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Journal of Pharmacological Sciences

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https://www.readbyqxmd.com/read/29317180/oral-administration-of-fisetin-promotes-the-induction-of-hippocampal-long-term-potentiation-in%C3%A2-vivo
#1
Wen-Bin He, Kazuho Abe, Tatsuhiro Akaishi
To explore memory enhancing effect of the flavonoid fisetin, we investigated the effect of oral administration of flavonoids on the induction of long-term potentiation (LTP) at hippocampal CA1 synapses of anesthetized rats. Among four flavonoids (fisetin, quercetin, luteolin and myricetin) tested, only fisetin significantly facilitated the induction of hippocampal LTP. The effect of oral fisetin was abolished by intracerebroventricular injection of U0126, an agent that was previously found to inhibit its effect in hippocampal slices in vitro...
December 20, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29292053/the-anti-influenza-drug-oseltamivir-evokes-hypothermia-in-mice-through-dopamine-d2-receptor-activation-via-central-actions
#2
Akihiro Fukushima, Arisa Fukui, Yuki Takemura, Yasuhiro Maeda, Hideki Ono
Oseltamivir has a hypothermic effect in mice when injected intraperitoneally (i.p.) and intracerebroventricularly (i.c.v.). Here we show that the hypothermia evoked by i.c.v.-oseltamivir is inhibited by non-selective dopamine receptor antagonists (sulpiride and haloperidol) and the D2-selective antagonist L-741,626, but not by D1/D5-selective and D3-selective antagonists (SCH-23390 and SB-277011-A, respectively). The hypothermic effect of i.p.-administered oseltamivir was not inhibited by sulpiride, haloperidol, L-741,626 and SCH-23390...
December 15, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29289470/prostanoid-dependent-bladder-pain-caused-by-proteinase-activated-receptor-2-activation-in-mice-involvement-of-trpv1-and-t-type-ca2-channels
#3
Maho Tsubota, Tomoka Ozaki, Yuko Hayashi, Yasumasa Okawa, Ayaka Fujimura, Fumiko Sekiguchi, Hiroyuki Nishikawa, Atsufumi Kawabata
We studied the pronociceptive role of proteinase-activated receptor-2 (PAR2) in mouse bladder. In female mice, intravesical infusion of the PAR2-activating peptide, SLIGRL-amide (SL), caused delayed mechanical hypersensitivity in the lower abdomen, namely 'referred hyperalgesia', 6-24 h after the administration. The PAR2-triggered referred hyperalgesia was prevented by indomethacin or a selective TRPV1 blocker, and restored by a T-type Ca2+ channel blocker. In human urothelial T24 cells, SL caused delayed prostaglandin E2 production and COX-2 upregulation...
December 15, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29277372/effects-of-chlorogenic-acid-on-carbachol-induced-contraction-of-mouse-urinary-bladder
#4
Takeharu Kaneda, Noriyasu Sasaki, Norimoto Urakawa, Kazumasa Shimizu
Chlorogenic acid (CGA) is a polyphenol found in coffee and medicinal herbs such as Lonicera japonica. In this study, the effect of CGA-induced relaxation on carbachol (CCh)-induced contraction of mouse urinary bladder was investigated. CGA (30-300 μg/ml) inhibited CCh- or U46619-induced contraction in a concentration-dependent manner. SQ22536 (adenylyl cyclase inhibitor) recovered CGA-induced relaxation of CCh-induced contraction; however, ODQ (guanylyl cyclase inhibitor) did not have the same effect. In addition, 3-isobutyl-1-methylxanthine (IBMX) enhanced CGA-induced relaxation; however, forskolin or sodium nitroprusside did not have the same effect...
December 15, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29277371/repeated-fluvoxamine-treatment-recovers-early-postnatal-stress-induced-hypersociability-like-behavior-in-adult-rats
#5
Haruko Kumamoto, Taku Yamaguchi, Kohtarou Konno, Takeshi Izumi, Takayuki Yoshida, Yu Ohmura, Masahiko Watanabe, Mitsuhiro Yoshioka
Childhood maltreatment is associated with impaired adult brain function, particularly in the hippocampus, and is not only a major risk factor for some psychiatric diseases but also affects early social development and social adaptation in later life. The aims of this study were to determine whether early postnatal stress affects social behavior and whether repeated fluvoxamine treatment reverses these changes. Rat pups were exposed to footshock stress during postnatal days 21-25 (at 3 weeks old: 3wFS). During the post-adolescent period (10-14 weeks postnatal), the social interaction test and Golgi-cox staining of dorsal hippocampal pyramidal neurons were performed...
December 9, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29276114/acacetin-protects-against-cardiac-remodeling-after-myocardial-infarction-by-mediating-mapk-and-pi3k-akt-signal-pathway
#6
Wei Chang, Qing-Qing Wu, Yang Xiao, Xiao-Han Jiang, Yuan Yuan, Xiao-Feng Zeng, Qi-Zhu Tang
Since inhibiting cardiac remodeling is a critical treatment goal after myocardial infarction (MI), many drugs have been evaluated for this purpose. Acacetin is a flavonoid compound that has been shown to have anti-cancer, anti-mutagenic, anti-inflammatory and anti-peroxidative effects. In this study, we investigated whether acacetin is able to exert a protective effect against MI. One week after anterior wall standard MI surgeries or sham surgeries were performed in mice, acacetin was administered via gavage for two weeks...
December 1, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29249634/the-effects-of-dipeptidyl-peptidase-4-on-cardiac-fibrosis-in-pressure-overload-induced-heart-failure
#7
Masanori Hirose, Hiroyuki Takano, Hiroshi Hasegawa, Hiroyuki Tadokoro, Naoko Hashimoto, Genzo Takemura, Yoshio Kobayashi
Dipeptidyl peptidase-4 (DPP-4) inhibitors are hypoglycemic agents. DPP-4 inhibitor has cardioprotective effects after transverse aortic constriction (TAC), but role of DPP-4 on cardiac fibrosis after TAC is not well known. Our aim was to determine the effects of DPP-4 on cardiac fibrosis in murine TAC model. Wild-type mice and DPP-4 knockout mice were subjected to TAC. Wild-type mice were then treated with vehicle or DPP-4 inhibitor. DPP-4 activities in serum and heart tissue were significantly increased at 2 weeks after TAC, but they were significantly decreased by DPP-4 inhibitor treatment...
November 24, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29274665/red-ginseng-extracts-attenuate-skin-inflammation-in-atopic-dermatitis-through-p70-ribosomal-protein-s6-kinase-activation
#8
Mayuko Osada-Oka, Sayaka Hirai, Yasukatsu Izumi, Kazuhiro Misumi, Keiichi Samukawa, Shuhei Tomita, Katsuyuki Miura, Yukiko Minamiyama, Hiroshi Iwao
Atopic dermatitis (AD) is a chronic and relapsing inflammatory skin disease with increased immunoglobulin E (IgE) levels. Activation of the mammalian target of rapamycin (mTOR)/p70 ribosomal protein S6 kinase (p70S6K) signaling is known to occur in the inflammatory regions of AD skin. We previously demonstrated that red ginseng extract (RGE), as an anti-inflammatory agent, had potential for treating AD. However, it is still unclear whether RGE inhibits mTOR/p70S6K signaling. Thus, we examined the anti-inflammatory effects of RGE on IgE or interferon-γ (IFN-γ) induced signaling pathways...
November 10, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29174627/role-of-nmda-receptor-glun2d-subunit-in-the-antidepressant-effects-of-enantiomers-of-ketamine
#9
Soichiro Ide, Yuiko Ikekubo, Masayoshi Mishina, Kenji Hashimoto, Kazutaka Ikeda
We investigated the rapid and sustained antidepressant effects of enantiomers of ketamine in N-methyl-d-aspartate (NMDA) receptor GluN2D subunit knockout (GluN2D-KO) mice. Intraperitoneal administration of ketamine or its enantiomers 10 min before the tail-suspension test exerted significant antidepressant effects on restraint stress-induced depression in both wildtype and GluN2D-KO mice. The antidepressant effects of (RS)-ketamine and (S)-ketamine were sustained 96 h after the injection in both wildtype and GluN2D-KO mice, but such sustained antidepressant effects of (R)-ketamine were only observed in wildtype mice...
November 10, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29146480/neuroprotection-by-chotosan-a-kampo-formula-against-glutamate-excitotoxicity-involves-the-inhibition-of-glun2b-but-not-glun2a-containing-nmda-receptor-mediated-responses-in-primary-cultured-cortical-neurons
#10
Sachie Sasaki-Hamada, Azusa Suzuki, Emi Sanai, Kinzo Matsumoto, Jun-Ichiro Oka
Chotosan (CTS), a traditional herbal formula called Kampo medicine, was shown to be effective in the treatment of vascular dementia in a clinical study, and exerted protective effects against transient cerebral ischemia-induced cognitive impairment in mice. In the present study, we investigated the neuroprotective effects of CTS using primary cultured rat cortical neurons. CTS (250-1000 μg/mL) inhibited neuronal death induced by 100 μM glutamate. This glutamate-induced neuronal death was blocked by a GluN2B-, but not GluN2A-containing NMDA receptor antagonist...
November 1, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29132796/old-drug-new-indication-olsalazine-sodium-reduced-serum-uric-acid-levels-in-mice-via-inhibiting-xanthine-oxidoreductase-activity
#11
Yanfen Niu, Hongjian Li, Lihui Gao, Hua Lin, Hsiangfu Kung, Marie Chia-Mi Lin, Kwong-Sak Leung, Man-Hon Wong, Wenyong Xiong, Ling Li
Hyperuricemia, a long-term purine metabolic disorder, is a well-known risk factor for gout, hypertension and diabetes. In maintaining normal whole-body purine levels, xanthine oxidase (XOD) is a key enzyme in the purine metabolic pathway, as it catalyzes the oxidation of hypoxanthine to xanthine and finally to uric acid. Here we used the protein-ligand docking software idock to virtually screen potential XOD inhibitors from 3167 approved small compounds/drugs. The inhibitory activities of the ten compounds with the highest scores were tested on XOD in vitro...
October 31, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29122532/pathological-prolongation-of-action-potential-duration-as-a-cause-of-the-reduced-alpha-adrenoceptor-mediated-negative-inotropy-in-streptozotocin-induced-diabetic-mice-myocardium
#12
Haruna Kanae, Shogo Hamaguchi, Yumi Wakasugi, Taichi Kusakabe, Keisuke Kato, Iyuki Namekata, Hikaru Tanaka
Effect of pathological prolongation of action potential duration on the α-adrenoceptor-mediated negative inotropy was studied in streptozotocin-induced diabetic mice myocardium. In streptozotocin-treated mouse ventricular myocardium, which had longer duration of action potential than that in control mice, the negative inotropic response induced by phenylephrine was smaller than that in control mice. 4-Aminopyridine prolonged the action potential duration and decreased the negative inotropy in control mice...
October 31, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29113791/pd149163-induces-hypothermia-to-protect-against-brain-injury-in-acute-cerebral-ischemic-rats
#13
Teng-Fei Xue, Xu Ding, Juan Ji, Hui Yan, Ji-Ye Huang, Xu-Dong Guo, Jin Yang, Xiu-Lan Sun
Therapeutic hypothermia is a promising strategy for acute cerebral ischemia via physical or pharmacological methods. In this study, we pharmacologically induced hypothermia on Sprague Dawley rats by intraperitoneally injecting PD149163. We found that mild hypothermia was induced by PD149163 treatment without local cerebral blood flow (LCBF) alteration. To evaluate the neuroprotective effects of PD149163, TTC staining, HE staining and Nissl's staining were performed in our study. We found that PD149163 could prevent neuronal damage, and inhibit proliferation and activation of glial cells induced by ischemia...
October 23, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29113790/the-persistent-inhibitory-properties-of-saxagliptin-on-renal-dipeptidyl-peptidase-4-studies-with-hk-2-cells-in%C3%A2-vitro-and-normal-rats-in%C3%A2-vivo
#14
Masako Uchii, Mariko Sakai, Yuhei Hotta, Satoshi Saeki, Naoya Kimoto, Akinori Hamaguchi, Tetsuya Kitayama, Shunji Kunori
Saxagliptin, a potent and selective DPP-4 inhibitor, exhibits a slow dissociation from DPP-4. We investigated the sustained effects of saxagliptin on renal DPP-4 activity in a washout study using renal tubular (HK-2) cells, and in a pharmacodynamic study using normal rats. In HK-2 cells, the inhibitory potency of saxagliptin on DPP-4 activity persisted after washout, while that of sitagliptin was clearly reduced. In normal rats, a single treatment of saxagliptin or sitagliptin inhibited the plasma DPP-4 activity to similar levels...
October 23, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29233468/butyrate-suppresses-motility-of-colorectal-cancer-cells-via-deactivating-akt-erk-signaling-in-histone-deacetylase-dependent-manner
#15
Qingran Li, Chujie Ding, Tuo Meng, Wenjie Lu, Wenyue Liu, Haiping Hao, Lijuan Cao
Butyrate is a typical short chain fatty acid produced by gut microbiota of which the dysmetabolism has been consistently associated with colorectal diseases. However, whether butyrate affects metastatic colorectal cancer is not clear. In this study we investigated in vitro the effect of butyrate on motility, a significant metastatic factor of colorectal cancer cells and explored the potential mechanism. By using wound healing and transwell-based invasion models, we demonstrated that pretreatment of butyrate significantly inhibited motility of HCT116, HT29, LOVO and HCT8 cells, this activity was further attributed to deactivation of Akt1 and ERK1/2...
December 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29217355/crocetin-attenuates-spared-nerve-injury-induced-neuropathic-pain-in%C3%A2-mice
#16
Xiaolei Wang, Guangqing Zhang, Yong Qiao, Chang Feng, Xin Zhao
Crocetin is the main component of saffron and exhibits anti-oxidative and anti-inflammatory effects. Neuroinflammation and oxidative stress have been recognized to play a crucial role in the pathogenesis of neuropathic pain. We investigated the effect of crocetin in a mouse model with neuropathic pain induced by spared nerve injury (SNI). Crocetin was intrathecally perfused at various doses for up to 12 days starting 3 days before the surgery. Behavioral tests were performed to determine pain sensitivity. The concentrations of proinflammatory cytokines tumor necrosis factor (TNF-α) and interleukin-1β (IL-1β) were measured to assess neuroinflammation...
December 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29083842/retraction-inhibition-of-arachidonic-acid-release-by-cytosolic-phospholipase-a2-is-involved-in-the-antiapoptotic-effect-of-fk506-and-cyclosporin-a-on-astrocytes-exposed-to-simulated-ischemia-in-vitro
#17
(no author information available yet)
No abstract text is available yet for this article.
October 19, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29107444/dopamine-d2l-receptor-interacting-proteins-regulate-dopaminergic-signaling
#18
REVIEW
Norifumi Shioda
Dopamine receptor family proteins include seven transmembrane and trimeric GTP-binding protein-coupled receptors (GPCRs). Among them, the dopamine D2 receptor (D2R) is most extensively studied. All clinically used antipsychotic drugs serve as D2R antagonists in the mesolimbic dopamine system, and their ability to block D2R signaling is positively correlated with antipsychotic efficiency. Human genetic studies also show a significant association of DRD2 polymorphisms with disorders including schizophrenia and Parkinson's disease...
October 14, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29129584/high-salt-loading-induces-urinary-storage-dysfunction-via-upregulation-of-epithelial-sodium-channel-alpha-in-the-bladder-epithelium-in-dahl-salt-sensitive-rats
#19
Seiji Yamamoto, Yuji Hotta, Kotomi Maeda, Tomoya Kataoka, Yasuhiro Maeda, Takashi Hamakawa, Yasuhiro Shibata, Shoichi Sasaki, Shinya Ugawa, Takahiro Yasui, Kazunori Kimura
We aimed to investigate whether high salt intake affects bladder function via epithelial sodium channel (ENaC) by using Dahl salt-resistant (DR) and salt-sensitive (DS) rats. Bladder weight of DR + high-salt diet (HS, 8% NaCl) and DS + HS groups were significantly higher than those of DR + normal-salt diet (NS, 0.3% NaCl) and DS + NS groups after one week treatment. We thereafter used only DR + HS and DS + HS group. Systolic and diastolic blood pressures were significantly higher in DS + HS group than in DR + HS group after the treatment period...
October 10, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29056256/glibenclamide-inhibits-nlrp3-inflammasome-mediated-il-1%C3%AE-secretion-in-human-trophoblasts
#20
Kazuhiro Tamura, Gen Ishikawa, Mikihiro Yoshie, Wakana Ohneda, Akihito Nakai, Toshiyuki Takeshita, Eiichi Tachikawa
Infection-associated pregnancy complications cause premature delivery. Caspase-1 is involved in the maturation of interleukin (IL)-1β, which is activated by the NLRP3 inflammasome. To characterize the significance of the NLRP3 inflammasome pathway in the placenta, the effects of activators and inhibitors on NLRP3-related molecules were examined using isolated primary trophoblasts. Caspase-1 and IL-1β mRNA expression was markedly increased in response to lipopolysaccharide (LPS), a toll-like receptor (TLR)4 ligand...
October 6, 2017: Journal of Pharmacological Sciences
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