| 体外研究 | Olcegepant possesses higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology. Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (K i ) for human CGRP receptors of 14.4±6.3 (n=4) pM. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Olcegepant (BIBN4096BS) exhibits competitive antagonism at the CGRP receptor present in SK-N-MC cells. Isolated human cerebral, coronary, and omental arteries are studied with a sensitive myograph technique. CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner. |
| 体内研究 | Olcegepant (BIBN4096BS) in doses between 1 and 30 μg/kg (i.v.) inhibits the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly reduces mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly reduces the number of c-Fos immunolabeled cells in spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in trigeminal ganglion of CCI-ION rats. |
586368-06-1 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.104 ml | 5.518 ml | 11.036 ml |
| 5 mM | 0.221 ml | 1.104 ml | 2.207 ml |
| 10 mM | 0.11 ml | 0.552 ml | 1.104 ml |
| 5 mM | 0.022 ml | 0.11 ml | 0.221 ml |
586368-06-1 - 简介
Olcegepant (hydrochloride)是一种化合物，其化学名为N-[(3R,6R)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(1H-indol-5-yl)benzamide hydrochloride。以下是关于Olcegepant (hydrochloride)的性质，用途，制法和安全信息的介绍：性质：
- Olcegepant (hydrochloride)是一种白色结晶粉末，可溶于水和有机溶剂。
- 它的化学结构使其属于一类被称为CGRP（钙调蛋白基因相关肽）受体拮抗剂。
用途：
- 它的作用机制是通过抑制CGRP受体的活性，从而减少CGRP介导的神经递质的释放。
制法：
- Olcegepant (hydrochloride)的制备一般涉及一系列的有机合成化学反应步骤。
- 具体的制法通常属于专利范畴，相关的具体合成工艺并不公开。
安全信息：
- Olcegepant (hydrochloride)的安全性和副作用受多种因素影响，如剂量、服用方式、个体差异等。
- 在临床试验中，Olcegepant (hydrochloride)显示出一定程度的耐受性。
- 一些可能的副作用包括头痛、注射部位疼痛、恶心、呕吐等。最后更新：2024-04-09 20:49:11
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