Abstract：
:The Nuclear factor (erythroid 2-derived)-like 2 (Nrf2) plays a key role in inflammation which is implicated in the pathophysiology of depression. The Nrf2 activators have antidepressant effects in animal models of depression. The present study was undertaken to examine whether TBE-31 [(±)-(4bS,8aR,10aS)-10a-ethynyl-4b,8,8-trimethyl-3,7-dioxo-3,4b,7,8,8a,9,10,10a-octahydrophenanthrene-2,6-dicarbonitrile] and MCE-1 [(±)-3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile], the novel Nrf2 activators, could show antidepressant effects in inflammation model of depression. We found that TBE-31 and MCE-1 significantly potentiated nerve growth factor (NGF)-induced neurite outgrowth in PC12 cells, in a concentration dependent manner. The Nrf2 siRNA, but not negative control of siRNA, significantly blocked the potentiating effects of TBE-31 and MCE-1 on neurite outgrowth in PC12 cells. Furthermore, oral administration of TBE-31 or MCE-1 significantly attenuated an increase in serum levels of tumor necrosis factor-α (TNF-α) after administration of lipopolysaccharide (LPS: 0.5mg/kg). In the tail-suspension test and forced swimming test, oral administration of TBE-31 or MCE-1 significantly attenuated an increase in the immobility time after LPS (0.5mg/kg) administration. These findings suggest that the novel Nrf2 activators such as TBE-31 and MCE-1 might be potential therapeutic drugs for inflammation-related depression.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Yao W,Zhang JC,Ishima T,Ren Q,Yang C,Dong C,Ma M,Saito A,Honda T,Hashimoto Kdoi
10.1016/j.ejphar.2016.10.037subject
Has Abstractpub_date
2016-12-15 00:00:00pages
21-27eissn
0014-2999issn
1879-0712pii
S0014-2999(16)30677-Xjournal_volume
793pub_type
杂志文章abstract：:Longitudinal organ bath preparations of the rat duodenum, jejunum and ileum were tested for their responsiveness to GABA-receptor agonists. The GABAA-receptor agonists, GABA and 3APS, induced non-adrenergic, non-cholinergic relaxations and/or contractions, although the magnitude and type of response varied depending u...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90274-3
更新日期：1987-09-11 00:00:00
abstract：:The aim of this study was to elucidate the possible mechanism of the potentiating action of metal ions (Cu2+, Hg2+, Ag+ and SeO3(2-)) on the ryanodine-induced contracture of the mouse diaphragm. The ryanodine contracture in the quiescent muscle could be augmented by either electrical stimulation or pretreatment with h...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90443-x
更新日期：1994-01-04 00:00:00
abstract：:Pyrethroid insecticides have been reported to increase transmembrane sodium influx and inhibit ion-dependent ATPases in insect, squid, and toad nerve tissues. Since changes in sarcolemmal ion fluxes and inhibition of membrane-bound ATPases can alter myocardial contractility, the effects of a potent synthetic pyrethroi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90279-6
更新日期：1984-03-02 00:00:00
abstract：:The lack of specific receptors (and antagonists) has hampered the research on the neural mechanism of action of adrenocorticotropic hormone (ACTH)- and melanocyte-stimulating hormone (MSH)-like peptides. Yet the original observations in the 1970s already pointed to cAMP as a possible mediator of ACTH/MSH effects in ne...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(00)00537-9
更新日期：2000-09-29 00:00:00
abstract：:The antithrombotic effect of desethyl KBT-3022, which is the main active metabolite of the new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl] pyrrol-1-ylacetate; a cyclooxygenase inhibitor), was determined using a photochemically induced arterial thrombosis model in the rat femoral artery...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)83044-0
更新日期：1997-06-11 00:00:00
abstract：:Rovatirelin ([1-[-[(4S,5S)-(5-methyl-2-oxo oxazolidin-4-yl) carbonyl]-3-(thiazol-4-yl)-l-alanyl]-(2R)-2-methylpyrrolidine) is a novel synthetic agent that mimics the actions of thyrotropin-releasing hormone (TRH). The aim of this study was to investigate the electrophysiological and pharmacological effects of rovatire...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.05.047
更新日期：2015-08-15 00:00:00
abstract：:Intravenous infusions of sodium nitroprusside (SNP) at doses of 20, 40 or 80 micrograms/kg min-1 for 30 min produced dose-related decrements in blood pressure in conscious rats fitted with indwelling aortic and vena caval catheters. Immediately upon termination of SNP infusions, blood pressure rebounded to levels whic...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90473-4
更新日期：1979-10-01 00:00:00
abstract：:A possible new common action of immunosuppressants, besides suppression of the genes for cytokines like interleukin-2, was investigated in in vivo models. Dexamethasone (0.1 mg/kg, s.c.) failed to suppress ischemic paw edema in mice 1 h after its injection, but maximal suppression was achieved at 3 h (20%) whereafter ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01561-6
更新日期：1998-03-05 00:00:00
abstract：:R-isovaline is a non-proteinogenic amino acid which produces analgesia in a range of nociceptive assays. Mediation of this effect by metabotropic receptors for γ-aminobutyric acid (GABA) and glutamate, demonstrated by previous work, may depend on the type of tissue or receptor system. The objective of this study was t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.08.005
更新日期：2016-11-15 00:00:00
abstract：:Hruska et al. (1980) reported that hypophysectomy prevented the onset of dopamine receptor supersensitivity. We have repeated this investigation administering haloperidol (0.75 mg/day) or sulpiride (2 X 15 mg/day) or saline for 17 days, followed by a 3 day drug washout period, to sham-operated or hypophysectomised rat...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90006-6
更新日期：1981-11-19 00:00:00
abstract：:To test whether there is a common site of action for intravenous anaesthetics at the glycine receptor, the effects of binary combinations of thiopentone, pentobarbitone, methohexitone, and propofol have been tested on human alpha(1) glycine receptors expressed in Xenopus laevis oocytes using two-electrode voltage-clam...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.08.017
更新日期：2003-09-12 00:00:00
abstract：:The possible influence of several neuropeptides on muscarinic receptor binding and function in fronto-parietal cortex of young and senescent Fischer 344 rats was examined. Low concentrations (100 nM) of cholecystokinin, neurotensin and vasoactive intestinal polypeptide (VIP), added in vitro, enhanced carbachol-stimula...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90095-d
更新日期：1992-02-13 00:00:00
abstract：:The effects of beta-chlornaltrexamine (CNA, 5 mg/kg s.c.) on social conflict analgesia and brain opioid binding were investigated in mice at different times after the administration of the alkylating antagonist. The specific binding of [3H]etorphine to high-affinity binding sites and the stress-induced analgesia of at...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90525-0
更新日期：1988-10-18 00:00:00
abstract：:Because of their importance in pathophysiology, the dopamine receptors have been the subjects of intense pharmacological and physiological research. Their structures have remained mostly unknown until recently with the application of molecular biological approaches. The cloning of the first dopamine receptor, the D2 r...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/0922-4106(91)90001-x
更新日期：1991-08-14 00:00:00
abstract：:We determined the role of high-grade inflammation on endothelial function and its association with biomarkers of endothelial dysfunction in collagen-induced arthritis. Sprague-Dawley rats were divided into a control (n = 12) or collagen-induced arthritis (CIA; n = 21) group. To induce arthritis, Bovine-type-II collage...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172786
更新日期：2019-12-15 00:00:00
abstract：:The effects of substitutions in the xanthine nucleus on tracheal relaxant activity, atrium chronotropic activity, adenosine A1 affinity, and inhibitory activities on cyclic AMP-phosphodiesterase isoenzymes in guinea pigs were studied. Substitution with a long alkyl chain at the N1-position of xanthine nucleus increase...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90156-2
更新日期：1994-05-17 00:00:00
abstract：:Neurotoxins are harmful to nervous system and cause either neuronal cell death or impairment of synaptic activity, which contributes to Parkinson's disease or other neuronal disorders. Hippocampal synaptic plasticity was proposed as a cellular model for memory processing. In this study, we reported a novel effect of n...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.048
更新日期：2017-01-15 00:00:00
abstract：:Dopamine hyperpolarizes growth hormone-producing cells (GHC) in the CNS of Lymnaea stagnalis. This effect of dopamine was mimicked by the D-2 receptor agonist LY 141865 and antagonized by the D-2 receptor antagonists (-)-sulpiride and YM 09151-2. SKF 38393, a selective D-1 receptor agonist, increased the excitability ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90735-0
更新日期：1984-11-13 00:00:00
abstract：:Cyclophosphamide (CPA) is a chemotherapeutic drug widely used in the treatment of breast cancer or leukemia in clinic. However, CPA was reported to have hepatotoxicity. This study aims to observe the engaged mechanism of CPA-induced liver injury in mice and the protection of liquiritin (LQ) and liquiritigenin (LG). Li...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172421
更新日期：2019-08-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.03.047
更新日期：2008-06-10 00:00:00
abstract：:Affinity cross-linking of the bradykinin B2 receptor was performed using [125I-Tyr8]bradykinin, disulfosuccinimidyl tartrate as linker and crude membranes from guinea pig ileum smooth muscle immobilized on Whatman GF/B glass fiber filters. After SDS (sodium dodecylsulfate)-polyacrylamide gel electrophoresis under redu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90199-6
更新日期：1994-07-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.05.029
更新日期：2007-09-10 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90701-3
更新日期：1994-05-12 00:00:00
abstract：:The effects of bepridil and nifedipine, newly developed Ca2+ antagonists, were studied on the spontaneous action potentials of the true pacemaker cell preparations (0.5 X 0.5 mm) obtained from the rabbit sino-atrial (SA) node. At the lower concentrations, bepridil (10(-6) M) and nifedipine (10(-8) M) decreased the spo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90245-0
更新日期：1984-03-23 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)00670-3
更新日期：1995-02-14 00:00:00
abstract：:The effect of i.v. morphine on the spinal nociceptive flexor reflex was examined in decerebrate, unanesthetized rats in which the spinal cord was acutely or chronically transected. In acutely spinalized rats i.v. morphine dose dependently depressed the flexor reflex with an ED50 of 1.4 mg/kg. In rats in which the spin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94175-w
更新日期：1990-12-04 00:00:00
abstract：:Itching is known as a commonly side effect of opioid administration. However, the relationship of opioid receptors to itching is unclear. In this study, we examined the effect of intradermal injection of morphine and fentanyl on the itching sensation. When injected intradermally into the rostral back of mice, morphine...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.10.066
更新日期：2010-02-10 00:00:00
abstract：:The objective of this study was to determine the in vivo effectiveness of the selective endothelin ETA receptor antagonist PD 156707 (sodium 2-benzo[1,3]dioxol-5-yl-4-(4-methoxy-phenyl)-4-oxo-3-(3,4,5-trimet hoxy- benzyl)-but-2-enoate). Effectiveness was defined by the ability of the compound to block increases in ren...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00954-5
更新日期：1997-03-05 00:00:00
abstract：:Activation of muscarinic M2 receptors has been suggested to account, in part, for the reduced relaxant potency of beta-adrenoceptor agonists in canine and guinea-pig tracheal smooth muscle pre-contracted with muscarinic agonists as compared to histamine. The aim of the present study was to determine whether the potenc...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00048-p
更新日期：1995-03-14 00:00:00
abstract：:Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00967-4
更新日期：1999-02-19 00:00:00
