Asimadoline-HCl
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- CAS号:
- 185951-07-9
- 英文名:
- Asimadoline-HCl
- 英文别名:
- Asimadoline-HCl;EMD-61753 hydrochloride;Asimadoline Hydrochlorine;Asimadoline hydrochloride;N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide;syndrome,bowel,diabetic,EMD61753,Asimadoline,irritable,κ-opioid,δ-opioid,EMD 61753,inhibit,Asimadoline hydrochloride,EMD-61753,μ-opioid,Opioid Receptor,allodynia,Inhibitor
- 中文名:
- Asimadoline-HCl
- 中文别名:
- 阿西马朵林盐酸盐;化合物ASIMADOLINE HYDROCHLORIDE;PERFEMIKER]ASIMADOLINE HYDROCHLORIDE,98%
- CBNumber:
- CB53363778
- 分子式:
- C27H31ClN2O2
- 分子量:
- 451.01
- MOL File:
- 185951-07-9.mol
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Asimadoline-HCl化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 240 mg/mL (532.15 mM)
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Asimadoline-HCl性质、用途与生产工艺
Asimadoline (EMD-61753) hydrochloride 是一种口服有效的,选择性的,具有周边活性的 κ-opioid 激动剂,对豚鼠和人重组 κ-opioid 的 IC50s 分别为 5.6 nM 和 1.2 nM。Asimadoline hydrochloride 对血脑屏障的渗透性低,具有外周抗炎作用。Asimadoline hydrochloride 可改善糖尿病大鼠的异常性疼痛,并具有用于肠易激综合征 (IBS) 研究的潜力。
IC50: 5.6 nM (guinea pig κ opioid), 1.2 nM (human recombinant κ opioid)
Asimadoline (EMD-61753) hydrochloride has high selectively in κ: μ: δ opioid binding ratios of 1:501:498 in human recombinant receptors. The IC
50
for Asimadoline hydrochloride binding to μ-opioid receptors is 3 µM and to δ-opioid receptors is 0.7 µM. The IC
50
values for D1, D2, kainate, σ, PCP/NMDA, H1, α1, α2, M1/M2, glycine, 5HT1A, 5HT1C, 5HT1D, 5HT2, 5HT3, AMPA and kainate/AMPA receptors are all >10 µM.
Asimadoline hydrochloride has affinity to sodium and L type Ca
2+
ion channels at IC
50
concentrations 150 to 800 fold the IC
50
for the κ receptors.
At high concentrations, Asimadoline hydrochloride demonstrates spasmolytic action against 400 µM barium chloride in the rat duodenum (IC
50
=4.2 µM), suggesting that Asimadoline hydrochloride may block the direct stimulant effects of barium on smooth muscle through mechanisms that are not identified.
Asimadoline (EMD-61753 hydrochloride; 1, 5, 15 mg/kg; s.c.) acutely ameliorates both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
The absorption rate following oral administration is 80% in rats and >90% in dogs and monkeys. The metabolism of Asimadoline hydrochloride is rapid and appears similar in animals and man. Asimadoline hydrochloride has peripheral anti-inflammatory actions that are partly mediated through increase in joint fluid substance P levels.
Treatment with Asimadoline hydrochloride (5 mg/kg/day; i.p.) produces marked (and sustained) attenuation of the disease with all three time regimes.
Animal Model:
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Adult female Sprague-Dawley rats
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Dosage:
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1, 5, 15 mg/kg
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Administration:
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SC; single dose
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Result:
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Acutely ameliorated both formalin-evoked hyperalgesia and tactile allodynia in diabetic rats.
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Asimadoline-HCl
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-107384A | Asimadoline-HCl Asimadoline hydrochloride | 185951-07-9 | 5mg | 950元 |
2024/01/25 | HY-107384A | Asimadoline-HCl Asimadoline hydrochloride | 185951-07-9 | 10mM * 1mLin DMSO | 1045元 |
185951-07-9, Asimadoline-HCl 相关搜索:
- PERFEMIKER]ASIMADOLINE HYDROCHLORIDE,98%
- 化合物ASIMADOLINE HYDROCHLORIDE
- 阿西马朵林盐酸盐
- 185951-07-9
- syndrome,bowel,diabetic,EMD61753,Asimadoline,irritable,κ-opioid,δ-opioid,EMD 61753,inhibit,Asimadoline hydrochloride,EMD-61753,μ-opioid,Opioid Receptor,allodynia,Inhibitor
- EMD-61753 hydrochloride
- N-[(1S)-2-[(3S)-3-hydroxypyrrolidin-1-yl]-1-phenylethyl]-N-methyl-2,2-diphenylacetamide
- Asimadoline Hydrochlorine
- Asimadoline hydrochloride
- Asimadoline-HCl