Olcegepant (hydrochloride),英文名:Olcegepant (hydrochloride),CAS:586368-06-1,化学式:C38H48Br2ClN9O5,分子量:90

586368-06-1 询问

Olcegepant (hydrochloride)(Olcegepant (hydrochloride))

CAS: 586368-06-1

化学式: C38H48Br2ClN9O5

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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

最后更新：2024-01-02 23:10:35

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