Abstract:
:The insulinogenic response to a standard i.v. dose of a sulfonylurea can be markedly augmented in normal, conscious dogs if they are given 30 min earlier a single i.v. dose of dihydroergotamine (DHE). Since the parent substance ergotamine posssed no such amplifying properties, further experiments were conducted to clarify the essential structural requirements that have to be fulfilled for an ergot alkaloid to act as an amplifier of sulfonylurea-stimulated insulin secretion. Amine alkaloids ergonovine, dihydroergonovone and dihydromethylergonovine had no amplifying potency, but the hydrogenated amino acid alkaloids dihydroergocornine, dihydroergocristine and dihydroergokryptine (Hydergine) were almost as potent amplifiers as was DHE. The data indicate that (a) DHE, Hydergine and by inference all hydrogenated amino acid alkaloids are potent amplifiers of sulfonylurea-stimulated insulin secretion; (b) saturation of the double bond at C9 and C10 of the lysergic acid moiety and the pressence of an amino acid side chain are essential structual requirements for an ergot alkaloid to function as an amplifier of the action of sulfonylureas; and (c) it appears that these compounds are acting chiefly by mechanisms other than alpha-adrenergic and serotonergic receptor blockade, perhaps as regulatory molecules inducing positive cooperative changes in integral proteins of the plasma membrane of beta cells.
journal_name
Pharmacologyjournal_title
Pharmacologyauthors
Sirek A,Sirek OV,Policova Z,Kerekes Adoi
10.1159/000136697subject
Has Abstractpub_date
1977-01-01 00:00:00pages
259-67issue
3eissn
0031-7012issn
1423-0313journal_volume
15pub_type
杂志文章相关文献
PHARMACOLOGY文献大全abstract:BACKGROUND/AIMS:Serotonin (5-hydroxytryptamine, 5-HT)-induced contraction and the involvement of RhoA/Rho-kinase pathway in the 5-HT-induced contraction was investigated isometrically in vitro in both diabetic and nondiabetic human corpus cavernosum (HCC) tissues. METHODS:HCC tissues were obtained from 12 patients. Th...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000221380
更新日期:2009-01-01 00:00:00
abstract::The metabolism of sennosides is discussed in view of the results obtained during the last years. Rhein anthrone is to be considered as the ultimate active form produced by microorganisms in the colon. Several contributions of this senna symposium bring complementary information of utmost interest. ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138431
更新日期:1988-01-01 00:00:00
abstract::In the present paper, two experiments are performed to test the efficacy of the intravenous administration of hypertonic glucose (25 or 50%) in alcoholic intoxication. In a first experiment, 10 healthy, nonstarved volunteers, received 15 min after the ingestion of 1.0 g/kg alcohol, 40 ml of 25% glucose i.v., the same ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137769
更新日期:1983-01-01 00:00:00
abstract::The oral bioavailability of two investigational formulations of bicalutamide was compared with the current clinical formulation. The first formulation was amorphous R-/S-bicalutamide in solid dispersion with a polymeric matrix of hydroxypropyl methylcellulose phthalate (HP55S) (R-/S-bicalutamide/HP55S); the second was...
journal_title:Pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1159/000094599
更新日期:2006-01-01 00:00:00
abstract::Sarcopenia is a geriatric syndrome characterized by progressive and generalized loss of skeletal muscle mass and function. Reported prevalence of this geriatric syndrome, differs depending on the definition, the population and the method used to identify sarcopenia. The causes of sarcopenia are multifactorial, and can...
journal_title:Pharmacology
pub_type: 杂志文章,评审
doi:10.1159/000448247
更新日期:2017-01-01 00:00:00
abstract::Anoxia has been shown to potentiate the constrictor effects of 5-hydroxytryptamine (5HT) in isolated vascular tissue. In the present study, canine coronary arterial rings were incubated with various treatments and exposed to 5HT (4 X 10(-7) M) and anoxia (95% N2 and 5% CO2). Developed tension was increased by 250 +/- ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138211
更新日期:1986-01-01 00:00:00
abstract::Erythrocytes can take up amino acids from the blood by using a variety of transport systems. GLYT is a key transport protein in the plasma membrane responsible for the Na(2+)-dependent uptake of glycine needed for glutathione biosynthesis. Certain cysteine-specific compounds, particularly mercuric chloride and 5,5'-di...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000074973
更新日期:2004-03-01 00:00:00
abstract::The pathogenesis of aplastic anemia from chloramphenicol (CAP) remains uncertain. Recent observations suggest that metabolites of CAP generated by intestinal bacteria may play an important role in mediating hematotoxicity from the drug. Thus, it is possible that once in circulation and after passage through the liver,...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138394
更新日期:1988-01-01 00:00:00
abstract::In anesthetized rats the glucose release of the kidneys was estimated from the glucose concentrations in the arterial and renal venous plasma, urinary glucose excretion and the total renal plasma flow. Net renal glucose release was found in control experiments. The glucose release of the kidneys decreased with rising ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136914
更新日期:1975-01-01 00:00:00
abstract:AIM:Superfluous reactive nitrogen and oxygen species generation is implicated in the damage of tissues at sites of inflammation where activated neutrophils and macrophages are involved. This study was conducted to investigate whether the beneficial effects of carvedilol involve modulation of respiratory burst, degranul...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000097818
更新日期:2007-01-01 00:00:00
abstract::Interferons are known to prevent liver collagen by an antifibrogenic mechanism that involves mRNA procollagen regulation. The aim of the present work was to determine whether interferon could also decrease collagen by increasing its degradation. Fibrosis was induced in male Wistar rats by double ligation and section o...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139345
更新日期:1995-12-01 00:00:00
abstract::The marijuana plant Cannabis sp. and its derivatives and analogues, known as cannabinoids (CBs), induce many effects throughout the whole body. Herein we briefly review the gastrointestinal (GI) pharmacology of CBs, with special focus on motor function. Some drugs are available to treat nausea and emesis, and evidence...
journal_title:Pharmacology
pub_type: 杂志文章,评审
doi:10.1159/000339072
更新日期:2012-01-01 00:00:00
abstract::Exposure of rat portal veins to an N2-gassed buffer markedly increased 86Rb outflow. Moreover, glucose caused a pronounced reduction in 86Rb outflow from portal veins perfused with an N2-gassed buffer. Pinacidil, cromakalim and diazoxide provoked a sustained increase in 86Rb outflow. The stimulatory effect of pinacidi...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138878
更新日期:1992-01-01 00:00:00
abstract::Previously published data from this laboratory on the urinary excretion of 3-hydroxymethyl antipyrine (one of the major metabolites of antipyrine in man) have to be reconsidered, because of use of an impure reference substance in the high-pressure liquid chromatographic assay method. Comparison with newly synthesized,...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137594
更新日期:1982-01-01 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::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::Five healthy subjects performed submaximal physical exercise approximately 20 h after a single oral dose of phenytoin (5 mg/kg of the sodium salt). The plasma levels of free fatty acids (FFA) increased 2- to 3-fold in the post-exercise period. In spite of this, the degree of plasma binding of phenytoin and its total c...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136744
更新日期:1978-01-01 00:00:00
abstract::Previous studies have indicated that structurally dissimilar serotonin2 (5HT2) antagonists can protect globally ischemic/reperfused reperfused rat hearts. We therefore determined if the 5HT2 antagonist cinanserin can protect the ischemic myocardium in two models of pacing-induced ischemia in anesthetized dogs. In one ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139294
更新日期:1995-05-01 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:BACKGROUND/AIM:Perception of risk of adverse drug events (ADEs) is different between health and nonhealth professionals, but these differences have not been investigated sufficiently in the general population. Women are more affected by ADEs. With the aim to investigate ADE risk perception in a sample of nonhealth prof...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000346737
更新日期:2013-01-01 00:00:00
abstract::The present study was designed to investigate the effects of fluid administration on survival in endotoxemic or septicemic male Sprague-Dawley rats. Endotoxemia was induced by intravenous injection of Escherichia coli lipopolysaccharide (LPS), and septicemia produced by cecal ligation and puncture (CLP). In endotoxemi...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139053
更新日期:1993-05-01 00:00:00
abstract:BACKGROUND/AIMS:Putative in vitro-in vivo correlations of pharmacokinetic (PK) parameters are regarded as a prerequisite to filter hits derived from high-throughput screening (HTS) approaches for subsequent murine in vivo PK studies. METHODS:In this study, we assessed stabilities in rat and human microsomes of 121 com...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000343241
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Surgery plays a significant role in the comprehensive treatment of breast cancer, and opioids are often the first-choice analgesics in the perioperative period. However, recent studies showed that opioids may enhance the angiogenesis of breast cancer and the recurrence and metastasis of tumor cells. OBJECTI...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000502107
更新日期:2019-01-01 00:00:00
abstract::We studied the anti-inflammatory activity of meloxicam on rat carrageenin-induced pleurisy and its toxicity for rat gastric mucosa, relative to its in vitro inhibitory potency against partially purified cyclooxygenase (COX)-1 and COX-2 preparations in order to clarify the pharmacological profile of the compound as an ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139511
更新日期:1997-07-01 00:00:00
abstract::Serum protein binding and serum levels of antipyrine, phenytoin and phenylbutazone were measured in rabbits with acute renal failure induced by uranyl nitrate. The kinetics of antipyrine are not altered in the uraemic rabbit. Serum protein binding of phenytoin and phenylbutazone is decreased and the volume of distribu...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136871
更新日期:1978-01-01 00:00:00
abstract::The influence of hyperthyroidism on the functional vascular responsiveness of isolated coronary and renal resistance vessels was investigated. Hyperthyroidism was established by feeding rats for 1 and 4 weeks with 5 mg/kg L-thyroxine (T4)-containing rat chow. Preparations of either coronary or renal resistance vessels...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139519
更新日期:1997-09-01 00:00:00
abstract::Vascular dementia (VaD) is the second most common type of dementia and has become a major public health challenge as the global population ages. VaD is caused by cerebrovascular disease, and most patients with VaD have been reported to also have Alzheimer's pathologies, which is the formation of neurofibrillary tangle...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000504056
更新日期:2020-01-01 00:00:00
abstract::The observations that people infected with HIV suffer not only from an inflammatory stress but also from depleted glutathione levels have led to a general hypothesis that these two are causally related, and that treatment of AIDS should include thiol-replenishment therapy. In particular, inflammatory stimulations are ...
journal_title:Pharmacology
pub_type: 杂志文章,评审
doi:10.1159/000139037
更新日期:1993-01-01 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::In the present study, chronic treatment of atorvastatin was evaluated on isoproterenol-induced myocardial infarction. Male Sprague-Dawley rats (200 +/- 25 g) were randomized into the following four groups: (1) control group, (2) isoproterenol-treated group, (3) atorvastatin-treated group, and (4) isoproterenol- and at...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000092308
更新日期:2006-01-01 00:00:00