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Fentanyl Analogs Exert Antinociceptive Effects via Sodium Channel Blockade in Mice
This study investigated whether opioid-related compounds could suppress glutamate- and veratrine-induced nociceptive responses in mice at the same dose. The administration of morphine (3 mg/kg), hydromorphone (0.4 mg/kg), or fentanyl (0.03 mg/kg) suppressed glutamate-induced nociceptive response, but not veratrine-induced nociceptive response at the same doses. However, high doses of morphine (10 mg/kg), hydromorphone (2 mg/kg), or fentanyl (0.1 mg/kg) produced a significant reduction in the veratrine-induced nociceptive response. These results indicate that high doses are required when using morphine, hydromorphone, or fe...
Source: Biological and Pharmaceutical Bulletin - April 24, 2024 Category: Drugs & Pharmacology Authors: Satoka Kasai Natsuki Ogawa Miho Takagi Yukino Takahashi Kosho Makino Hironobu Arita Hideyo Takahashi Kazumi Yoshizawa Source Type: research

Modeling Developmental Changes in Caffeine Clearance Considering Differences between Pre- and Postnatal Period
Biol Pharm Bull. 2024;47(4):861-867. doi: 10.1248/bpb.b23-00650.ABSTRACTTaguchi et al. reported that postmenstrual age (PMA) is a promising factor in describing and understanding the developmental change of caffeine (CAF) clearance. The aim of the present study was to quantify how developmental changes occur and to determine the effect of the length of the gestational period on CAF clearance. We performed a nonlinear mixed effect model (NONMEM) analysis and evaluated the fit of six models. A total of 115 samples were obtained from 52 patients with a mean age of 34.3 ± 18.2 d. The median values of gestational age (GA) and ...
Source: Biological and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Haruka Ide Yukako Kawasaki Kentaro Tamura Taketoshi Yoshida Ryosuke Fujihara Akane Hara Masato Taguchi Source Type: research

Carbon Monoxide Alleviates Post-ischemia-reperfusion Skeletal Muscle Injury and Systemic Inflammation
Biol Pharm Bull. 2024;47(4):868-871. doi: 10.1248/bpb.b23-00917.ABSTRACTRestoration of blood flow in skeletal muscle after a prolonged period of ischemia induces muscular ischemia-reperfusion injury, leading to local injury/dysfunction in muscles followed by systemic inflammatory responses. However, preventive/curative agents for skeletal muscle ischemia injury are unavailable in clinics to date. Increasing evidence has validated that carbon monoxide (CO) prevents the progression of ischemia-reperfusion injury in various organs owing to its versatile bioactivity. Previously, we developed a bioinspired CO donor, CO-bound re...
Source: Biological and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Kazuaki Taguchi Shigeru Ogaki Hitoshi Maeda Yu Ishima Hiroshi Watanabe Masaki Otagiri Toru Maruyama Source Type: research

Detoxification and Activating Blood Circulation Decoction Promotes Reendothelialization of Damaged Blood Vessels via VEGF Signaling Pathway Activation by miRNA-126
In this study, we clarified the mechanism by which Detoxification and Activating Blood Circulation Decoction (DABCD) promotes vascular reendothelialization to avoid ISR by miRNA-126-mediated modulation of the vascular endothelial growth factor (VEGF) signaling pathway. A rat model of post-PCI restenosis was established by balloon injury. The injured aortic segment was collected 14 and 28 d after model establishment. Our findings indicate that on the 14th and 28th days following balloon injury, DABCD reduced intimal hyperplasia and inflammation and promoted vascular reendothelialization. Additionally, DABCD markedly increas...
Source: Biological and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Zhiming Liu Guangmie Xie Zuwei Li Hanbin Luo Jianhong Zhou Jie Cheng Xiaolin Wang Xiaoyan Huang Guohui Zou Source Type: research

The Influence of Emodin Succinyl Ethyl Ester on Non-Alcoholic Steatohepatitis Induced by a Diet High in Fructose, Cholesterol, and Fat in Mice
In this study, after 12 weeks of induction, the mice were treated with emodin succinyl ethyl ester (ESEE) for four weeks at doses of 10/30/90 mg/kg/day. The blood analysis of experimental endpoints showed that ESEE exhibited significant therapeutic effects on the progression of disorders of glycolipid metabolism and the induced liver injury in the model animals. Histopathological diagnosis of the liver and total triglyceride measurements revealed that ESEE had a significant therapeutic effect on the histopathological features of nonalcoholic fatty liver disease/hepatitis, such as cellular steatosis and activation of intrah...
Source: Biological and Pharmaceutical Bulletin - April 17, 2024 Category: Drugs & Pharmacology Authors: Yanxue Wang Liang Li Lingling Chen Jinlei Xia Tongli Wang Lei Han Liang Cao Zhenzhong Wang Wei Xiao Shan Jiang Source Type: research

Maitake Beta-Glucan Enhances the Therapeutic Effect of Trastuzumab via Antibody-Dependent Cellular Cytotoxicity and Complement-Dependent Cytotoxicity
This study demonstrates that the combination of trastuzumab and MD-Fraction exerts a greater antitumor effect than trastuzumab alone by enhancing ADCC, CDCC, and CDC in HER2-positive breast cancer.PMID:38616114 | DOI:10.1248/bpb.b23-00802 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - April 14, 2024 Category: Drugs & Pharmacology Authors: Yuki Masuda Shizuka Yamashita Yoshiaki Nakayama Ryohei Shimizu Morichika Konishi Source Type: research

Oral Administration of PLGA Nanoparticles to Deliver Antisense Oligonucleotides to Inflammatory Lesions in the Gastrointestinal Tract
In this study, we prepared antisense oligonucleotide (ASO)-encapsulated nanoparticles (NPs) with a suitable profile for oral administration for the treatment of inflammatory bowel disease (IBD). We chose a water-in-oil-in-water (w/o/w) method to prepare the NPs using poly(lactide-co-glycolide) as a matrix and Pluronic as a stabilizer. The obtained NPs had a suitable diameter (158 nm) for the penetration of the mucus layer, endocytic uptake by enterocytes, and accumulation in inflammatory lesions in the intestine. The amount of ASOs in the NPs was relatively large (6.41% (w/w)). When the NPs were stably dispersed in solutio...
Source: Biological and Pharmaceutical Bulletin - April 14, 2024 Category: Drugs & Pharmacology Authors: Yuta Yagi Yiwei Liu Jinting Li Shunsuke Shimada Munetaka Ohkouchi Yasushi Taguchi Teruki Nii Takeshi Mori Yoshiki Katayama Source Type: research