Search results for "Histamine"
showing 10 items of 254 documents
Cost-Effectiveness Analysis: Stress Ulcer Bleeding Prophylaxis with Proton Pump Inhibitors, H2 Receptor Antagonists
2012
Abstract Objectives Proton pump inhibitors (PPIs) and H2-receptor antagonists (H2RAs) present varying pharmacological efficacy in preventing stress ulcer bleeding (SUB) in intensive care units. The literature also reports disparate rates of ventilator-assisted pneumonia (VAP) as side effects of these treatments. We compared the cost-effectiveness of these two prophylactic pharmacological options. Methods We constructed a decision tree with a 60-day time horizon for patients at high risk for developing SUB, receiving either PPIs or H2RAs. For each treatment strategy, patients could be in one of three states of health: SUB, VAP, or no complication. Contemporary, clinically relevant probabilit…
Histamine analogues. 32nd communication: synthesis and pharmacology of sopromidine, a potent and stereoselective isomer of the achiral H2-agonist imp…
1989
Abstract Synthesis and pharmacology of sopromidine (( R )-7) and ( S )- 7 , 2 position isomers of impromidine derived from the enantiomeric α-methylhistamines, are reported. The enantiomers of 7 show high stereoselectivity at the atrial H 2 -receptor of the guinea-pig. ( R )- 7 is revealed to be a full H 2 -agonist with 7.4-fold potency relative to histamine, while ( S )- 7 is a competitive H 2 -antagonist.
Structure-activity relationship of histamine H2-receptor agonists
1978
As demonstrated by the results the active C-5(4) substituted histamines and Nα-methyl-histamines are to various extents selective H2-receptor agonists.
Analgesic Activity and Effects on Isolated Smooth Muscle of Different Fractions of Hexane Extract fromAraujia sericifera Brot
1996
The present study analyses the analgesic activity and action on in vitro motility of methanol soluble and methanol insoluble fractions obtained from the hexane extract of fruits from Araujia sericifera. The methanol fraction did not show any pharmacological activity on the different tests evaluated. However, the insoluble methanol fraction exhibited an interesting analgesic effect in models of chemical and thermal stimulus and it reduced the E max induced by histamine in vitro on guinea-pig ileum. This extract lacked any central depressor activity since it did not modify the number of mouse movements in the activity cage.
In vitro studies of methanol and dichloromethanol extracts ofJuniperus oxycedrus L.
1997
The present study evaluated the effect of methanol and dichloromethanol extracts obtained from the leaves and stems of Juniperus oxycedrus against neurotransmitter-induced contraction in different isolated tissues of rats and guinea-pigs. Diverse concentrations of these extracts inhibit the concentration curve response to histamine, serotonin and acetylcholine. These results contribute to explaining the use of this plant in folk medicine. © 1997 John Wiley & Sons, Ltd.
Pharmacological evaluation of the dichloromethanol extract fromInula crithmoides L.
1995
The pharmacological effect of the dichloromethanol extract of Inula crithmoides L. was analysed in in vitro and in vivo models. The extract dose-dependently decreased arterial blood pressure and furthermore it showed low acute toxicity, CNS depressor activity and analgesic and antiinflammatory effects. Preincubation of the guinea-pig ileum and rat duodenum (100 μg/mL) produced a significant reduction in the contractile effects of histamine and acetylcholine and a concentration-related inhibition of the effects of serotonin. Following further fractionation the methylene chloride/acetone (50/50) fraction caused a significant decrease in motor activity and significantly reduced the threshold o…
H2-antihistaminics. 20. Structure-activity relationships in H2-receptor antagonists containing a 4-pyrimidone moiety.
1984
In a series of 5,6-substituted 4- pyrimidones 1 a-v the H2-antihistaminic activity was determined (guinea-pig atrium) and lipophilicity data are given in form of Rmo -values. The influence of different substituents at position 5 or 6 of a pyrimidone moiety has been studied. Quantitative structure-activity analyses showed the importance of lipophilicity for drug activity. Additionally other physicochemical substituent-properties may play a major role.
Antiinflammatory activity and effects on isolated smooth muscle of extracts from differentTeucrium species
1995
The present study analyses the antiinflammatory effects and the action on in vitro motility of methanol and dichloromethanol extracts and stems of four Teucrium species (T. flavum, T. cartaginenses, T. buxifolium and T. pumillum). The antiinflammatory activity was tested in the carrageenan-induced paw oedema in rats. T. flavum methanol (200 mg/kg, i.p.) and dichloromethanol (138 mg/kg, i.p.) extracts showed a significant anti-inflammatory effect through the 24 h experimental period and reduced the Emax induced by histamine and serotonin in vitro on guinea-pig ileum and rat uterus respectively. These extracts did not modify the contractile effects induced by acetylcholine on rat duodenum and…
Pharmacological screening of the methanol and dichloromethanol extracts ofGenista patens
1995
The pharmacological effects of the dichloromethanol and methanol extracts obtained from leaves and stems of Genista patens DC were analysed in in vitro and in vivo models. Both extracts showed low acute toxicity (LD 50 >3 g/kg), CNS depressor and antiinflammatory activity, and similar analgesic effect in models of chemical and thermal stimulation. Furthermore, the dichloromethanol extract (1-20 mg/kg) induced a pronounced dose-dependent decrease on blood pressure. On isolated organs, the dichloromethanol extract (1, 10, 100 μg/mL) shifted the concentration-effect curve to the right for ACh and reduced the E max induced by histamine without modifying responses induced by noradrenaline and se…
A pharmacological study ofAraujia sericifera B. extracts in rodents
1995
The present study analyses the pharmacological activity in in vitro and in vivo models of different extracts obtained from Araujia sericifera. The hexane extract of fruits lacked toxicity, but exhibited an analgesic effect in models of chemical and thermal stimulation. Such an extract was the only one which exhibited antiinflammatory actions. The intrinsic effect on arterial blood pressure was biphasic: at low doses it significantly increased blood pressure, whereas at high doses it exerted the opposite effect. On isolated organs it produced a marked decrease in the maximum effect of histamine and acetylcholine. The dichloromethanol extract of fruits decreased arterial pressure and the maxi…