Abstract：
:Even though conventional systemic doses of cimetidine and other histamine H(2) antagonists display minimal brain penetration, central nervous system (CNS) effects (including seizures and analgesia) have been reported after administration of these drugs in animals and man. To test the hypothesis that cimetidine-like drugs produce these CNS effects via inhibition of GABA(A) receptors, the actions of these drugs were studied on seven different, precisely-defined rat recombinant GABA(A) receptors using whole-cell patch clamp recordings. The H(2) antagonists famotidine and tiotidine produced competitive and reversible inhibition of GABA-evoked currents in HEK293 cells transfected with various GABA(A) receptor subunits (IC(50) values were between 10-50 microM). In contrast, the H(2) antagonist ranitidine and the cimetidine congener improgan had very weak (if any) effects (IC(50) > 50 microM). Since the concentrations of cimetidine-like drugs required to inhibit GABA(A) receptors in vitro (greater than 50 microM) are considerably higher than those found during analgesia and/or seizures (1-2 microM), the present results suggest that cimetidine-like drugs do not appear to produce seizures or analgesia by directly inhibiting GABA(A) receptors.
journal_name
Life Scijournal_title
Life sciencesauthors
Cannon KE,Fleck MW,Hough LBdoi
10.1016/j.lfs.2004.05.020subject
Has Abstractpub_date
2004-10-08 00:00:00pages
2551-8issue
21eissn
0024-3205issn
1879-0631pii
S0024-3205(04)00661-7journal_volume
75pub_type
杂志文章相关文献
LIFE SCIENCES文献大全abstract：:Aim Determine changes in the expressions of the ion channel-TRPV1-and neuropeptides-NKA, NKB, calcitonin gene-related peptide (CGRP), and SP-in 14-, 21-, and 42-day-old rats after inhaling 1.5% and 2.6% sevoflurane. MAIN METHODS:A small in-house inhalation anesthesia chamber was designed to allow 14-, 21-, and 42-day...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.117472
更新日期：2020-05-15 00:00:00
abstract：AIMS:The beneficial effects of cannabinoid type 2 receptor (CB2R) activation have been verified in various tissue repair processes. Our recent study revealed CB2R activation promotes myogenesis partly through Nrf2 signaling in a mouse skeletal muscle ischemia-reperfusion (IR) injury model. Other relevant mechanisms nee...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.117989
更新日期：2020-09-01 00:00:00
abstract：:Benzamide riboside (BR) is a novel anticancer agent exhibiting pronounced activity against several human tumor cell lines via the inhibition of inosine 5'-monophosphate dehydrogenase (IMPDH), thereby restricting the biosynthesis of guanylates. Although it has been demonstrated that BR inhibits IMPDH and induces apopto...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2003.11.026
更新日期：2004-05-28 00:00:00
abstract：:Obesity, the metabolic syndrome (MetS), and type 2 diabetes (T2DM) are associated with heightened cardiovascular risk. Given the vasoconstrictor and proatherogenic properties of endothelin (ET)-1, increased ET-1 activity has been postulated to participate in the derangement of adiposity-related vascular homeostasis. T...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2014.02.028
更新日期：2014-11-24 00:00:00
abstract：:We have determined the effects of chronic exposure to the protein kinase C (PKC) activating drug 4-beta phorbol 12-myristate-13-acetate (PMA) on PKC isozymes and the rate of spontaneous contraction in neonatal rat cardiac myocytes in culture. Western blot analyses revealed that a two day exposure to 0.1-1 nM PMA incre...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(95)02048-n
更新日期：1995-01-01 00:00:00
abstract：:The ontogeny of endothelin (ET) system in rats was studied in preterm (18 days of gestation), term (21 days of gestation) and 1 week post term rats. Brains were dissected out and (1) processed for the estimation of endogenous ET-1 by RIA and (2) membranes were prepared for radioreceptor binding. Receptor characteristi...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(92)90300-e
更新日期：1992-01-01 00:00:00
abstract：:Male and female rats with two permanently indwelling intravenous catheters were infused for 2 hours with ovine prolactin. During equilibrium conditions the effects of intravenously injected L-DOPA and benzerazide (a blocker of dopa-decarboxylase) on steady state levels of ovine prolactin were measured. A dose of 4.5 m...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(82)90549-5
更新日期：1982-08-30 00:00:00
abstract：:Sphinganine (SP) pre-treatment potentiated the retinoic acid (RA)-induced (4-96h exposures) differentiation and increase of alkaline phosphatase (ALP) activity. A higher percentage of SP pre-treated cells in RA exposures resembled mature myelocytes or granulocytes; greater increase in ALP activity was observed. In cel...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(93)90688-y
更新日期：1993-01-01 00:00:00
abstract：:DNA is considered to be one of the most promising targets for anticancer agents. Acridine analogues have anticancer activity based on DNA binding and topoisomerases inhibition. However, due to the side effects, resistance and low bioavailability, a few have entered into clinical usage and the mechanisms of action are ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2018.05.010
更新日期：2018-08-01 00:00:00
abstract：:Chlordimeform (CDM) and demethylchloridimeform (DCDM) mimic the action of octopamine in elevating adenylate cyclase activity in intact nerve cords of the American cockroach, Periplaneta americana. At a concentration of 1 x 10(-5)M, DCDM (13.5x increase within 20 minutes) is a more potent effector of the response than ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90644-6
更新日期：1983-06-27 00:00:00
abstract：:Urine flow, osmolality, concentrations of sodium and potassium were measured every 10 min for 24 hours in 6 female dogs, whose sleep-wake stages were monitored electrographically. Experiments were conducted under hydration and progressive dehydration conditions. Visual examination and spectral analysis revealed signif...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(82)90718-4
更新日期：1982-12-13 00:00:00
abstract：:Using hot plate method, analgesia induced by noncatecholic phenylethylamines, phenethylamine, phenylethanolamine and amphetamine, was inhibited by naloxone, reserpine, apomorphine and p-chlorophenylalanine, while potentiated by haloperidol. These results suggest that phenylethylamines induced analgesia involves centra...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(82)90347-2
更新日期：1982-09-20 00:00:00
abstract：AIMS:Active immunization with human vascular endothelial growth factor (hVEGF) vaccines provides a therapeutic option instead of bevacizumab therapy. However, the immunity to self-molecule is difficult to elicit due to immune tolerance. A bioactive peptide of two tandem repeats of mHSP70407-426 (M2) has exhibited poten...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2018.03.039
更新日期：2018-05-15 00:00:00
abstract：:Rats were administered intravenously liposome-encapsulated or free cobalt, and the organ distribution of the metal was explored using Co57 tracer. Two hours after administration, the cobalt level in the heart was about 40% of the control when given in sphingomyelin (SM)/cholesterol (CH) (1:1 mole ratio) liposomes. The...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(89)90092-1
更新日期：1989-01-01 00:00:00
abstract：AIM:Pancreatic stellate cells (PSCs) are the main functional cells leading to pancreatic fibrosis. Nicotine is widely considered as an independent risk factor of pancreatic fibrosis, but the mechanism is still unclear. Our study was aimed to explore the effects of nicotine on human pancreatic stellate cells (hPSCs) and...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.117301
更新日期：2020-02-15 00:00:00
abstract：:The antioxidative and superoxide- and hydroxyl radical-scavenging activities and pro-oxidant effect of twelve selected medicinal herbs were studied. The aqueous extracts of Coptis chinensis, Paeonia suffruticosa, Prunella vulgaris and Senecio scandens exhibited the highest potency in inhibiting rat erythrocyte hemolys...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(99)00643-8
更新日期：2000-01-14 00:00:00
abstract：:The dramatic activities of bradykinin and related peptides as mediators of pain, inflammation and hypotension have been intensely studied for several decades. More recently, the involvement of bradykinin in regulation of ion transport by epithelia, hormone release from endocrine organs, energy metabolism, tissue growt...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/0024-3205(92)90201-y
更新日期：1992-01-01 00:00:00
abstract：:The effects of t-butylhydroperoxide (TBH) and cigarette smoke on lung mechanics (CDYN and RL) and glutathione status (GSH) were studied using an isolated perfused and ventilated rat lung preparation. TBH (200, 400, 1000 microM) infused via the pulmonary circulation caused a dose-related bronchoconstriction. The lung G...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(88)90054-9
更新日期：1988-01-01 00:00:00
abstract：AIMS:Fructose administration induces hepatic oxidative stress, insulin resistance, inflammatory and metabolic changes. We tested their potential pathogenic relationship and whether these alterations can be prevented by R/S-α-lipoic acid. MAIN METHODS:Wistar rats received during 21days a commercial diet or the same die...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2015.07.010
更新日期：2015-09-15 00:00:00
abstract：:Autophagy is an essential mechanism of cellular degradation, a way to protect the cells under stress conditions, such as deprivation of nutrients, growth factors and cellular damage. However, in normal physiology autophagy plays a significant role in cancer cells. Current research is in progress to understand how auto...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2020.118184
更新日期：2020-10-15 00:00:00
abstract：:Increased oxidative stress and antioxidant deficit have been suggested to play a major role in adriamycin induced cardiomyopathy and congestive heart failure due to multiple treatments with adriamycin. In this study the cardio protective effect of Centella asiatica on myocardial marker enzymes and antioxidant enzymes ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2004.09.009
更新日期：2004-12-17 00:00:00
abstract：AIMS:The roles of miR-141 in various types of cancers and inflammatory bowel diseases are researched, whereas, little information about its function in lung inflammation is available. This study was designed to explore the effect of miR-141 on inflammation injury in WI-38 cells, possibly providing basis for targeted th...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2018.11.056
更新日期：2019-01-01 00:00:00
abstract：:The objective of the present study was to investigate the roles of protein kinase A and/or C in agonist-induced beta adrenoceptor activation in intact human lymphocytes. LYmphocytes from healthy subjects were incubated with isoproterenol and phosphodiesterase inhibitor (IBMX, 1.0 mM) after 20 minutes of preincubation ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(90)90584-e
更新日期：1990-01-01 00:00:00
abstract：BACKGROUND:Cigarette smoke extract (CSE) affects the expression of non-neuronal components of cholinergic system in bronchial epithelial cells and, as PEBP1/Raf-mediated MAPK1/2 and ERK1/2 pathway, promotes inflammation and oxidative stress. AIMS:We studied whether Acetylcholine (ACh) is involved in the mechanism of c...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2017.11.034
更新日期：2018-01-01 00:00:00
abstract：AIMS:Diabetic nephropathy is a growing health concern, which is reported to be associated with inflammation. Luteolin has been explored for the treatment of some diabetic complications. Although several studies have verified the effect of luteolin on diabetic nephropathy, the mechanism by which the therapeutic effects ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2019.03.073
更新日期：2019-05-15 00:00:00
abstract：:Endogenous dopamine (DA) and norepinephrine (NE) in the superfusate from slices of rat medial prefrontal cortex were measured by high-performance liquid chromatography coupled to electrochemical detection (HPLC-ECD). Stimulation with high K+ or methamphetamine (MAP) evoked a dose-dependent elevation in the release of ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(91)90356-g
更新日期：1991-01-01 00:00:00
abstract：:According to our previously proposed auto-addiction hypothesis of chronic anorexia nervosa, patients become addicted to an initial period of dieting through endogenous opioid mediated mechanisms. Morphine causes hyperactivity and anorexia in the mouse, symptoms of anorexia nervosa but responses opposite to those of mo...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(87)90457-7
更新日期：1987-08-10 00:00:00
abstract：AIMS:Antitumour effects of pentapeptide (LH) derived from donkey serum albumin hydrolysates were tested against tumour cells both in vitro and in vivo. The mechanism of LH induced tumour cell apoptosis was investigated. MAIN METHODS:Human promyelocytic leukaemia cells (HL 60) were cultured to observe inhibition in vit...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2013.02.013
更新日期：2013-05-20 00:00:00
abstract：:Recent studies suggest that the time of day at which food is consumed dramatically influences clinically-relevant cardiometabolic parameters (e.g., adiposity, insulin sensitivity, and cardiac function). Meal feeding benefits may be the result of daily periods of feeding and/or fasting, highlighting the need for improv...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2018.01.031
更新日期：2018-03-15 00:00:00
abstract：:In order to clarify the role played by interleukin-2 (IL-2) in the regulation of fibroblast function, we investigated the effect of rat IL-2 and human recombinant IL-2 on 3T3 fibroblast proliferation and collagen synthesis. Fibroblasts were incubated with various concentrations of IL-2 for different periods of time. I...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(96)00125-7
更新日期：1996-01-01 00:00:00
