Abstract:
:U-54494A, a 1,2-diamine anticonvulsant, and U-50488H, a structurally related agonist for opiate kappa receptors, were tested for effects on spontaneous and glutamate-evoked firing rates in cerebral cortex of urethane-anesthetized male Sprague-Dawley rats. Iontophoretic application of 1,2-diamines, glutamate diethyl ether (GDEE), or procaine depressed spontaneous and amino acid-induced firing of cortical neurones. With continued ejection of 1,2-diamines or procaine, firing was silenced completely, but GDEE could maintain a partial suppression. A rapid rebound of excitation followed cessation of procaine ejections, but not of other agents. Procaine, but not U-54494A, blocked axonal conduction of rabbit sciatic nerve. Intravenous U-54494A and U-50488H significantly depressed spontaneous firing rates of cortical neurones, but only the U-50488H effects were antagonized by naloxone. It is concluded that U-54494A inhibits neuronal excitability by a mechanism independent of the analgesic kappa receptor. Biochemical and physiological studies have demonstrated that U-54494A and the kappa opioid agonist U-50488H (a structurally related diamine) (1) have anticonvulsant activity (2, 3). U-54494A lacks kappa analgesic and sedative properties, and it has been suggested that the mechanism of action of this compound may be mediated by a subtype of kappa opioid receptor (3). The effects of kappa analgesics on neuronal firing in nociceptive pathways have been described (4, 5). However, no previous electrophysiological studies on U-54494A have been done. Since U-54494A antagonizes amino acid-induced seizures (3), the interactions of this compound with glutamate are of interest. In the present study, the antagonist efficacies of U-54494A and U-50488H for inhibiting spontaneous and 1-glutamate stimulated neurons of the rat prefrontal cerebral cortex were assessed after i.v. and microiontophoretic administration of the compounds. Effects observed with these routes of administration allow the observation of neuronal changes occurring immediately after administration and take advantage of the high temporal resolution provided by the electrophysiological recording techniques of single cells. A preliminary account of portions of this work have been previously disclosed (6).
journal_name
Life Scijournal_title
Life sciencesauthors
Ochoa MC,Vogelsang GD,Lum JT,VonVoigtlander PF,Piercey MFdoi
10.1016/0024-3205(92)90322-gsubject
Has Abstractpub_date
1992-01-01 00:00:00pages
1225-33issue
17eissn
0024-3205issn
1879-0631pii
0024-3205(92)90322-Gjournal_volume
50pub_type
杂志文章相关文献
LIFE SCIENCES文献大全abstract::To understand whether chronic inflammation alters the development of morphine tolerance, the tail-flick test was used to evaluate the analgesic effect of morphine (75 mg tablet, s.c.) in the arthritic rats at the day 9-12 after the inoculation with Freund's adjuvant. Spinal cord monoamines and amino acid neurotransmit...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(99)00008-9
更新日期:1999-01-01 00:00:00
abstract::Voltage clamp recordings of GH3/B6 pituitary cells reveal the presence of non linear steady state membrane properties at the level of the resting potential (about -41 mV). Clamping the cells to potentials more depolarized than -60 mV is associated with a potential dependent increase in membrane conductance and membran...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(82)90475-1
更新日期:1982-05-31 00:00:00
abstract::From the fruiting bodies of the edible mushroom Flammulina velutipes a single-chained ribosome inactivating protein with a molecular weight of 13.8 kDa was isolated with a procedure involving ion exchange chromatography on DEAE-cellulose and SP-Sepharose and affinity chromatography on Affi-gel blue gel. The protein wa...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(01)01023-2
更新日期:2001-03-23 00:00:00
abstract::The human placental villus tissue contains opioid receptors and peptides. The opioid peptides extracted from the villus tissue were fractionated using reverse-phase high performance liquid chromatography and a radio-receptor assay. The presence of dynorphin 1-8 was corroborated by mass spectrometric production of (M +...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(87)90099-3
更新日期:1987-05-25 00:00:00
abstract::The ontogenetic development of [3H]-spiroperidol binding sites was measured in the optic tectum, cerebellum, forebrain base, and forebrain roof of 1-, 4-, and 16-day-old chicks. In the chick optic tectum and cerebellum both the density and the total number of [3H]-spiroperidol binding sites increased from 4- to 16-day...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(89)90331-7
更新日期:1989-01-01 00:00:00
abstract:AIMS:Endothelial microparticles (EMPs) are extracellular vesicles secreted by endothelial cells. The purpose of this research is to explore that the clinical significance and roles in angiogenesis and endothelial dysfunction of circulating microparticles in Perthes disease. MAIN METHODS:We collected platelet-poor plas...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2020.118749
更新日期:2021-01-15 00:00:00
abstract::Diabetic retinopathy, a common secondary complication of diabetes mellitus, involves extensive damage to the retinal microvasculature. Retina, being a susceptible target, is highly prone to hyperglycemia-induced molecular damages. PPAR receptor, chiefly gamma subtype, mediates numerous responses related to glucose met...
journal_title:Life sciences
pub_type: 杂志文章,评审
doi:10.1016/j.lfs.2016.03.054
更新日期:2016-05-15 00:00:00
abstract:AIM:Nontuberculous mycobacterial (NTM) infection such as endophthalmitis, dacryocystitis, and canaliculitis are pervasive across the globe and are currently managed by antibiotics. However, the recent cases of Mycobacteroides developing drug resistance reported along with the improper practice of medicine intrigued us ...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2020.117541
更新日期:2020-06-01 00:00:00
abstract::According to recent epidemiological reports, almost 40% of American population use complimentary and alternative medicine (CAM) during their lifetime. Patients detected with HIV or cancer often consume herbal products especially St. John's wort (SJW) for antidepressants in combination with prescription medicines. Such...
journal_title:Life sciences
pub_type: 杂志文章,评审
doi:10.1016/j.lfs.2005.12.010
更新日期:2006-03-27 00:00:00
abstract::The effects of 14-day physical exercise or iloprost treatment (0.5-2 ng/Kg/min) on endogenous nitric oxide production and neutrophil adhesion were evaluated in 20 patients with peripheral arterial occlusive disease (Fontaine Stage II). Peripheral venous blood samples and 4-h urine samples were collected before, immedi...
journal_title:Life sciences
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0024-3205(99)00550-0
更新日期:1999-01-01 00:00:00
abstract::We have investigated the antidiabetic activity of luteolin 5-rutinoside in streptozotocin(STZ)-induced diabetic rats. Treatment for 20 days with 2 mg/kg increased both pancreatic insulin and DNA content. When both luteolin 5-rutinoside (2 mg/kg) and glibenclamide (1 mg/kg) were administered concurrently to STZ-diabeti...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(96)00231-7
更新日期:1996-01-01 00:00:00
abstract::This study examined whether there is increased production of oxygen free radicals during chronic renal failure. Rats subjected to 3/4 nephrectomy and sham operated controls were killed after 3 weeks. Lipid extracts of plasma and renal tissue were examined by HPLC and kidney specimens were also analyzed by EPR spectros...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(92)90548-4
更新日期:1992-01-01 00:00:00
abstract::By using multiple time-point constant-rate infusions of deuterium-labeled phosphorylcholine, appropriate kinetic parameters were obtained for use in the calculation of the turnover rate of acetylcholine (TRACh) in selected mouse brain regions. After obtaining these data, the relationship between the analgesic agent co...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(92)90499-f
更新日期:1992-01-01 00:00:00
abstract::Obesity leads to various changes in the body. Among them, the existing inflammatory process may lead to an increase in the production of reactive oxygen species (ROS) and cause oxidative stress. Oxidative stress, in turn, can trigger mitochondrial changes, which is called mitochondrial dysfunction. Moreover, excess nu...
journal_title:Life sciences
pub_type: 杂志文章,评审
doi:10.1016/j.lfs.2017.11.019
更新日期:2018-01-01 00:00:00
abstract::The mechanism by which benzoate enhances total nitrogen excretion was investigated in-situ and in separated rat renal proximal tubules. Orally administered benzoate augmented NH4+, urea and hippurate excretion 2, 1.9 and 76 fold respectively, as compared to baseline for control. Hippurate had similar effects. Benzoate...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(91)90086-q
更新日期:1991-01-01 00:00:00
abstract:AIMS:Schisandra is a good choice in Traditional Chinese Medicine for the therapy of cardiovascular diseases, but whether it contains a or some specific component (s) responsible these effects are still unclear. In the present study, we explored whether Schisantherin A (SCA) causes vasorelaxation in isolated rat thoraci...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2020.117357
更新日期:2020-03-15 00:00:00
abstract::Maternal malnutrition is known to impair fetal growth and predispose to the development of hypertension and type 2 diabetes. Recently, studies have demonstrated that intrauterine malnutrition is followed later in male offspring by oxidative stress characterized by increased superoxide generation due to activation of N...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2006.10.028
更新日期:2007-01-30 00:00:00
abstract:BACKGROUND:Cisplatin resistance has been found to contribute to the failure of ovarian carcinoma treatment. Oridonin is a natural en-kaurane tetracyclic diterpenoid compound discovered in Rabdosia rubescene (Henmsl.) Hara. Herein, we tested whether oridonin could exert chemo-sensitization activity on cisplatin-resistan...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2019.116709
更新日期:2019-09-15 00:00:00
abstract::Besides an isomer of the cardenolide ouabain, a material with a similar HPLC retention time as ouabain but cross-reactivating with antibodies against the bufadienolide proscillaridin A and inhibiting the sodium pump is known to circulate in human blood plasma (B. SICH et al., Hypertension 27, 1073-1078 (1996).). The c...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(98)00023-x
更新日期:1998-01-01 00:00:00
abstract:UNLABELLED:The present study was conducted to examine whether melatonin impairs serotonin (5HT) release and uptake in rat platelets. Exposure of platelet-rich plasma samples (PRP) to melatonin induced a concentration-dependent inhibition of 5HT uptake and the value of IC50 was 1.3 x 10(-3) M. We have also investigated ...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(93)90261-z
更新日期:1993-01-01 00:00:00
abstract::Gestational exposure to nicotine has been shown to affect development of noradrenergic activity in both the central and peripheral nervous systems. In the current study, pregnant rats received nicotine infusions of 6 mg/kg/day throughout gestation, administered by osmotic minipump implants. After birth, offspring of t...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(90)90185-t
更新日期:1990-01-01 00:00:00
abstract::The effect of diabetes mellitus on serum cholesterol and aortic microsomal prostanoid synthesis was studied in cholesterol fed male Lewis rats. Normal, diabetic and diabetic rats treated with pancreatic islets were divided into three diet subgroups, control diet, control +2% cholesterol for 8 weeks and control +2% cho...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(90)90620-7
更新日期:1990-01-01 00:00:00
abstract::Morning urine samples were assayed for human EGF (hEGF) in 137 non-insulin dependent diabetic patients with normal serum creatinine and beta 2-microglobulin levels. Serving as controls, 80 age- and sex-matched healthy subjects were also examined. A significant positive correlation between hEGF excretion and the level ...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(93)90100-h
更新日期:1993-01-01 00:00:00
abstract::Daily s.c. injection of (-)deprenyl (2.0 mg/kg/day) for three weeks in young male rats caused a threefold increase in superoxide dismutase (SOD) activity in the striatum of the brain compared with the value in saline-injected control rats. Furthermore, the activity of catalase (but not of glutathione peroxidase) was a...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(91)90466-o
更新日期:1991-01-01 00:00:00
abstract::The human eye being a complex and a very sensitive organ makes the drug delivery task challenging. An increase in the intra-ocular pressure at the aqueous humour leads to glaucoma which is not only indecipherable but can also be the reason of blindness for many. The presently available marketed formulations using anti...
journal_title:Life sciences
pub_type: 杂志文章,评审
doi:10.1016/j.lfs.2019.02.029
更新日期:2019-03-15 00:00:00
abstract::Endogenous levels of salsolinol and dopamine were measured by a gas chromatography/mass spectrometry (GC/MS) - selected ion monitoring technique using deuterated internal standards in Long Evans rats chronically exposed to ethanol for ten months. Chronic ethanol exposure produced significant increases of dopamine and ...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(85)90115-8
更新日期:1985-01-28 00:00:00
abstract::The binding of the D2-like agonists, (+)-7-hydroxy-N,N-di-n-[3H]propyl-2-aminotetralin (7-OH-DPAT) and [3H]pramipexole (2-amino-4,5,6-tetrahydro-6-propylaminobenzthiazole; MIRAPEX) were determined in membranes from adult male Sprague-Dawley and Fischer-344 rats. Saturation analysis, which optimized binding to D3 recep...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(98)00446-9
更新日期:1998-01-01 00:00:00
abstract::Alpha adrenergic agonists and antagonists as clonidine, guanfacine, yohimbine, phenylephrine and prazosin inhibited the [3H]-QNB binding to rat brain cortex muscarinic acetylcholine receptor (mAChR, M-1 subtype), heart (M-2 subtype) and parotid gland homogenate (M-3 subtype) in a dose-dependent competitive fashion. Ki...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(90)90436-u
更新日期:1990-01-01 00:00:00
abstract::The rate of oxidation of sparteine by the 9000 x g supernatant fraction of a human liver was measured in the presence of various drugs which exert cardiovascular effects. Hexamethonium, ouabain, caffeine and isoproterenol had no effect on this rate, while alprenolol, metoprolol, oxprenolol, propranolol, timolol, pindo...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(84)90332-1
更新日期:1984-01-02 00:00:00
abstract::The present investigation was aimed at comparing the influence of the partial dopamine (DA) receptor agonist (-)-3-PPP (preclamol) on prolactin release in acutely hyperprolactinemic but otherwise intact female rats and female rats subjected to chronic DA depletion. One group of animals received daily vehicle injection...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(88)90100-2
更新日期:1988-01-01 00:00:00