Abstract:
:High-affinity (104 +/- 18 pmol/l) and high-density (204 +/- 25 fmol/mg) angiotensin II (AII) binding sites have been identified in Xenopus laevis heart membranes. Competition binding of [125I]Sar1,Ile8 angiotensin (SIA) to these receptors by peptide analogs selective for the mammalian AII receptor subtypes AT1 and AT2 suggested that the amphibian AII binding sites were more closely related to the AT1 receptor subtype. Also in common with AT1 receptors, dithiothreitol and GTP gamma S inhibited [125I]SIA binding to Xenopus heart receptors, exhibiting IC50 values of 600 and 0.95 mumol/l, respectively. In addition, Xenopus oocytes injected with Xenopus heart mRNA were capable of mobilizing calcium when exposed to AII, demonstrating that Xenopus AII receptors are functionally linked to a second-messenger system similar to that coupled to mammalian AT1 receptors. However, in contrast to both AT1 and AT2 receptor subtypes, nonpeptide antagonists DUP 753 and SK&F 108566 (AT1 receptor selective) and PD123319 (AT2 selective) did not bind the Xenopus AII receptors, thus establishing that the amphibian receptors were pharmacologically unique. Together, these results demonstrate that Xenopus heart AII receptors are functionally similar to mammalian AT1 receptors but are pharmacologically distinct from both AT1 and AT2 receptors.
journal_name
Pharmacologyjournal_title
Pharmacologyauthors
Aiyar N,Baker E,Pullen M,Nuthulaganti P,Bergsma DJ,Kumar C,Nambi Pdoi
10.1159/000139186subject
Has Abstractpub_date
1994-04-01 00:00:00pages
242-9issue
4eissn
0031-7012issn
1423-0313journal_volume
48pub_type
杂志文章相关文献
PHARMACOLOGY文献大全abstract::When rat mast cells were cultured for a short period in plastic dishes and adhering cells were permeabilized with beta-escin and exposed to Ca2+ at concentrations higher than 10(-7) mol/l, histamine release was induced dose-dependently. Protein kinase C (PKC) activity in the crude extracts obtained from adhering mast ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138874
更新日期:1992-01-01 00:00:00
abstract::The effect of age on the clearance (CL) of therapeutic proteins has not been explored extensively in pediatric subjects. Recently, resting energy expenditure (REE) has been proposed to link age-dependent CL with developmental changes. Allometric relationship was explored to assess the impact of REE on the CL of therap...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000362562
更新日期:2014-01-01 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::Incubation of rat brain homogenates or 14,500 g pellet isolated from the homogenate with (14C)-mescaline was associated with accumulation of (14C)-mescaline in the pellet. 1.33 mumol/ml of chlorpromazine, trifluoperazine, fluphenazine, imipramine, desmethylimipramine, nortriptyline and amitriptyline inhibited the accu...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136916
更新日期:1975-01-01 00:00:00
abstract::The cardioprotective effects of (2S,3R,4S)-N'-benzyl- N"-cyano-N-(3,4-dihydro-2-dimethoxymethyl-3-hydro- xy-2-methyl-6-nitro-2H-benzopyran-4-yl)-guanidine (KR-31372) were evaluated against ischemic/reperfusion injury in isolated rat hearts in vitro and in anesthetized rats and dogs in vivo. In isolated perfused rat he...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000074671
更新日期:2004-02-01 00:00:00
abstract::Peroxisome proliferator-activated receptor-gamma (PPARgamma) is a nuclear receptor that regulates lipid metabolism. Recently, PPARgamma was reported to be a negative regulator in the immune system. Eosinophils also express PPARgamma, however, the role of PPARgamma in eosinophil functions is not well understood. Surfac...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000085034
更新日期:2005-07-01 00:00:00
abstract::Various new butyridenyl-2-hydroxybenzylidenyl-1,3-thiazolidinones were synthesized and characterized by elemental analyses, IR and PMR spectral data. The compounds were evaluated for their ability to afford protection against inflammation by carrageenin-induced oedema and cotton pellet implantation in albino rats of e...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138130
更新日期:1985-01-01 00:00:00
abstract::The possible role of carbonic anhydrase in bone resorption induced by prostaglandin E2 (PGE2) was studied using an in vitro neonatal mouse calvarial culture system. PGE2 (10(-6) M) was effective in stimulating resorption, as assessed by calcium release into culture media. This enhanced resorption was accompanied by si...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138088
更新日期:1985-01-01 00:00:00
abstract::The systemic and coronary hemodynamic effects of the nitrovasodilator, pirsidomine, were compared with SIN-1, nitroprusside, and nitroglycerin. Four groups consisting of 32 experiments were performed in 17 conscious dogs chronically instrumented for measurement of aortic and left ventricular pressure, left ventricular...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139372
更新日期:1996-02-01 00:00:00
abstract::The effects of some ergot derivatives on the electroencephalogram and behavior of laboratory animals (mice, rats, rabbits) have been surveyed. The interference of bromocriptine on the dopaminergic central systems has been studied using behavioral (interference with the effects induced by L-dopa, 5HT, TRF or neurolepti...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136819
更新日期:1978-01-01 00:00:00
abstract:OBJECTIVE:The aim of this study was to investigate the effects of trichostatin A (TSA) on cervical cancer and the related mechanisms. METHODS:The HeLa and Caski cervical cancer cell lines were treated with different concentrations of TSA. Cell viability was measured by MTT assays. Cell apoptosis was analysed using flo...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000507937
更新日期:2020-11-03 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::In a three-phase study, single oral doses of placebo, followed in 1 week by pyrazinoylguanidine (PZG; 900 mg), followed in 3 weeks by pyrazinoic acid (PZA; 300 mg) were given to 8 normal male subjects. Blood analyses performed 0, 2 and 4 h after administration of placebo or drug revealed that compared to mean 0 h valu...
journal_title:Pharmacology
pub_type: 临床试验,杂志文章
doi:10.1159/000028276
更新日期:1999-03-01 00:00:00
abstract::The aim of the present study was to compare the cardioprotective properties of long-acting calcium channel antagonist pranidipine with amlodipine in rat model of heart failure induced by autoimmune myocarditis. Twenty-eight days after immunization the surviving rats were randomized for the oral administration of low-d...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000091746
更新日期:2006-01-01 00:00:00
abstract:AIM:The purpose of the present study was to examine the effects of acetaldehyde on the contractile force and membrane potentials and currents in the bullfrog heart. METHODS:Contractile force was recorded using right atrial tissues, and membrane potentials and currents were measured by using whole cell patch clamp meth...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000342388
更新日期:2012-01-01 00:00:00
abstract::This study tests the hypothesis that contractile responses in aortae of hypertensive rats are more dependent on gap junctional communication compared to those from normotensive rats. The experimental approach was pharmacological, using inhibitors of gap junctional activity (heptanol and octanol). Two models of experim...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000056069
更新日期:2001-01-01 00:00:00
abstract::The absorption into the systemic circulation of compounds administered intraperitoneally in large volumes was investigated in the rat. The influence on absorption of molecular weight, lipid-water partition coefficient (K), and dissociation constant (pKa) was studied. Nine neutral compounds ranging in molecular weight ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136874
更新日期:1978-01-01 00:00:00
abstract::The purpose of the study was to test the hypothesis that the postischemic neuronal damage is accompanied by changes of the electrocorticogram (ECoG) of freely moving rats during long-term recovery after forebrain ischemia. Ten minutes forebrain ischemia was induced in male Wistar rats. ECoG was recorded 1 day before a...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139287
更新日期:1995-04-01 00:00:00
abstract::Noradrenergic neurotransmission in the electrically stimulated isolated splenic strip of the cat was found to be modulated via opiate receptor. Pharmacodynamic parameters of morphine, methionine-enkephalin, azidomorphine, naloxone and N-cyclopropylmethyl-norazidomorphine (CAM) were determined. As CAM proved to be more...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137467
更新日期:1981-01-01 00:00:00
abstract::Metabotropic G protein-coupled receptors have recently been recognized as targets for anesthetics and analgesics. In particular, G(q)-coupled receptors such as muscarinic M(1) receptors (M(1)R) and 5-hydroxytryptamine (5-HT) type 2A receptors have been reported to be targets for anesthetics. Much less is known, howeve...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000080106
更新日期:2004-11-01 00:00:00
abstract::The radioligand binding profiles and in vivo pharmacological characteristics of YM-44781, YM-44778 and YM-49598, novel non-peptide tachykinin receptor antagonists, were examined and compared to those of FK-888 and GR-159897. Since no functional NK(3) receptors were found in the rat bladder, the emphasis will be on the...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000056193
更新日期:2002-05-01 00:00:00
abstract:BACKGROUND/AIMS:The in vivo metabolic profile of a benzopyridooxathiazepine (BPT) derivative, a potent tubulin polymerization inhibitor with a promising in vitro activity, was investigated. METHODS:The quantification of the BPT derivative and the identification of metabolites in the plasma of Wistar rats after i.p. an...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000368084
更新日期:2014-01-01 00:00:00
abstract::Sensitive radiometric assays were adapted to study the development and kinetics of meperidine and methadone N-demethylation and morphine glucuronidation by microsomes isolated from livers of fetal stump-tailed macaques (Macaca arctoides). Times in development selected for study were midterm, three-quarter term, near t...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137259
更新日期:1979-01-01 00:00:00
abstract::This study was designed to evaluate the antidepressant activity of various antidepressants using the learned helplessness test (LH) or the forced swimming test (FS) in rats. Repeated treatment of the tricyclic antidepressants imipramine (10 mg/kg, p.o.), clomipramine (0.625 mg/kg, p.o.), amitriptyline (10 mg/kg, p.o.)...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000056126
更新日期:2001-01-01 00:00:00
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...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000335127
更新日期:2012-01-01 00:00:00
abstract::The vasodepressor responses to intravenous injections of arachidonic acid, and the formation of its metabolites, were studied in rats made diabetic 1 or 2 weeks after a 1-dose alloxan treatment. Arachidonic acid dose-dependently decreased the diastolic blood pressure in normal animals, but this hypotensive effect was ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138612
更新日期:1989-01-01 00:00:00
abstract::Double-stranded, RNA-dependent protein kinase R (PKR) is a serine/threonine protein kinase activated by various stress signals. It plays an important role in inflammation, insulin sensitivity and glucose homeostasis. Increased PKR activity has been observed in obese humans as well as in obese diabetic mice. Indirubin-...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000441727
更新日期:2016-01-01 00:00:00
abstract::The effects of several paired analogs of angiotensin II and angiotensin III, designed as antagonists, have been compared in isolated smooth muscle (rat uterus) and by in vivo rat blood pressure assay. These analogs were (1) the angiotensin II series: (1-sarcosine, 7-X, 8-isoleucine-) angiotensin II, and (2) the angiot...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137342
更新日期:1980-01-01 00:00:00
abstract::The first step in the conversion of spironolactone (SP) to its biologically active metabolites is deacetylation to 7 alpha-thiospirolactone (7 alpha-thio-SL). Studies were done to evaluate the effects of reduced glutathione (GSH) on SP deacetylation by adrenal microsomal preparations. In the absence of GSH, adrenal mi...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139358
更新日期:1996-01-01 00:00:00
abstract::Danthron infused intravenously in rats shows a complex dose-dependent pattern of metabolism and excretion. The metabolites, particularly the more polar ones, are in general excreted predominantly in bile, to a lesser extent in urine. They can be separated as metabolite groups according to polarity and molecular size o...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139852
更新日期:1993-10-01 00:00:00