Abstract：
:We investigated the mechanism of action of a novel 'high ceiling' diuretic, M17055, in in vivo clearance studies with anesthetized dogs during water diuresis and in vitro microperfusion studies of isolated rabbit renal tubules. In the clearance study, intravenous infusion of M17055 (1 mg/kg per h) decreased free water clearance and increased urinary excretion of Na+ and Cl- to a greater extent than did a maximum dose of furosemide (30 mg/kg per h). With the maximum dose of furosemide, an additional dose of M17055 or hydrochlorothiazide resulted in additional suppression of free water clearance. These results indicate that M17055 has some additional mechanisms of action in the distal nephron. In isolated rabbit cortical thick ascending limb of Henle's loop, M17055 applied to the lumen decreased the lumen positive transepithelial voltage at concentrations over 10(-6) M and suppressed the lumen-to-bath 36Cl- flux at 10(-5) M. In the connecting tubule, M17055 added to the lumen suppressed lumen negative transepithelial voltage in a concentration-dependent manner in a range from 10(-4) to 10(-3) M. The effect of M17055 on transepithelial voltage was also observed in the distal convoluted tubule and cortical collecting duct. Moreover, 10(-3) M of M17055 in the lumen significantly decreased the lumen-to-bath 22Na+ flux in the cortical collecting duct. From these observations, it appears that M17055 acts not only on the thick ascending limb of Henle's loop but also on the distal segments via inhibition of electrogenic Na+ transport.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Shinkawa T,Yamasaki F,Notsu T,Nakakuki M,Nishijima K,Yoshitomi K,Imai Mdoi
10.1016/0014-2999(93)90863-dsubject
Has Abstractpub_date
1993-07-20 00:00:00pages
317-25issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(93)90863-Djournal_volume
238pub_type
杂志文章abstract：:Overexpression of Cav3.2 T-type Ca2+ channels in L4 dorsal root ganglion (DRG) participates in neuropathic pain after L5 spinal nerve cutting (L5SNC) in rats. The L5SNC-induced neuropathic pain also involves high mobility group box 1 (HMGB1), a damage-associated molecular pattern protein, and its target, the receptor ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173587
更新日期：2020-12-05 00:00:00
abstract：:We examined the feasibility of coupling the 5-HT(6) receptor to a Ca(2+) signaling read-out using a chimeric G-protein, comprising of G(alphaq) with the C-terminal five amino acids from G(alphas), to facilitate assays on the fluorometric imaging plate reader (FLIPR). Using a transient transfection assay in human embry...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01855-7
更新日期：2003-07-04 00:00:00
abstract：:Clinical use of gentamicin over prolonged periods is limited because of dose- and time-dependent nephrotoxicity. Primarily, lysosomal phospholipidosis, intracellular oxidative stress and heightened inflammation have been implicated. Hydrogen sulphide is an endogenously produced signal transduction molecule with strong...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.04.030
更新日期：2012-06-15 00:00:00
abstract：:Dinitrosyl iron complexes (DNIC) with glutathione exert a cytotoxic effect on endometrioid tumours in rats with surgically induced experimental endometriosis. Intraperitoneal treatment of rats (Group 1) with DNIC (12.5μmoles/kg, daily, for 12 days), beginning with day 4 after the surgical operation (implantation of tw...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.002
更新日期：2014-03-15 00:00:00
abstract：:Terfenadine and astemizole rarely cause cardiac arrhythmias by suppressing the cardiac rapid delayed rectifier K+ channel encoded by the human ether-a-go-go-related gene (HERG). Epinastine, however, has not been reported to have the adverse effect. We have therefore compared the effects of epinastine, terfenadine and ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00375-1
更新日期：1999-06-25 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90484-8
更新日期：1991-04-03 00:00:00
abstract：:Platelet aggregation induced in mice or rats by i.v. ADP can be antagonized by oral administration of suloctidil. This effect on platelet behaviour appears to be sufficient to reduce the rate of thrombotic occlusion of the femoral artery in the dog and to protect the rat against occurrence of thrombophlebitis. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90034-0
更新日期：1976-06-01 00:00:00
abstract：:Rolipram was characterized for its emetic, behavioral, cardiovascular and pulmonary activities in dogs, to assess its systemic pharmacology and potential bronchodilatory selectivity. At doses > or = 0.1 mg/kg i.v., rolipram induced emesis, anxiety, and stepping behaviors in conscious dogs, and increased heart rate and...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00457-2
更新日期：1995-11-24 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)02001-6
更新日期：2003-07-25 00:00:00
abstract：:Kinin B1 receptors on rabbit aorta smooth muscle cells in culture were investigated. [3H]Des-Arg10-kallidin labeled a single site in cells at early passage with an equilibrium dissociation constant of 258 pM and a maximal binding density of approximately 680 sites/cell. Treatment of the same cells for 18 h with epider...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90137-6
更新日期：1994-02-15 00:00:00
abstract：:The purpose of the present study was to investigate the effects of reactive oxygen species on the activity of epithelium-derived relaxant factor (EpDRF) released by guinea-pig tracheal epithelium. Reactive oxygen species were generated by the electrolysis of the physiological buffer in which the tissues were bathed. E...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00390-8
更新日期：1999-07-28 00:00:00
abstract：:S 38093, a novel histamine H3 receptor inverse agonist, was tested in a series of neurochemical and behavioral paradigms designed to evaluate its procognitive and arousal properties. In intracerebral microdialysis studies performed in rats, S 38093 dose-dependently increased histamine extracellular levels in the prefr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.03.008
更新日期：2017-05-15 00:00:00
abstract：:Cells exposed to ionizing radiation show DNA damage, apoptosis, chromosomal aberrations or increased mutation frequency and for a long time it was generally accepted that these effects resulted from ionization of cell structures and the action of reactive oxygen species formed by water radiolysis. In the last few year...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.07.028
更新日期：2009-12-25 00:00:00
abstract：:Phencyclidine (PCP) is widely used as an animal model of schizophrenia. In rats, acute PCP treatment increased locomotor activity and induced stereotyped behaviours consisting of head weaving, turning and backpedalling. PCP had differential regional effects on c-fos expression in rat brain, suggesting different patter...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00830-x
更新日期：2000-12-01 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.02.031
更新日期：2008-06-10 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01474-1
更新日期：2001-12-07 00:00:00
abstract：:To investigate cellular electrophysiologic alterations due to lipid peroxidation of the cell membrane by free radicals as a possible cause of coronary reperfusion arrhythmias, we studied the effects of t-butyl hydroperoxide on the spontaneous action potential and membrane currents of the rabbit sinoatrial and atrioven...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)90027-6
更新日期：1995-03-16 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172496
更新日期：2019-09-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.09.070
更新日期：2010-01-10 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(92)90016-6
更新日期：1992-09-01 00:00:00
abstract：:Quantitative characterization of the kappa opioid receptor in the rabbit ear artery was carried out using three kappa-selective agonist compounds, dynorphin-(1-13), U-69593 and ethylketocyclazocine. Kinetic analysis was performed using the antagonist, MR 2266. Two other in vitro preparations were studied for compariso...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90542-0
更新日期：1988-07-14 00:00:00
abstract：:The effects of trichokonin VI (= gliodeliquescin A), a peptaibol isolated from the culture broth of Trichoderma koningii Oudemans, on L-type Ca2+ channel currents in single bullfrog atrial cells were investigated. Our results showed that trichokonin VI is a new potent agonist of L-type Ca2+ channels in cardiac membran...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90290-9
更新日期：1994-12-12 00:00:00
abstract：:The binding of tritium-labelled BIBP3226, N2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]-D-arginine amide, to human neuroblastoma SK-N-MC cells was investigated. [3H]BIBP3226 reversibly binds to neuropeptide Y receptors of the Y1 subtype expressed in SK-N-MC cells with a KD of 2.1 +/- 0.3 nM (mean +/- S.E.M., n = 3)...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00161-d
更新日期：1995-05-24 00:00:00
abstract：:The effects of a single dose of naloxone and of [D-Met2,Pro5]enkephalinamide on the DNA synthesis in the uterus of 7, 14 and 21-day-old rat were studied. After [D-Met2,Pro5]enkephalinamide treatment, an age-dependent decrease in in vitro [3H]thymidine incorporation into DNA was observed in all studied age groups. In t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(95)90132-9
更新日期：1995-10-15 00:00:00
abstract：:Observations of sigma (sigma) receptor heterogeneity have prompted interest in identifying ligands for sigma receptor subtypes. Selective ligands for the sigma-2 are unavailable, but [3H]ifenprodil labels sigma-2 sites. Therefore, isomers and analogues of ifenprodil were compared as potential sigma-2 ligands. Threo-if...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)00763-w
更新日期：1995-02-06 00:00:00
abstract：:In the presence of RS-15385-197 to preclude binding to alpha 2-adrenoceptors, [3H]p-aminoclonidine labelled a low affinity high capacity site, (Kd = 127.6 +/- 19.7 nM, Bmax 978 +/- 172 fmol/mg protein) whereas [3H]idazoxan labelled a high affinity low capacity site (Kd = 1.66 +/- 0.28 nM, Bmax 45.3 +/- 11.4 fmol/mg pr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90731-v
更新日期：1993-02-23 00:00:00
abstract：:The i.c.v. administration of 0.5 microgram pertussis toxin to mice led to a non-competitive reduction (approximately 60 to 70%) of the supraspinal analgesia evoked by i.c.v. injection of ED90 doses of [D-Ala2,N-MePhe4,Gly-ol5]enkephalin, [D-Ala2,N-MePhe4,Met-(O)5-ol]enkephalin, [D-Ala2,Met5]enkephalinamide, [D-Ala2,D-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90732-7
更新日期：1988-08-02 00:00:00
abstract：:The vasodilatory role of calcitonin gene-related peptide in activating K+ channels was examined in isolated, suffused human uterine arteries. Calcitonin gene-related peptide produced a concentration-dependent relaxation of norepinephrine (1 microM)-induced contractions. Calcitonin gene-related peptide was antagonized ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90249-h
更新日期：1993-10-05 00:00:00
abstract：:5-methoxy-N,N-dimethyltryptamine (5-MeODMT) produced a dose-dependent decrease in the discharge rate of serotonin-containing neurons in the dorsal raphe nucleus of freely moving cats. This ranged from a 15% decrease at 10 microgran/kg, i.m., to a virtual complete depression of activity at 250 microgram/kg. 5-MeODMT's ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90406-0
更新日期：1979-02-15 00:00:00
abstract：:The effects of intra- and extraluminal capsaicin administration were evaluated in isolated perfused rat mesenteric bed. Capsaicin (10 nM-1 microM) produced a potent concentration-dependent relaxation of the tonic vasoconstriction induced by norepinephrine (1 microM) but not by high-K+ (60 mM). The capsaicin-induced re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90559-6
更新日期：1988-03-29 00:00:00
