Abstract:
:We recently reported that physiological concentrations of 17beta-estradiol partially down-regulate cardiac rapidly-activating delayed rectifier K(+) currents (hERG currents) independently of estrogen-receptor signaling. To determine if other estrogens have the same effect as that of 17beta-estradiol, we investigated receptor-independent effects of estrone, estrone 3-sulfate, and estriol on hERG currents in patch-clamped estrogen-negative HEK293 cells. Only estrone 3-sulfate partially suppressed hERG currents in a receptor-independent manner by modifying the gating. The concentration-dependence of estrone 3-sulfate revealed that physiological levels of circulating estrone 3-sulfate can modulate hERG currents to the maximal extent in both women and men at any age.
journal_name
J Pharmacol Scijournal_title
Journal of pharmacological sciencesauthors
Kakusaka S,Asayama M,Kaihara A,Sasano T,Suzuki T,Kurokawa J,Furukawa Tdoi
10.1254/jphs.08257scsubject
Has Abstractpub_date
2009-01-01 00:00:00pages
152-6issue
1eissn
1347-8613issn
1347-8648pii
JST.JSTAGE/jphs/08257SCjournal_volume
109pub_type
杂志文章abstract::Protective effect of valsartan (Val), an angiotensin II (AII)-receptor blocker (ARB), against organ damage is reported to depend on the dosing time in hypertensive patients. Dosing-time-dependent effect of Val on survival of stroke-prone spontaneously hypertensive rats (SHRSP) under a 12-h lighting cycle was examined....
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.10284fp
更新日期:2011-01-01 00:00:00
abstract::Intravital multiphoton microscopy has opened a new era in the field of biological imaging. Focal excitation of fluorophores by simultaneous attack of multiple (normally "two") photons generates images with high spatial resolution, and use of near-infrared lasers for multiphoton excitation allows penetration of thicker...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章,评审
doi:10.1254/jphs.12r03cp
更新日期:2012-01-01 00:00:00
abstract::Selegiline is used an adjunct to L-DOPA therapy. We investigated extracellular striatal dopamine (DA) level in awake rats treated with L-DOPA and/or selegiline using a microdialysis method. Rats given 10 mg/kg, i.p. per day selegiline for 7 days were administered with a single dose of 100 mg/kg, i.p. L-DOPA 0 (3 h), 1...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.fp0051085
更新日期:2006-08-01 00:00:00
abstract::L-Dihydroxyphenylalanine (L-DOPA) is considered the gold standard for the treatment of Parkinson's disease (PD). However, long-term administration of L-DOPA can induce abnormal side effects. On the other hand, selective serotonin reuptake inhibitors (SSRIs) including fluoxetine have gained tremendous popularity in the...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.12003fp
更新日期:2012-01-01 00:00:00
abstract::There is no direct evidence for the exact cilia-inhibitory effects of opioids, which are generally used to achieve general anesthesia in combination with other anesthetic drugs. These are the reasons, why we analysed direct concentration-dependent or systemic effects of anesthetics (propofol, sufentanil, and midazolam...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2020.01.005
更新日期:2020-04-01 00:00:00
abstract::Sargassum hemiphyllum (SH) has long been used in Korean folk medicine for the therapeutic treatment of various allergic diseases. The effects of SH in previous experimental models, however, have been inconclusive. We studied the effects of methanol extract of SH on mast cells. Our experiments showed that SH significan...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.fp0040326
更新日期:2005-02-01 00:00:00
abstract::Ca(2+) release from intracellular store sites via the ryanodine receptor (RyR) and hormonal regulation by flutamide, an androgen-receptor (AR) antagonist, on it were examined in vas deferens (VD) smooth muscle cells (SMCs). VD and VDSMCs were obtained from two groups of male rats that were treated p.o. with 100 mg/kg ...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.09037fp
更新日期:2009-05-01 00:00:00
abstract::Cancer remains a major health problem around the world. A Shiga toxin is a bacterial toxin often produced by Shigella dysenteriae and Escherichia coli. A subunit of the Shiga toxin (StxA) is a cytotoxic agent which could be used to induce death in cancer cells. StxA expressed from baculovirus was evaluated in a pTriEx...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2018.09.003
更新日期:2018-09-01 00:00:00
abstract::Our previous study showed that oridonin isolated from Rabdosia rubescens enhanced phagocytosis of apoptotic cells by macrophage-like U937 cells through tumor necrosis factor (TNF) alpha and interleukin (IL)-1beta release. In this study, we further investigated signaling events involved in oridonin-augmented phagocytos...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.fpj05005x
更新日期:2005-08-01 00:00:00
abstract::Sneezing and persistent itching of the nasal mucosa are distressing symptoms of allergic rhinitis (AR). Recent studies have revealed that hyperinnervation of sensory neurons in the nasal turbinate is one of the underlying causes of sneezing and itching. Since Semaphorin-3A (Sema3A) has been previously shown to restric...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.11005fp
更新日期:2011-01-01 00:00:00
abstract::We previously reported that nicotine (NIC)-induced analgesia was elicited in part by activation of the endogenous opioid system. Moreover, it is well known that NIC has physical-dependence liability, but its mechanism is unclear. Therefore, we examined whether physical dependence on NIC was mediated by activation of t...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.13172fp
更新日期:2014-01-01 00:00:00
abstract::Hot flushes are the most common complaint of menopausal women. In the present study, a new animal model of hot flushes was established. Tail skin temperature was measured with a thermo tracer after mice were subjected to a forced exercise task using a motor driven treadmill. In ovariectomized mice, forced exercise for...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.sc0050046
更新日期:2005-07-01 00:00:00
abstract::The optimum strategy for heart failure (HF) treatment has yet to be elucidated. This study intended to test the benefit of a combination of valsartan (VAL) and perifosine (PER), a specific AKT inhibitor, in protecting against pressure overload induced mouse HF. Mouse were subjected to aortic banding (AB) surgery to es...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2020.04.001
更新日期:2020-07-01 00:00:00
abstract::This study examines the influence of receptor expression level on signaling pathways activated via endothelin type A receptor (ET(A)R) expressed in Chinese hamster ovary cells at 32,100 (ET(A)R-high-CHO) and 893 (ET(A)R-low-CHO) fmolmg protein(-1). Endothelin-1 (ET-1) elicited a sustained increase in intracellular Ca(...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.09233fp
更新日期:2009-12-01 00:00:00
abstract::The beneficial effects of physical activity for pain are denominated exercise-induced hypoalgesia (EIH). Here, we examined the age-related change and potential role of the neurosteroid allopregnanolone (ALLO) on EIH in rats. Adult and aged rats were randomly divided into one of three groups; non-exercise control, Low-...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2018.11.009
更新日期:2019-02-01 00:00:00
abstract::The L-type Ca(2+) channel (Ca(V)1.2) shows clear Ca(2+)-dependent facilitation and inactivation. Here we have examined the effects of calmodulin (CaM) and Ca(2+) on Ca(2+) channel in guinea-pig ventricular myocytes in the inside-out patch mode, where rundown of the channels was controlled. At a free [Ca(2+)] of 0.1 mi...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.09282fp
更新日期:2010-01-01 00:00:00
abstract::Neurosteroids are known as allosteric modulators of the ligand-gated ion channel superfamily. Voltage-gated sodium channels (Na(v)) play an important role in mediating excitotoxic damages. Here we report the effects of neurosteroids on the function of Na(v), using voltage-clamp techniques in Xenopus oocytes expressed ...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.12106sc
更新日期:2012-01-01 00:00:00
abstract::Mood disorders are not merely attributed to the functional defect of neurotransmission, but also are due to the structural impairment of neuroplasticity. Chronic stress decreases neurotrophin levels, precipitating or exacerbating depression; conversely, antidepressants increase expression of various neurotrophins (e.g...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章,评审
doi:10.1254/jphs.09r02cr
更新日期:2009-05-01 00:00:00
abstract::Secretory diarrhea is one of the most common causes of death world-wide especially in children under 5 years old. Isoliquiritigenin (ISLQ), a plant-derived chalcone, has previously been shown to exert anti-secretory action in vitro and in vivo by inhibiting CFTR Cl- channels. However, its CFTR inhibition potency is co...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2019.07.012
更新日期:2019-07-01 00:00:00
abstract::Forsythiae Fructus is known to have diuretic, anti-bacterial, and anti-inflammatory activities. This study examined the hepatoprotective effects of pinoresinol, a lignan isolated from Forsythiae Fructus, against carbon tetrachloride (CCl(4))-induced liver injury. Mice were treated intraperitoneally with vehicle or pin...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.09234fp
更新日期:2010-01-01 00:00:00
abstract::We characterized the effects of vanadate, an inhibitor of tyrosine phosphatase, on the tension, the level of myosin light chain (MLC) phosphorylation, and Rho A activation in intact ileal longitudinal smooth muscle of the guinea pig to study the role of tyrosine phosphorylation in contraction signaling. Vanadate exert...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.fp0030576
更新日期:2004-08-01 00:00:00
abstract::Lymphangiogenesis is related to the growth of endometriosis. Here, we examined whether vascular endothelial growth factor (VEGF) receptor 1 (VEGFR1) signaling plays a role in lymphangiogenesis during endometriosis. Endometrial fragments from wild-type (WT) mice transplanted into the peritoneal wall of host WT mice (WT...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2020.05.003
更新日期:2020-08-01 00:00:00
abstract::This study investigated endogenous mediators involved in mosquito allergy-associated itching in mice. An intradermal injection of an extract of mosquito salivary gland elicited marked scratching in sensitized mice. The 5-lipoxygenase inhibitor zileuton (100 mg/kg), the 5-lipoxygenase activating peptide inhibitor MK-88...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.fp0070404
更新日期:2007-09-01 00:00:00
abstract::The purpose of this study is to identify transient receptor potential canonical (TRPC) channels responsible for receptor-operated Ca(2+) entry (ROCE) triggered by activation of endothelin type A receptor (ET(A)R) and to clarify the importance of calmodulin (CaM) / inositol 1,4,5-trisphosphate (IP(3)) receptor binding ...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.11162fp
更新日期:2011-01-01 00:00:00
abstract::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 saxa...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2017.10.003
更新日期:2017-11-01 00:00:00
abstract::We have demonstrated previously that the ketamine-induced discriminative stimulus effect is likely to reflect the phencyclidine-like psychotomimetic effects. Therefore, the present study was designed to investigate the effects of the antipsychotics and 5-HT2 receptor antagonist on the discriminative stimulus effects o...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.12148sc
更新日期:2013-01-01 00:00:00
abstract::Clinically, hemorrhoidal bleeding and prolapse disappeared immediately after injection of the sclerosing agent OC-108 into submucosa of hemorrhoids. The aim of this study was to elucidate the mechanism of action responsible for the immediate hemostatic effect of OC-108 using anesthetized rats. Subcutaneous injection o...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1254/jphs.fp0060583
更新日期:2006-11-01 00:00:00
abstract::Vascular endothelial cells (VECs) secrete tissue plasminogen activator (tPA) in an active form and thus its facilitated secretion directly enhances fibrinolytic activity. We have recently demonstrated its unique secretory dynamics in GFP-tagged tPA expressing VECs using total internal reflection fluorescence microscop...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章,评审
doi:10.1254/jphs.10r23fm
更新日期:2011-01-01 00:00:00
abstract::Boron neutron capture therapy (BNCT) is a radiotherapy utilizing the neutron capture and nuclear fission reaction of 10B taken up into tumor cells. The most commonly used boron agent in BNCT, p-borono-l-phenylalanine (BPA), is accumulated in tumors by amino acid transporters upregulated in tumor cells. Here, by using ...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2019.01.012
更新日期:2019-03-01 00:00:00
abstract::Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems. The ASIC3 subtype is found primarily in the periphery where the channel mediates pain signals caused by ischemia and inflammation. He...
journal_title:Journal of pharmacological sciences
pub_type: 杂志文章
doi:10.1016/j.jphs.2017.02.007
更新日期:2017-03-01 00:00:00