aladdin 阿拉丁 L408678 盐酸洛哌丁胺 34552-83-5 10mM in DMSO

中文名：盐酸洛哌丁胺

英文名：Loperamide HCl

英文别名：ADL 2-1294;4-​(4-​chlorophenyl)​-​4-​hydroxy-​N,​N-​dimethyl-​α,​α-​diphenyl-1-​piperidinebutanamide​, hydrochloride (1:1)

纯度：10mM in DMSO

货号：L408678

包装：1ml

Cas号：34552-83-5

存储温度：-80℃储存

产品介绍：

Information

Loperamide HCl (ADL 2-1294) is a selectiveμ-opioid receptoragonist opioid withKiof 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bow
In vitro

Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [³⁵S]guanosine-5\'-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM.

In vivo

Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

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