Abstract:
:The cannabinoid 1 receptor antagonist AM 251 is known to block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. We examined the ability of AM 251 to inhibit sodium channel-dependent functions and the binding of [3H]batrachotoxinin A 20-alpha-benzoate to sodium channels in mouse brain synaptic preparations. Depolarization of synaptoneurosomes by the sodium channel site 2-specific neurotoxin veratridine, which is abolished by tetrodotoxin, was found to be inhibited in a concentration-dependent fashion by AM 251 (IC50=8.9 microM). Veratridine-dependent (tetrodotoxin suppressible) release, of L-glutamic acid and GABA from synaptosomes was also reduced by AM 251 [IC50s=8.5 microM (L-glutamic acid), 9.2 microM (GABA)]. The binding of the radioligand [3H]batrachotoxinin A 20-alpha-benzoate to site 2 on sodium channels was displaced by AM 251 (IC50=11.2 microM). Scatchard analysis of binding showed that at its IC50, AM 251 increased (by 2.3 times) the KD of radioligand without altering Bmax, suggesting a competitive mechanism of inhibition by AM 251. Kinetic experiments indicated that AM 251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex. Our data suggest that micromolar concentrations of AM 251 are capable of reducing neuronal excitability and inhibiting release of excitatory and inhibitory transmitters through blockade of voltage-sensitive sodium channels in brain.
journal_name
Basic Clin Pharmacol Toxicoljournal_title
Basic & clinical pharmacology & toxicologyauthors
Liao C,Zheng J,David LS,Nicholson RAdoi
10.1111/j.1742-7843.2004.pto940204.xsubject
Has Abstractpub_date
2004-02-01 00:00:00pages
73-8issue
2eissn
1742-7835issn
1742-7843journal_volume
94pub_type
杂志文章abstract::Upper gastrointestinal bleeding is a feared complication of using non-steroidal anti-inflammatory drugs (NSAIDs) or aspirin. Studies predicting the incidence rate for individuals with a given set of characteristics are lacking. The aim of this study was to develop a risk model to predict the incidence rate of upper ga...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.13370
更新日期:2020-05-01 00:00:00
abstract::Mildronate is a cardioprotective drug that improves cardiac function during ischaemia and functions by lowering l-carnitine concentration in body tissues and modulating myocardial energy metabolism. The aim of the present study was to characterise cardiovascular function and liver condition after long-term mildronate ...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2009.00461.x
更新日期:2009-12-01 00:00:00
abstract::The aim of the present study was to examine the effects of formaldehyde solution on rat left ventricular function and compare it with those in hypertrophic hearts treated with isoproterenol by pressure-volume measurements with the catheter method. After 20-30 min. of intravenous infusion of 3.7% formaldehyde solution ...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2009.00442.x
更新日期:2009-10-01 00:00:00
abstract:BACKGROUND:It is well known that antibiotic use is the main driver for the increasing problems with resistant bacteria. Consequently, some countries have recommended shortening the duration of antibiotic treatment of community-acquired pneumonia (CAP). The aim of this study was to investigate whether the effectiveness ...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,评审
doi:10.1111/bcpt.13205
更新日期:2019-05-01 00:00:00
abstract::High-dose cyclophosphamide (HD-CTX) treatment often leads to severe nephrotoxicity and neurotoxicity, which are mainly caused by one of its metabolites, chloroacetaldehyde (CAA). However, there are no effective antidotes to prevent these side effects. The objective of this study was to evaluate the effect of Wuzhi Cap...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.13211
更新日期:2019-08-01 00:00:00
abstract::Gambogic acid, the main active compound of gamboge resin of Garcinia hanburryi, has recently exhibited marked antitumour potency on solid tumours of various derivations. We demonstrate here that gambogic acid also present powerful antileukaemic potency through both growth arrest and apoptosis induction in Jurkat cells...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2008.00292.x
更新日期:2008-12-01 00:00:00
abstract::Since the 1970s, we have known that aspirin can reduce the risk of pre-eclampsia. However, the underlying mechanisms explaining this risk reduction are poorly understood. Both cyclooxygenase (COX)-1- and COX-2-dependent effects might be involved. As a consequence of this knowledge hiatus, the optimal dose and timing o...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,评审
doi:10.1111/bcpt.13308
更新日期:2020-08-01 00:00:00
abstract::Vitamin D metabolism was studied in primary human dermal fibroblasts with focus on drug-mediated gene regulation related to adverse side effects of antiretroviral drugs used in HIV therapy. The fibroblasts expressed mRNA for cytochrome P450 (CYP) enzymes catalysing bioactivating (CYP2R1, CYP27A1 and CYP27B1) and catab...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12641
更新日期:2017-01-01 00:00:00
abstract::Eudesmols are naturally occurring sesquiterpenoid alcohols that present cytotoxic effect to cancer cells. Herein, all eudesmol isomers displayed cytotoxicity to different tumour cell lines. α-Eudesmol showed IC₅₀ values ranging from 5.38 ± 1.10 to 10.60 ± 1.33 μg/mL for B16-F10 and K562 cell lines, β-eudesmol showed I...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12097
更新日期:2013-11-01 00:00:00
abstract::Whilst mitotic rat embryonic cardiomyoblast-derived H9c2 cells have been widely used as a model system to study the protective mechanisms associated with flavonoids, they are not fully differentiated cardiac cells. Hence, the aim of this study was to investigate the cardioprotective and cardiotoxic actions of querceti...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12319
更新日期:2015-02-01 00:00:00
abstract::Melatonin possesses chronobiotic properties, which affects sleep/wake rhythms. We investigated a 7-day administration of melatonin (0.25, 2.5 and 5 mg/kg body weight) on the activity/rest rhythms of a diurnal animal (the ringdove, Streptopelia risoria), aged 2-3 (young) and 10-12 (old) years, and its possible relation...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2006.00032.x
更新日期:2007-04-01 00:00:00
abstract::Vanishing bile duct syndrome is a severe cholestatic disease associated with toxic effects of medications. Stevens-Johnson syndrome is a hypersensitivity disorder that may also be caused by medications. We present a case of a 62-year-old male patient who developed vanishing bile duct syndrome a month after Stevens-Joh...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2009.00474.x
更新日期:2010-01-01 00:00:00
abstract::This retrospective study investigated whether the serum albumin (SA) concentration at presentation is associated with mortality and the mechanism underlying the association. This study enrolled 217 patients poisoned with organophosphate (OP). Hypoalbuminemia (albumin <3.5 g/dL) at presentation was identified in 18.4% ...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.13546
更新日期:2020-12-11 00:00:00
abstract::Seijo-bofu-to, a traditional medicine used to treat acne in Asian countries, contains twelve herbal components, including Angelica dahurica root, a source of furanocoumarin derivatives. In this study, we investigated potential herb-drug interactions of seijo-bofu-to in healthy male volunteers. Thirty-two young, health...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12224
更新日期:2014-10-01 00:00:00
abstract::Mercaptopurine is a drug commonly used in the treatment of different types of cancer, especially acute lymphoblastic leukaemia, and autoimmune diseases such as ulcerative colitis or Crohn's disease and in patients receiving organ transplants. It is metabolized by three cytosolic enzymes. One of them, thiopurine S-meth...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,随机对照试验
doi:10.1111/bcpt.13153
更新日期:2019-04-01 00:00:00
abstract::To study the influence of single or repeated low-level sarin inhalation exposure on immune functions, inbred BALB/c mice were exposed to low clinically asymptomatic concentrations of sarin for 60 min. in the inhalation chamber. The evaluation of immune functions was carried out using phenotyping of CD3 (T-lymphocytes)...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2004.pto940307.x
更新日期:2004-03-01 00:00:00
abstract::In the last decades, a number of new antimuscarinic drugs have been introduced for treatment of the overactive bladder (OAB), defined symptomatically (OAB syndrome) or urodynamically (detrusor overactivity). Recently, three new drug principles have been approved for clinical use, the β3 -adrenoceptor agonist, mirabegr...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,评审
doi:10.1111/bcpt.12577
更新日期:2016-10-01 00:00:00
abstract::Prolyl oligopeptidase (POP) has been connected to learning, memory and mood. Changes in serum or plasma POP activity have been linked to psychiatric disorders. POP has been thought to interfere in these conditions by cleaving neuroactive peptides or via the phosphatidylinositol second messenger system. However, little...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2010.00626.x
更新日期:2011-01-01 00:00:00
abstract::We investigated the effects of (1,4)-alpha-D-glucan (alpha-DG), a novel immune stimulatory drug from Tinospora cordifolia, on the concentration of pro- and anti-inflammatory cytokines (interleukin [IL]-1beta, IL-6, tumour necrosis factor-alpha [TNF-alpha], gamma-interferon [IFN-gamma] and IL-10) in the lung and spleen...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2009.00447.x
更新日期:2009-11-01 00:00:00
abstract::The development of medium to high-throughput in vitro screening of ADME (Absorption, Distribution, Metabolism, Excretion) properties has been the reply to higher demands on drug metabolism scientists to cope with progress in chemistry and biology. Two areas will be discussed here, namely screens for oral absorption an...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,评审
doi:10.1111/j.1742-7843.2005.pto960304.x
更新日期:2005-03-01 00:00:00
abstract::The six commonly used trade herbal products, St. John's wort, common valerian, common sage, Ginkgo biloba, Echinacea purpurea and horse chestnut, and ethanol, were investigated for their in vitro inhibitory potential of cytochrome P450 2D6 (CYP2D6)-mediated metabolism. Herbal components were extracted from commerciall...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2007.00121.x
更新日期:2007-11-01 00:00:00
abstract::Is it not more comfortable to spit saliva in a tube than to be pricked with a needle to draw blood to analyse your health and disease risk? Many patients, study participants and (parents of) young children undoubtedly prefer non-invasive and convenient procedures. Such procedures increase compliance rates especially f...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,评审
doi:10.1111/bcpt.12721
更新日期:2017-09-01 00:00:00
abstract::Cytochrome P450 3A4 (CYP3A4) is quantitatively the most important P450 enzyme in adults. It is suggested that CYP3A4 genetic polymorphisms may influence the rate of the metabolism and elimination of CYP3A4 substrates in human beings. Ibrutinib is an anticancer drug and primarily metabolized by CYP3A4. The aim of this ...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12934
更新日期:2018-04-01 00:00:00
abstract::In the present study, we investigated the hepatoprotective effects of salvianolic acid A, a novel antioxidant, against oxidative stress and acute liver injury induced by carbon tetrachloride (CCl(4)) in rats, and the mechanisms underlying its protective effects. Administration of CCl(4) to rats caused severe hepatic d...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7835.2007.00020.x
更新日期:2007-02-01 00:00:00
abstract::In this study, we tested the hypothesis that fasudil, a Rho kinase inhibitor, would protect against contrast-induced acute kidney injury (CI-AKI) in a mouse model and attempted to elucidate the mechanism involved. Mice subjected to unilateral ligation of the left anterior renal pedicle were divided into four groups: (...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12895
更新日期:2018-02-01 00:00:00
abstract::Opioids given to pregnant and parturient women are relatively freely transferred across the placenta. Spinal, epidural and intravenous fentanyl has been studied in pregnant women and neonates, but foetal safety of fentanyl dosing with transdermal patch during pregnancy and labour is not sufficiently studied. Foetal pH...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12665
更新日期:2017-02-01 00:00:00
abstract::Inadequate antidote stocking is a global problem in hospitals. Insufficient supplies and delays in the administration of antidotes could lead to death and additional potentially negative clinical consequences. Our objective was to determine the availability of antidotes in hospitals listed on the Saudi Ministry of Hea...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12897
更新日期:2018-02-01 00:00:00
abstract::Vitamin D deficiency seems to be implicated in the onset and progression of some autoimmune disorders. No previous study has investigated vitamin D homeostasis in post-partum thyroiditis. We compared 25-hydroxyvitamin D and parathyroid hormone (PTH) levels between four groups of non-lactating women who gave birth with...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/bcpt.12349
更新日期:2015-06-01 00:00:00
abstract::Previous studies have shown that generation of free radicals is increased following pentylenetetrazol kindling, due to increased cytosolic Ca2+ concentrations. Topiramate, a voltage-gated calcium channel inhibitor, has an evident effect in the treatment of childhood epilepsy; however, topiramate may cause nephrotoxici...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章
doi:10.1111/j.1742-7843.2008.00271.x
更新日期:2008-08-01 00:00:00
abstract::In this MiniReview, we provide general considerations for the planning and conduct of pharmacoepidemiological studies of associations between drug use and cancer development. We address data sources, study design, assessment of drug exposure, ascertainment of cancer outcomes, confounder adjustment and future perspecti...
journal_title:Basic & clinical pharmacology & toxicology
pub_type: 杂志文章,评审
doi:10.1111/bcpt.12946
更新日期:2018-05-01 00:00:00