Abstract:
:We report that the loop diuretic drugs bumetanide and furosemide used in the treatment of hypertension are GPR35 agonists. We utilized calcium flux, inositol phosphate accumulation, and dynamic redistribution assays to examine the pharmacology of these compounds on the human, mouse and rat GPR35. While potent on human GPR35, neither bumetanide nor furosemide were active against mouse or rat GPR35. Furthermore, the Na(+)-Cl(-) cotransporter inhibi- tors chlorothiazide and hydrochlorothiazide were inactive against GPR35 in all three species. We also demonstrate that GPR35 is expressed in human skin where it has been shown that loop diuretics inhibit histamine-induced flare and itch response. These findings suggest that GPR35 may play an important role in skin cell biology and be a potential target for the treatment of a variety of immune disorders.
journal_name
Pharmacologyjournal_title
Pharmacologyauthors
Yang Y,Fu A,Wu X,Reagan JDdoi
10.1159/000335127subject
Has Abstractpub_date
2012-01-01 00:00:00pages
13-7issue
1-2eissn
0031-7012issn
1423-0313pii
000335127journal_volume
89pub_type
杂志文章相关文献
PHARMACOLOGY文献大全abstract::Acute ethanol administration to rats fasted overnight resulted in a significant decrease in the content of glutathione (GSH) of the liver concomitantly with a partial increase in oxidized glutathione levels, representing a net 38% decrease in total GSH equivalents. In these conditions, liver lipoperoxidation is signif...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137514
更新日期:1981-01-01 00:00:00
abstract::We investigated the vascular effects of glucagon-like peptide-1 (GLP-1) and Exendin-4 in type 2 diabetic rat aortae. Studies were performed in a normal control group (NC) (0.2 ml i.p. saline, n = 10), streptozotocin (STZ)/nicotinamide diabetic control group (DC) (a single dose of 80 mg/kg STZ i.p. injection 15 min aft...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000084277
更新日期:2005-06-01 00:00:00
abstract::Protective influence of verapamil upon ouabain-induced cardiac arrhythmias was investigated in anesthetized (alpha-chloralose 60 mg/kg and urethane 500 mg/kg) open-chest guinea pigs. Verapamil in doses between 100 and 150 micrograms/kg significantly increased (80-90%) the dose of ouabain, necessary to cause ventricula...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138326
更新日期:1988-01-01 00:00:00
abstract::To determine the existence of beta 3-adrenoceptors in functional assays in isolated preparations for which data are lacking, we compared the effects of SR 58611A, a selective beta 3-adrenoceptor agonist, and isoprenaline in the guinea pig common bile duct, distal colon and urinary bladder. SR 58611A and isoprenaline r...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139338
更新日期:1995-11-01 00:00:00
abstract::Increased concentrations of immunoreactive methionine-enkephalin but not leucine-enkephalin were measured in fractions of cerebrospinal fluid perfusate collected from ventricular-cisternally perfused, urethane-anesthetized rats exposed to a mixture of 75% nitrous oxide/25% oxygen for 60 min. These findings suggest tha...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138056
更新日期:1985-01-01 00:00:00
abstract:BACKGROUND AND PURPOSE:Carvedilol is used clinically as a β-adrenoceptor antagonist for the treatment of chronic heart failure and is primarily metabolized into glucuronides by UDP-glucuronosyltransferase (UGT). In this study, the stereoselective glucuronidation of carvedilol by the human liver and intestinal microsome...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000340020
更新日期:2012-01-01 00:00:00
abstract::It has previously been demonstrated in several species that the secretory granules of pancreatic beta-cells have the ability to store substantial amounts of calcium and bioactive amines, such as dopamine and serotonin. Furthermore, evidence for a similar topographical localization for amine and calcium within the peri...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138053
更新日期:1985-01-01 00:00:00
abstract:BACKGROUND:Historical evidence has verified the multifaceted antiviral efficacy of polyoxometalates (PMs). METHODS:We carried out a study to investigate the antimicrobial effects of each of the 5 substances comprising virus block (VB): 3 PMs that have antibacterial and antiviral activity, an antibiotic agent, and an a...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000500897
更新日期:2019-06-06 00:00:00
abstract::The vascular relaxant effect of salbutamol and its dependence on the endothelium were studied in the isolated dog coronary artery, precontracted with prostaglandin F2 alpha. Salbutamol induced a concentration-dependent relaxation which was partially inhibited by removal of endothelial cells. Atenolol 10(-6) mol/l, a b...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138804
更新日期:1991-01-01 00:00:00
abstract:INTRODUCTION:The accumulation of amyloid-β (Aβ) plaque in the brain is a characteristic feature of Alzheimer's disease (AD) and the cause of fatal oxidative damage to neuronal cells. Korean red ginseng (RG) is used extensively in traditional medicine and is known to have anti-oxidative and anti-inflammatory properties....
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000505592
更新日期:2020-01-01 00:00:00
abstract::The antinociceptive effect in mice (hot-plate test) of caerulein (0.15 mg/kg s.c.) was many times more resistant to naloxone than that of morphine (2 mg/kg s.c., equipotent with the caerulein dose). The ED50 (mg/kg s.c.) of naloxone (given simultaneously with an agonist) was with morphine 0.01 and with caerulein 0.07....
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137733
更新日期:1982-01-01 00:00:00
abstract::The agent, 6-(N,N-diethylamino)-hexyl- 3, 4, 5,-Trimethoxybenzoate (TMB-6) which relaxes smooth and skeletal muscle by interfering with intracellular Ca ++ availability was tested for its electrophysiological effects on canine cardiac Purkinje fibres and feline papillary muscles. In both tissues the drug causes a decr...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136585
更新日期:1976-01-01 00:00:00
abstract::delta9-Tetrahydrocannabinol (THC) inhibited ulcer formation in the pylorus-ligated rat (Shay rat test). However, this antiulcer activity of THC was substantially less than for the anticholinergic substance tridihexethyl chloride both in terms of degree of activity and potency. In addition, the results of the present s...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136851
更新日期:1978-01-01 00:00:00
abstract::Both acute and chronic oral administration (1-20 mg/kg) of FCE 22716, a new ergoline derivative, resulted in a dose-related fall of arterial blood pressure lasting for more than 6 h. Tachycardia was observed only at high dosages. Yohimbine, propranolol and indometacin did not modify its antihypertensive effect; on the...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138523
更新日期:1989-01-01 00:00:00
abstract::Although proton pump inhibitors (PPI) are generally well tolerated, with most adverse effects being minor and self-limiting, there are singular reports on hypersensitivity immune reactions triggered by a PPI or its metabolites. Here we report a case of acute drug-induced fever with leukocytosis and a transient increas...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000364781
更新日期:2014-01-01 00:00:00
abstract::In a randomized three-phase crossover study, 12 healthy male volunteers were given three 12-hourly 500-mg doses of erythromycin base, as enteric coated pellets in capsules (2 X 250 mg), erythromycin stearate tablet (1 X 500 mg), or erythromycin ethylsuccinate sachet (1 X 500 mg). The reaction time after administration...
journal_title:Pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1159/000138029
更新日期:1984-01-01 00:00:00
abstract::Polybrominated diphenyl ethers (PBDEs) are a class of brominated flame retardants. PBDEs have been widely used in textiles, flexible polyurethane foams, electronic components, electrical components, and plastics. 11β-Hydroxysteroid dehydrogenases, isoform 1 (HSD11B1) and isoform 2 (HSD11B2), have been demonstrated to ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000445213
更新日期:2016-01-01 00:00:00
abstract::Ketotifen is an antiallergic drug and may have direct inhibitory effects on eosinophils. To investigate the anti-eosinophilic effect of ketotifen, we examined the effect of ketotifen on the production of reactive oxygen species (ROS) from eotaxin-primed human eosinophils. Ketotifen at 10(-10)-10(-6) mol/l significantl...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000072666
更新日期:2003-11-01 00:00:00
abstract::Combination therapy with antiretroviral drugs is used for the treatment of patients infected with the human immunodeficiency virus. To achieve optimal drug concentrations for viral suppression and avoidance of drug toxicity, monitoring of drug levels has been considered essential. We set up an analytical procedure for...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000073664
更新日期:2003-12-01 00:00:00
abstract::Renal lithium clearance, tissue lithium levels, serum lithium concentration, and body temperature were determined in rats given lithium alone or combined with haloperidol (0.5-1 mg/kg). A slight increase in serum lithium concentration occurred in one of the three groups given lithium plus haloperidol. Haloperidol fail...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136708
更新日期:1977-01-01 00:00:00
abstract::Various stressful stimuli cause mast cell degranulation. Hemorrhagic shock is one such stressful stimulus which may cause mast cell degranulation and histamine release. Histamine may be involved in the pathophysiology of hemorrhage. It was reported that there are large amounts of histamine in the anterior and posterio...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138826
更新日期:1991-01-01 00:00:00
abstract:BACKGROUND:Multidrug resistance (MDR) presents a problem in cancer chemotherapy, and developing new agents to overcome MDR is important. This study intends to investigate the reversal effect of -elemene on MDR in human breast carcinoma MCF-7 and doxorubicin-resistant MCF-7 cells. METHODS:MTT cytotoxicity assays, flow ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000337178
更新日期:2012-01-01 00:00:00
abstract::The transketolase activity (TKA) of the white and red blood cells of oral contraceptive users was studied in an unselected sample population. Compared with healthy controls of corresponding age, the white cell TKA in the oral contraceptive groups was lowered in about 30%. The red cell TKA was lowered in about 15% of...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136475
更新日期:1974-01-01 00:00:00
abstract::Two groups of rats were used to examine the effect of pioglitazone, a peroxisome proliferator-activated receptor gamma (PPARgamma) agonist, on rat hearts using an in vivo model of ischemia-reperfusion (I/R) to elucidate potential mechanisms. One group was the 30-min reperfusion group, which was further subdivided into...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000100870
更新日期:2007-01-01 00:00:00
abstract::Esculentoside A, a kind of saponin isolated from the root of the Chinese herb Phytolaca esculenta, is reported to possess potent anti-inflammatory effects in acute and chronic experimental models. In the present study, we investigated the effects of esculentoside A on the production of tumor necrosis factor (TNF), int...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000028197
更新日期:1998-04-01 00:00:00
abstract::Extracellular ATP regulates cell proliferation, muscle contraction and myoblast differentiation. ATP present in the muscle interstitium can be released from contracting skeletal muscle cells. L-Carnitine is a key element in muscle cell metabolism, as it serves as a carrier for fatty acid through mitochondrial membrane...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000114449
更新日期:2008-01-01 00:00:00
abstract::The H2-antagonist tiotidine inhibited the H2-receptor-mediated, histamine-induced increase in cyclic AMP in dispersed mucosal cells from guinea pig stomach (Ki, 4 X 10(-8) M). The radiolabeled [3H]-tiotidine bound specifically and reversibly to the same cells with a half-maximal binding occurring at 5 X 10(-7) M tioti...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138176
更新日期:1986-01-01 00:00:00
abstract::Papers published over 100 years since the beginning of the scientific study of drug metabolism in birds were reviewed. Birds were found to be able to accomplish more than 20 general biotransformation reactions in both functionalization and conjugation. Chickens were the primary subject of study but over 30 species of ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137327
更新日期:1979-01-01 00:00:00
abstract::Effects of schisandrin B enantiomer ((+)Sch B and (-)Sch B) treatment on the reduced cellular glutathione (GSH) level and susceptibility to menadione-induced toxicity were investigated and compared in AML12 hepatocytes. (+)Sch B or (-)Sch B treatment at 6.25 micromol/l produced a time-dependent change in cellular GSH ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000092773
更新日期:2006-01-01 00:00:00
abstract::The effects of alpha-tocopherol, ascorbic acid and rutin on peroxidative processes were studied in xanthine-xanthine oxidase system, linoleic acid ufasomes and human erythrocyte membranes. In these three systems, tested compounds scavenge superoxide anion radicals or inhibit lipid peroxidation in a concentration-depen...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138807
更新日期:1991-01-01 00:00:00