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Noah Scheinfeld
Dermatology online journal, 9(2), 4-4 (2003-03-18)
Cimetidine, approved by the FDA for inhibition of gastric acid secretion, has been advocated for a number of dermatological diseases. The cutaneous uses and immunological effects of cimetidine have been actively studied over the past few years, and this review
Wei Guo et al.
Environmental toxicology and pharmacology, 38(3), 901-912 (2014-12-03)
This study aimed to identify the specific cytochrome P450 (CYP450) enzymes involved in the metabolism of dipfluzine hydrochloride using the combination of a chemical inhibition study, a correlation analysis and a panel of recombinant rat CYP450 enzymes. The incubation of
Ana Salomé Correia et al.
Animals : an open access journal from MDPI, 11(8) (2021-08-28)
Drug repurposing and drug combination are important therapeutic approaches in cancer therapy. Drug repurposing aims to give new indications to drugs, rather than the original indication, whereas drug combination presupposes that the effect that is obtained should be more beneficial
Florence Lefranc et al.
International journal of oncology, 28(5), 1021-1030 (2006-04-06)
Cimetidine (CIM), the prototypical histamine H2 receptor antagonist (H2RA), was brought to market based on its ability to accelerate healing of gastrointestinal ulcers through the inhibition of gastric acid secretion. Cimetidine, the most studied H2RA, has been demonstrated to possess
Margaret O Sofidiya et al.
BMC complementary and alternative medicine, 12, 168-168 (2012-10-04)
The leaves and root of Flabellaria paniculata (Malpighiaceae) are frequently used in the treatment of wounds and ulcers in Nigerian folk medicine. The purpose of this study was to compare the effect of ethanolic extracts from the leaves (FPL) and
Sanjeev Deva et al.
The Cochrane database of systematic reviews, 8(8), CD007814-CD007814 (2012-08-17)
Anecdotal reports of tumour regression with histamine type 2 receptor antagonists (H(2)RAs) have lead to a series of trials with this class of drug as adjuvant therapy to try and improve outcomes in patients with resected colorectal cancers. There was
Rieko Oshima et al.
Metabolism: clinical and experimental, 64(2), 296-304 (2014-12-01)
5'-Adenosine monophosphate-activated protein kinase (AMPK) is a key molecule of metabolic enhancement in skeletal muscle. We investigated whether metformin (MET) acts directly on skeletal muscle, is transported into skeletal muscle via organic cation transporters (OCTs), and activates AMPK. Isolated rat
Xiaofeng Bao et al.
Nuclear medicine and biology, 39(8), 1128-1136 (2012-08-18)
Rhodamine-123 is a known substrate for the efflux transporter, P-glycoprotein (P-gp). We wished to assess whether rhodamine-123 might serve as a useful substrate for developing probes for imaging efflux transporters in vivo with positron emission tomography (PET). For this purpose
Tzu-Kai Lin et al.
The Journal of investigative dermatology, 133(2), 469-478 (2012-09-28)
Systemic antagonists of the histamine type 1 and 2 receptors (H1/2r) are widely used as anti-pruritics and central sedatives, but demonstrate only modest anti-inflammatory activity. Because many inflammatory dermatoses result from defects in cutaneous barrier function, and because keratinocytes express
Sarit Pal et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 318(3), R590-R604 (2020-01-09)
Lymphatic vessels play a critical role in mounting a proper immune response by trafficking peripheral immune cells to draining lymph nodes. Mast cells (MCs) are well known for their roles in type I hypersensitivity reactions, but little is known about
Hong Wei et al.
Pharmacological research, 90, 58-66 (2014-10-12)
Among brain structures receiving efferent projections from the histaminergic tuberomammillary nucleus is the pontine locus coeruleus (LC) involved in descending noradrenergic control of pain. Here we studied whether histamine in the LC is involved in descending regulation of neuropathic hypersensitivity.
H van der Goot et al.
European journal of medicinal chemistry, 35(1), 5-20 (2000-03-25)
In this review the histaminergic ligands for the histamine H(1), H(2) and H(3) receptors, which are currently used as tools in pharmacological studies, are described. To study interactions with the histamine H(1) receptor, the H(1) agonist 2-aminoethylthiazole has long since
Jia-Xing Yue et al.
CNS neuroscience & therapeutics, 20(10), 883-892 (2014-07-06)
The upregulation of Nav1.8 in primary afferents plays a critical role in the development and persistence of neuropathic pain. The mechanisms underlying the upregulation are not fully understood. The present study aims to investigate the regulatory effect of histamine on
Tonggui Ding et al.
Basic & clinical pharmacology & toxicology, 116(5), 385-389 (2014-09-25)
This study firstly investigated the effects of cucurbitacin E (CuE), a tetracyclic triterpene compound from Cucurbitaceae, on the pharmacokinetics (PK) and pharmacodynamics (PD) of warfarin, a model CYP2C probe substrate, in the rat. In PK studies, the concentration of warfarin
Jaclyn N Harper et al.
American journal of physiology. Renal physiology, 304(1), F56-F67 (2012-10-05)
OCT2 is the entry step for organic cation (OC) secretion by renal proximal tubules. Although many drugs inhibit OCT2 activity, neither the mechanistic basis of their inhibition nor their transport status is generally known. Using representatives of several structural classes
Organic cation transporter/solute carrier family 22a is involved in drug transfer into milk in mice.
Naoki Ito et al.
Journal of pharmaceutical sciences, 103(10), 3342-3348 (2014-09-02)
Drug transfer into milk is a general concern during lactation. So far, breast cancer resistance protein (Bcrp) is the only transporter known to be involved in this process, whereas participation of other transporters remains unclear. We investigated the importance of
Sandra Buratta et al.
Biochemical pharmacology, 95(3), 201-209 (2015-04-18)
The antiarrhythmic agent amiodarone, a cationic amphiphilic drug, is known to induce phospholipidosis, i.e. the accumulation of phospholipids within lysosomal structures to give multi-lamellar inclusion bodies. Despite the concerns raised about phospholipidosis in the recent years, the molecular mechanisms underlying
Swati Dumitras et al.
International journal of clinical pharmacology and therapeutics, 51(10), 771-779 (2013-09-18)
Glycopyrronium (NVA237), a novel once-daily long-acting muscarinic antagonist (LAMA), has recently been approved for maintenance treatment of COPD. This study evaluated the effect of organic cation transporter inhibition on inhaled glycopyrronium disposition using cimetidine as a probe inhibitor. In this
Seyoum Ayehunie et al.
Pharmaceutical research, 35(4), 72-72 (2018-02-25)
The study evaluates the use of new in vitro primary human cell-based organotypic small intestinal (SMI) microtissues for predicting intestinal drug absorption and drug-drug interaction. The SMI microtissues were reconstructed using human intestinal fibroblasts and enterocytes cultured on a permeable
J A Sprowl et al.
Clinical pharmacology and therapeutics, 94(5), 585-592 (2013-07-19)
The organic cation transporter 2 (OCT2) regulates uptake of cisplatin in proximal tubules, and inhibition of OCT2 protects against severe cisplatin-induced nephrotoxicity. However, it remains uncertain whether potent OCT2 inhibitors, such as cimetidine, can influence the antitumor properties and/or disposition
C E Elwin
Nordisk medicin, 106(5), 151-154 (1991-01-01)
Interactions between pharmaceutical preparations are common and can occur at almost every stage in a substance's metabolic clearance but frequently lack clinical significance. Different factors must be considered in the assessment of data on interactions. This article compares interactions between
G Stepek et al.
Parasitology, 134(Pt 1), 103-112 (2006-10-13)
Cysteine proteinases from the fruit and latex of plants, including papaya, pineapple and fig, were previously shown to have a rapid detrimental effect, in vitro, against the rodent gastrointestinal nematodes, Heligmosomoides polygyrus (which is found in the anterior small intestine)
L N Valenkevich et al.
Klinicheskaia meditsina, 69(3), 91-93 (1991-03-01)
The response of serum gastrin, insulin and glucagon to administration of sodium bicarbonate (SB) followed by cimetidine was studied in 35 duodenal ulcer patients. Relevant measurements were made using radioimmunoassay kits "Diagnostic" (USA) and "Oris" (France). It was established that
P D Rogers
The Annals of pharmacotherapy, 31(3), 365-367 (1997-03-01)
Treatment options for AIP remain limited. Although no single therapy has been proven superior in clinical trials, intravenous hemin appears to be more effective than increased carbohydrate intake, and remains the treatment of choice. At usual dosages the average wholesale
Brittany N Ross et al.
PloS one, 10(10), e0141845-e0141845 (2015-10-31)
A renewed interest in Shiga toxin-producing Escherichia coli (STEC) strains was sparked due to the appearance of an outbreak in 2011, causing 3,816 diarrheal cases and some deaths in Europe. The causative strain was classified as enteroaggregative E. coli of
G I Lobov et al.
Bulletin of experimental biology and medicine, 152(4), 406-408 (2012-07-18)
The effects of histamine and mechanisms of its action on the capsular smooth muscle cells of mesenteric lymph nodes were examined on isolated capsular strips under isometric conditions. Histamine (1×10(-8)-5×10(-7) M) decreased the tone of capsular smooth muscle cells and
Fatmanur Tuğcu-Demiröz et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 62, 105-110 (2014-06-03)
The aim of the present study was to develop a method for water flux reabsorption measurement in Doluisio's Perfusion Technique based on the use of phenol red as a non-absorbable marker and to validate it by comparison with gravimetric procedure.
Sarit Pal et al.
Biology open, 11(7) (2022-07-02)
Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types.
Ulcerogenic and intestinal motility/transit stimulating actions of nevirapine in albino Wistar rats.
Elizabeth Bassey Umoren et al.
Journal of physiology and biochemistry, 69(3), 547-557 (2013-03-29)
The antiretroviral is a non-nucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1. This study was undertaken to investigate the effect of nevirapine (NVP) administration on gastric acid secretion, pepsin secretion, mucosal secretion, intestinal motility, and transit using apparently
G A Balint
Trends in pharmacological sciences, 19(10), 401-403 (1998-11-06)
The exact mechanism of action of the anti-ulcerogenic drugs is still under debate. According to the literature, under normal conditions the cAMP:cGMP ratio in the rat gastric mucosa is approximately 8:10. Following prostacyclin administration, this ratio transiently decreases but later
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