BW-180C ([D-Ala2, D-Leu5]-Enkephalin) is a water soluble Opioid Receptor peptide agonist.
IC50 Target
Opioid Receptor[1]
体外研究 (In Vitro)
BW-180C ([D-Ala2, D-Leu5]-Enkephalin) significantly inhibits cellular transcription in SH-SY5Y cells without causing cell injury. Following recovery for 72 h without BW-180C in primary neurons, the transcriptional activity fully resumes[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
BW-180C ([D-Ala2, D-Leu5]-Enkephalin) protects against I-R injury in hepatocytes, but not in the sinusoidal endothelial cells of the liver in rats. GPT levels are significantly lower in the BW-180C group as compared to those of the Control group, but the serum levels of HA are not different between the two groups. The concentrations of MDA of the liver tissue are significantly lower in the BW-180C group than in the Control group[2]. BW-180C (DADLE)-induced analgesia is mediated by the stimulation of both mu- and delta-opioid receptors[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
569.65
Formula
C29H39N5O7
CAS 号
63631-40-3
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tian J, et al. [D-Ala2, D-Leu5] encephalin (DADLE) reversibly inhibits cellular transcription in neurons without causing cell injury. Brain Res. 2014 May 27;1565:1-7.
[2]. Yamanouchi K, et al. [D-Ala2, D-Leu5] enkephalin (DADLE) protects liver against ischemia-reperfusion injury in the rat. J Surg Res. 2003 Sep;114(1):72-7.
[3]. Suh HH, et al. Different types of opioid receptors mediating analgesia induced by morphine, DAMGO, DPDPE, DADLE and beta-endorphin in mice. Naunyn Schmiedebergs Arch Pharmacol. 1990 Jul;342(1):67-71.
Cell Assay [1]
Primary cortical neurons are plated in 96-well plates and cultured with 100 nM BW-180C for 72 h. 5 mg/mL MTT in an amount equal to 10% of the culture volume is added to each well 4 h before the end of treatment. After a 4-h incubation, the media is removed, and MTT solvent in amount equal to original culture volume is added to each well to dissolve the crystals. The formation of formazan is analyzed within one hour after adding MTT solvent, by measuring the absorbance at a wavelength of 570 nm and a reference wavelength of 690 nm by using a microplate reader. The values in absorbance are normalized to the PBS-treated control to calculate the fold change[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2][3]
Rats[2]
After administration of BW-180C (BW-180C group) or normal saline as a vehicle (Control group), partial hepatic ischemia is induced by occluding the vessels supplying 92% of the liver for 45 min, followed by declamping the vessels and resection of the non-ischemic lobe. After 120 min of reperfusion, serum glutamic-pyruvic transaminase (GPT), hyaluronic acid (HA) levels, and concentrations of malondialdehyde (MDA) of the liver tissue are measured. Additionally, bile output from the ischemic lobes is measured after reperfusion[2].
Mice[3]
A single i.c.v, injection of opioid agonist alone or agonist in combination with antagonist. Injection volume for i.c.v, injection is 5 μL. The dose-response relationships are established by injecting i.c.v, with different doses of morphine sulfate, DAMGO, DPDPE, BW-180C, or p-endorphin in the presence or absence of a fixed dose of CTOP (0.025 or 0.05 μg), ICI 174864 (5 μg), or ICI 154129 (5 μg). The agonists and antagonists are mixed, and given as a single i.c.v, injection[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Tian J, et al. [D-Ala2, D-Leu5] encephalin (DADLE) reversibly inhibits cellular transcription in neurons without causing cell injury. Brain Res. 2014 May 27;1565:1-7.
[2]. Yamanouchi K, et al. [D-Ala2, D-Leu5] enkephalin (DADLE) protects liver against ischemia-reperfusion injury in the rat. J Surg Res. 2003 Sep;114(1):72-7.
[3]. Suh HH, et al. Different types of opioid receptors mediating analgesia induced by morphine, DAMGO, DPDPE, DADLE and beta-endorphin in mice. Naunyn Schmiedebergs Arch Pharmacol. 1990 Jul;342(1):67-71.