Abstract：
:1 Nateglinide, a novel oral hypoglycemic agent, rapidly reaches the maximum serum concentration after oral administration, suggesting that it is rapidly absorbed in the gastrointestinal tract. The aim of this work is to clarify the intestinal absorption mechanism of nateglinide by means of in vitro studies. 2 We examined the transcellular transport and the apical uptake of [(14)C]nateglinide in a human colon carcinoma cell line (Caco-2). We also examined whether nateglinide is transported via monocarboxylate transport-1 (MCT1) by means of an uptake study using MCT1-expressing Xenopus laevis oocytes. 3 In Caco-2 cells, the transcellular transport of [(14)C]nateglinide from the apical to basolateral side was greater than that in the opposite direction. The uptake of [(14)C]nateglinide from the apical side was concentration-dependent, H(+)-dependent, and Na(+)-independent. Kinetic analysis revealed that the Kt and Jmax values of the initial uptake rate of [(14)C]nateglinide were 448 micro M and 43.2 nmol mg protein(-1) 5 min(-1), respectively. Various monocarboxylates, including salicylic acid and valproic acid, and glibenclamide significantly inhibited the uptake of [(14)C]nateglinide. 4 The uptake study using MCT1-expressing oocytes showed that nateglinide inhibits the MCT1-mediated uptake of [(14)C]L-lactic acid, though nateglinide itself is not transported by MCT1. 5 Taken together, these results suggest that the uptake of nateglinide from the apical membranes of Caco-2 cells is, at least in part, mediated by a proton-dependent transport system(s) distinct from MCT1.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Okamura A,Emoto A,Koyabu N,Ohtani H,Sawada Ydoi
10.1038/sj.bjp.0704875subject
Has Abstractpub_date
2002-10-01 00:00:00pages
391-9issue
3eissn
0007-1188issn
1476-5381journal_volume
137pub_type
杂志文章abstract：:1. Some hydroxy-, amino-, and methoxy- phenylalkyltrimethylammonium compounds, beta-pyridylmethyl- dimethylamine and pyrrolidine, and beta-pyridylethyltrimethylammonium, were tested on avoidance learning in mice and their effects were compared with those of (-)-nicotine.2. The o- and m- hydroxybenzyl-, o-hydroxyphenet...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1970.tb10372.x
更新日期：1970-07-01 00:00:00
abstract：:1. The effect of 4-aminopyridine (4-AP) on the slow afterhyperpolarization (sAHP) seen after high frequency dendritic or somatic firing was investigated in rat hippocampal CA1 pyramidal neurones (PC). Intracellular recordings were obtained from the distal apical dendrites and somata and suprathreshold depolarizing cur...
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0704533
更新日期：2002-02-01 00:00:00
abstract：:1. Stimulation of the murine macrophage cell line RAW 264.7 with thapsigargin, an endomembrane Ca(2+)-ATPase inhibitor, induced histamine production in a time- and concentration-dependent manner. 2. The protein kinase C activator, 12-O-tetradecanoylphorbol 13-acetate (TPA), also enhanced histamine production. 3. alpha...
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0703085
更新日期：2000-02-01 00:00:00
abstract：:1. The role of the sympathetic nervous system in experimental hypertension and associated changes in aortic sodium and potassium was studied using normal and immunosympathectomized Sprague-Dawley rats.2. A single injection of antiserum to nerve-growth factor to rats at birth produced less intensive destruction of the ...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1970.tb09911.x
更新日期：1970-10-01 00:00:00
abstract：:1. The present study was undertaken to investigate the effects of the novel nociceptin receptor antagonist, [Nphe(1)]-Nociceptin (1-13)-NH(2) (bilateral intrahippocampal injection, 50 nmole rat(-1)) on purported nociceptin-induced (bilateral intrahippocampal injection, 5 nmole rat(-1)) deficits in spatial learning in ...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0703724
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abstract：:1. Aqueous extracts of stratum corneum were found to cause histamine-like contractions of the guinea-pig ileum which were not antagonized by mepyramine, atropine or bromolysergic acid diethylamide.2. The compounds responsible for this contraction were isolated by chromatography and shown to be common amino acids, part...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1972.tb09581.x
更新日期：1972-05-01 00:00:00
abstract：:1. Inhalational anaesthetics modulate ligand-gated ion channels at clinical concentrations. In this paper we address submolecular mechanisms for gamma-aminobutyric acid (GABA) receptor modulation by isoflurane. 2. Wild-type Drosophila melanogaster homo-oligomeric GABA receptors were characterized and compared with an ...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0701417
更新日期：1997-10-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0703460
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0701412
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abstract：:Preclinical and clinical data suggest that a modification in GABA(B) receptor expression and function may contribute to the symptoms of major depression and the response to antidepressants. This includes laboratory animal experiments demonstrating that antidepressants modify brain GABA(B) receptor expression and funct...
journal_title：British journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1111/j.1476-5381.2010.01004.x
更新日期：2011-01-01 00:00:00
abstract：:1. Cannabinoids are potent inhibitors of endothelium-derived hyperpolarizing factor (EDHF)-mediated relaxations. We set out to study the mechanism underlying this effect and the possible role of cannabinoid-induced changes in intercellular gap junction communication. 2. In cultured endothelial cells, Delta(9)-tetrahyd...
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0704776
更新日期：2002-07-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1982.tb08775.x
更新日期：1982-01-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1980.tb10421.x
更新日期：1980-02-01 00:00:00
abstract：:1 Uniaxial cyclic stretch leads to an upregulation of cyclooxygenase (COX)-2 through increases in the intracellular Ca(2+) concentration via the stretch-activated (SA) channel and following nuclear factor kappa B (NF-kappaB) activation in human fibroblasts. However, the signaling mechanism as to how the elevated Ca(2+...
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0706182
更新日期：2005-06-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1995.tb14994.x
更新日期：1995-07-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1990.tb14708.x
更新日期：1990-02-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Tolerance induced by morphine and other opiates remains a major unresolved problem in the clinical management of pain. There is now good evidence for the importance of MAPKs in morphine-induced antinociceptive tolerance. A member of the MAPK kinase kinase family, TGF-β activated kinase 1 (TAK1) i...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/bph.13094
更新日期：2015-06-01 00:00:00
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0703754
更新日期：2000-12-01 00:00:00
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pub_type： 杂志文章
doi：10.1038/sj.bjp.0704076
更新日期：2001-05-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1975.tb07611.x
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abstract：:1. The effect of the calcitonin gene-related peptide antagonist (CGRP8-37, 400 nmol kg-1, i.v.) on the increased blood flow induced by calcitonin gene related peptide (CGRP), vasodilator prostaglandins, and topical capsaicin was measured with a laser Doppler blood flow meter in rat abdominal skin. 2. The saphenous ner...
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1993.tb13878.x
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doi：10.1038/sj.bjp.0703809
更新日期：2001-01-01 00:00:00
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doi：10.1038/sj.bjp.0703445
更新日期：2000-07-01 00:00:00
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更新日期：2002-03-01 00:00:00
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pub_type： 杂志文章
doi：10.1111/j.1476-5381.1995.tb15128.x
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abstract：:1. Changes in cutaneous water loss were followed by continuously monitoring total body weight loss.2. Sweating was induced in normal subjects by raising the environmental temperature or by subjecting them to the emotional stress of mental arithmetic.3. Propranolol in a dosage of 0.15 mg/kg body weight intravenously ha...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1973.tb08180.x
更新日期：1973-03-01 00:00:00
abstract：:1. Whole-cell patch-clamp recordings were made from smooth muscle cells isolated from the longitudinal muscle layer of guinea-pig ileum. Carbachol (acting at muscarinic receptors) or histamine (acting at H1 histamine receptors) suppressed Ca2+ channel current. The effect of either agonist had an initial transient comp...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0702112
更新日期：1998-10-01 00:00:00
abstract：:BACKGROUND AND PURPOSE The transepithelial absorption of Na(+) in the lungs is crucial for the maintenance of the volume and composition of epithelial lining fluid. The regulation of Na(+) transport is essential, because hypo- or hyperabsorption of Na(+) is associated with lung diseases such as pulmonary oedema or cys...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.2012.01909.x
更新日期：2012-07-01 00:00:00
abstract：:1. We have shown earlier that pilocarpine strongly inhibits mouse and human liver coumarin 7-hydroxylase activity of CYP 2A and pentoxyresorufin O-deethylase activity of CYP 2B in vitro. Since pilocarpine, like coumarin, contains a lactone structure we have studied in more detail its inhibitory potency on mouse and hu...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1995.tb17217.x
更新日期：1995-11-01 00:00:00
abstract：:In moderate-to-severe asthma, adding an inhaled long-acting β2 -adenoceptor agonist (LABA) to an inhaled corticosteroid (ICS) provides better disease control than simply increasing the dose of ICS. Acting on the glucocorticoid receptor (GR, gene NR3C1), ICSs promote anti-inflammatory/anti-asthma gene expression. In vi...
journal_title：British journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1111/bph.13628
更新日期：2016-12-01 00:00:00
