货号:A171923
同义名:
盐酸洛哌丁胺
/ R-18553 hydrochloride; Loperamide(hydrochloride)
Loperamide HCl是一种强效且选择性的μ-阿片受体激动剂。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Opioid receptor ↓ ↑ | ORL1 ↓ ↑ | μ-opioid receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Racecadotril | ✔ | 98% | |||||||||||||||||
JTC-801 |
++
Opioid receptor-like1 (ORL1), IC50: 94 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Loperamide (Hydrochloride) is an opioid receptor agonist widely used for the treatment of diarrhea[3]. In contrast with other opioid agonists, loperamide is a peripherally acting μ-receptor agonist exerting its effects mainly on the myenteric plexus of the gastrointestinal longitudinal muscle layer. It decreases peristalsis and fluid secretion resulting in longer gastrointestinal transit time. The bioavailability of the drug is extremely low. Moreover, it is actively excluded from the central nervous system; hence, it lacks the central effects of euphoria and analgesia at the recommended dosages[4]. Rats were orally gavaged with 1.5, 3, or 6 mg/kg body weight (BW) of loperamide hydrochloride for 7 days. The results after 7 days administration of loperamide, revealed dose-dependent increase in aspartate aminotransferase, lactate dehydrogenase, creatine kinase-MB, and serum concentration of cardiac troponin I, total homocysteine, and nitric oxide. Loperamide provoked cardiotoxicity through oxidative stress, lipid peroxidation, and DNA fragmentation in rats[5]. Loperamide decreased cell viability in a dose-dependent fashion and was most effective against canine osteosarcoma cells. When co-incubated with doxorubicin, loperamide induced a synergistic cell kill in canine carcinoma cells[6]. |
Concentration | Treated Time | Description | References | |
L-mdr1a | 2 μM | 4 hours | Loperamide was very effectively transported by the mouse mdr1a P-GP | J Clin Invest. 1996 Jun 1;97(11):2517-24. |
L-MDR1 | 2 μM | 4 hours | Loperamide was very effectively transported by the human MDR1 P-GP | J Clin Invest. 1996 Jun 1;97(11):2517-24. |
LLC-PK1 | 2 μM | 4 hours | Loperamide was very effectively transported by both the MDR1 and the mdr1a P-GP | J Clin Invest. 1996 Jun 1;97(11):2517-24. |
Pituitary GH4C1 cells | 30 μM | Loperamide augments intracellular calcium levels after activation of SOC channels. | 1997 Dec 23;94(26):14912-7. doi: 10.1073/pnas.94.26.14912. | |
RBL-2H3 mast cells | 30 μM | Loperamide augments intracellular calcium levels after activation of SOC channels. | 1997 Dec 23;94(26):14912-7. doi: 10.1073/pnas.94.26.14912. | |
Smooth muscle DDT-MF2 cells | 30 μM | Loperamide augments intracellular calcium levels after activation of SOC channels. | 1997 Dec 23;94(26):14912-7. doi: 10.1073/pnas.94.26.14912. | |
Astrocytoma 1321N cells | 30 μM | Loperamide augments intracellular calcium levels after activation of SOC channels and also causes elevation in calcium levels in the absence of SOC channel activation. | 1997 Dec 23;94(26):14912-7. doi: 10.1073/pnas.94.26.14912. | |
NIH 3T3 fibroblasts | 30 μM | Loperamide augments intracellular calcium levels after activation of SOC channels. | 1997 Dec 23;94(26):14912-7. doi: 10.1073/pnas.94.26.14912. | |
HL-60 leukemic cells | 10–30 μM | Loperamide augments intracellular calcium levels when SOC channels are activated but has no effect when SOC channels are not activated. | 1997 Dec 23;94(26):14912-7. doi: 10.1073/pnas.94.26.14912. | |
Administration | Dosage | Frequency | Description | References | ||
Mice | Mdr1a (−/−) mice | Oral | 1 mg/kg | Single dose, analyzed after 4 hours | Loperamide showed a marked 13.5-fold increase in brain radioactivity levels in mdr1a (?/?) mice, indicating that mdr1a P-GP in the blood-brain barrier restricts loperamide entry | J Clin Invest. 1996 Jun 1;97(11):2517-24. |
Mice | 5xFAD transgenic mice | Oral | 5 mg/kg body weight | Once per week for 4 weeks | To evaluate the effects of loperamide-induced slow gut transit on Alzheimer's disease pathology. Results showed that loperamide treatment increased amyloid-beta and microglia levels in the brain and altered the transcription of genes related to norepinephrine secretion and immune responses in colonic tissue. | J Adv Res. 2024 Nov;65:283-295 |
ICR CD1 mice | CFA-induced inflammatory pain model | Intrathecal injection, intraplantar injection, subcutaneous injection | 0.01–1 nmol (intrathecal), 4.6 nmol (intraplantar), 0.8 mg/kg (subcutaneous) | Single administration, behavioral tests performed 15 min (intraplantar) or 45 min (subcutaneous) post-injection | To evaluate the synergistic analgesic effects of loperamide-oxymorphindole combination in inflammatory pain. Results demonstrated significant synergy (10-150-fold ED50 reduction) across spinal, peripheral and systemic routes, mediated by peripheral μ- and δ-opioid receptors. | Anesthesiology. 2019 Sep;131(3):649-663 |
Transgenic CF mice | CF mouse model | Inhalation | 1 mmol/l | Single dose, two minutes duration | Loperamide inhibits sodium ion absorption in the airway epithelium of CF mice with a longer duration of action than amiloride. | Thorax. 1996 Dec;51(12):1229-32 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03575078 | Lymphoma | Phase 1 | Not yet recruiting | August 23, 2023 | - |
NCT00555620 | - | Completed | - | - | |
NCT02677844 | - | Completed | - | - | |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.19mL |
9.74mL 1.95mL 0.97mL |
19.47mL 3.89mL 1.95mL |
CAS号 | 34552-83-5 |
分子式 | C29H34Cl2N2O2 |
分子量 | 513.5 |
SMILES Code | O=C(N(C)C)C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3.[H]Cl |
MDL No. | MFCD00058581 |
别名 | 盐酸洛哌丁胺 ;R-18553 hydrochloride; Loperamide(hydrochloride); R 18553; PJ 185; NSC 696356; Loperamide hydrochloride; R-18553(hydrochloride) |
运输 | 蓝冰 |
InChI Key | PGYPOBZJRVSMDS-UHFFFAOYSA-N |
Pubchem ID | 71420 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature |
溶解方案 |
DMSO: 50 mg/mL(97.37 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 1 mg/mL(1.95 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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