Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0432222 (SEM)
 47,337 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Effects of purine nucleosides and asthma mediators on airway tone have been examined in the guinea-pig isolated perfused lung preparation. Acetylcholine (10 pmol-0.3 nmol), histamine (1-10 nmol), adenosine (10 nmol-0.3 mumol), ATP (10 nmol-0.3 mumol) and inosine (10 mumol-0.1 mmol) all produced a dose dependent increase in lung resistance (RL) and a decrease in dynamic compliance (CDYN). ATP was equipotent with adenosine whereas inosine was about 500 times less potent. The adenosine-induced bronchoconstriction was affected neither by disodium cromoglycate (150 microM) nor by the histamine H1-receptor antagonist, mepyramine (1 microM) suggesting that histamine is not involved in this response. Furthermore, it was studied whether the xanthines theophylline and enprofylline specifically interacted with the adenosine induced bronchoconstriction. Theophylline significantly (P less than 0.01-0.001) and concentration dependently prevented both acetylcholine and adenosine-induced increase in RL. The response to 0.1 nmol acetylcholine was reduced by 32.8 +/- 8.4% (mean +/- SEM) and 58.1 +/- 4.0%, respectively, by 75 and 150 microM theophylline. Theophylline, 75 and 150 microM, also inhibited the increase in RL caused by 0.1 mumol of adenosine by 61.4 +/- 9.6% and 83.4 +/- 5.2%, respectively. Theophylline, was significantly (P less than 0.05-0.01) more potent in preventing the RL increase produced by adenosine than that by acetylcholine. Enprofylline, 30 microM, equally well as 75 microM theophylline reduced the acetylcholine-induced bronchoconstriction by 41.8 +/- 7.6% (P less than 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Adenosine-induced bronchoconstriction in the guinea-pig isolated lung: interaction with theophylline and enprofylline. 298 Feb 92

Eight asthmatic out-patients with a history of exercise-induced asthma (EIA) were randomly treated with intravenously administered enprofylline 1.5 mg/kg b.wt., theophylline 5 mg/kg b.wt., and placebo immediately prior to a 6-min exercise provocation in this double-blind crossover comparison. A reduction in peak flow of more than 20% was seen in all patients after placebo pre-treatment. Mean plasma concentrations at the start of the exercise test were 3.3 mg/l and 13.2 mg/l after 20 min infusion of enprofylline and theophylline, respectively. The corresponding figures 25 min later were 2.3 and 11.7, respectively. Maximal fall in peak expiratory flow (PEF) after exercise in percent of pre-exercise PEF was 49% +/- 6% (mean +/- SEM), 39% +/- 6% and 24% +/- 5% after infusion of placebo, enprofylline, and theophylline, respectively. Theophylline produced a statistically significant better protection against EIA compared to enprofylline and placebo. Enprofylline produced a slight protection from EIA not statistically significantly different from placebo.
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PMID:Effects of enprofylline and theophylline on exercise-induced asthma. 390 95

Enprofylline, a new potent bronchodilator xanthine drug, was given orally as an aqueous solution to 6 healthy subjects in single doses of 2, 4 and 6 mg/kg. The two lower doses produced plasma concentrations in the range 1-4 mg/l, i.e. in the assumed "therapeutic interval" according to previous animal studies. A high 24 h urine recovery of unchanged drug, with mean values for the three dose levels ranging from 85 to 91% of the given dose, indicated good absorption and little metabolism. The dose-corrected area under the plasma concentration-time curve rose with dose as the latter was increased from 2 to 6 mg/kg. This indicates that the elimination of enprofylline is capacity-limited at high doses. Double peaks in the plasma concentration-time curves at the higher dose levels suggested intermittent and delayed gastric emptying as a possible explanation. This hypothesis was confirmed by studies in 6 other healthy subjects, who received the drug solution by three different routes; by mouth, via a catheter in the duodenum, and rectally via a catheter in the colon. The corresponding time to peak values (mean +/- SEM) were 32.5 +/- 8.7, 13.3 +/- 2.5, and 157 +/- 23 min.
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PMID:Absorption of enprofylline from the gastrointestinal tract in healthy subjects. 651 Apr 61