おすすめの製品
アッセイ
≥99% (HPLC)
品質水準
フォーム
solid
有効性
2 nM Ki
メーカー／製品名
Calbiochem®
保管条件
OK to freeze
protect from light
色
white
溶解性
DMSO: 50 mM
ethanol: 50 mM
保管温度
2-8°C
SMILES記法
[Cl-].Clc1ccc(cc1)C2(CC[N+H](CC2)CCC(c4ccccc4)(c3ccccc3)C(=O)N(C)C)O
InChI
1S/C29H33ClN2O2.ClH/c1-31(2)27(33)29(24-9-5-3-6-10-24,25-11-7-4-8-12-25)19-22-32-20-17-28(34,18-21-32)23-13-15-26(30)16-14-23;/h3-16,34H,17-22H2,1-2H3;1H
InChI Key
PGYPOBZJRVSMDS-UHFFFAOYSA-N
詳細
A very potent and highly selective peripheral resctricted µ-opioid receptor agonist (Ki = 2 nM). Often used as an antidiarrheal, antipruritic, and antihyperalgesic agent. In addition, shown to improve defective post-receptor insulin signaling in skeletal muscle cells and enhance insulin sensitivity in rats.
生物化学的／生理学的作用
Primary Target
u opioid receptor
u opioid receptor
警告
Toxicity: Toxic (F)
調製ノート
Warming is required for complete solubilization in ethanol.
再構成
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
その他情報
Cheng, K., et al. 2013. Pharmaco. Ther.139, 334.
Di Bosco, M., et al. 2008. Chem. Biol. Drug Des.71, 328.
DeHaven-Hudkins, D., et al. 1999. J. Pharmacol. Exp. Ther.289, 494.
Mackerer, C., et al. 1976. J. Pharmacol. Exp. Ther.199, 131.
Di Bosco, M., et al. 2008. Chem. Biol. Drug Des.71, 328.
DeHaven-Hudkins, D., et al. 1999. J. Pharmacol. Exp. Ther.289, 494.
Mackerer, C., et al. 1976. J. Pharmacol. Exp. Ther.199, 131.
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法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
シグナルワード
Danger
危険有害性情報
危険有害性の分類
Acute Tox. 3 Oral
保管分類コード
6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Binding site of loperamide: automated docking of loperamide in human mu- and delta-opioid receptors.
Antonio Mazzella di Bosco et al.
Chemical biology & drug design, 71(4), 328-335 (2008-02-21)
Loperamide is a piperidine analogue, acting as agonist on peripheral opioid receptors, exhibiting affinity and selectivity for the cloned mu human opioid receptor compared with the delta human opioid receptor. Automatic docking studies of loperamide, using AutoDock, on human mu-
C R Mackerer et al.
The Journal of pharmacology and experimental therapeutics, 199(1), 131-140 (1976-10-01)
Loperamide, a new antidiarrheal agent, was tested to determine whether its biological activity involves binding to opiate receptor sites. Loperamide and morphine competitively inhibited 3H-naloxone binding to homogenates a guinea-pig brain and myenteric plexus. The Kp values obtain in the
D L DeHaven-Hudkins et al.
The Journal of pharmacology and experimental therapeutics, 289(1), 494-502 (1999-03-23)
The antihyperalgesic properties of the opiate antidiarrheal agent loperamide (ADL 2-1294) were investigated in a variety of inflammatory pain models in rodents. Loperamide exhibited potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta
Kai-Chun Cheng et al.
Pharmacology & therapeutics, 139(3), 334-340 (2013-05-22)
Type-2 diabetes is one of the fastest growing public health problems worldwide resulting from both environmental and genetic factors. Activation of μ-opioid receptor (MOR) could result in reversal of the impairment of insulin-stimulated glucose disposal in genetically obese Zucker rats
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