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A Possible Therapeutic Role for Adenosine During Inflammation

Phase 1
Completed
Conditions
Endotoxemia
Interventions
Genetic: AMPD1 polymorphism
Drug: placebo
Registration Number
NCT00513110
Lead Sponsor
Radboud University Medical Center
Brief Summary

The adenosine receptor is known for its anti-inflammatory actions and could therefore be a potential target in the treatment of sepsis and septic shock. Stimulation of the adenosine receptor could potentially lead to a decrease in inflammation and tissue damage.

Under normal conditions adenosine is formed either by an intracellular 5'nucleotidase, which dephosphorylates AMP, or by the hydrolysis of S-adenosylhomcysteine by hydrolase. An alternative pathway of AMP degradations is provided by the cytosolic enzyme AMP deaminase (AMPD), which catalyses the irreversible deamination of AMP to inosine monophosphate and ammonia.

In humans four AMPD isoforms have been described, named after the source from which they were initially purified; M (muscle), L (liver), E1 and E2 (erythrocyte), encoded by AMPD1, AMPD2 and AMPD3. Approximately 15-20% of Caucasian and African American individuals are heterozygous or homozygous for the 34C\>T variant of AMPD1.

We hypothesize that healthy volunteers who have the polymorphism for AMPD1 have a less severe inflammatory response to LPS and show less (severe) organ failure. This hypothesis is based on the expected higher levels of adenosine in patients with the AMPD1 polymorphism. This hypothesis is strengthened by the fact that patients with coronary artery disease and the AMPD1 polymorphism show improved cardiovascular survival (Anderson JL et al. J Am Coll Cardiol 2000; 36: 1248-52) possibly based on higher adenosine levels by reduced AMPD activity. Furthermore the polymorphism predicts improved clinical outcome in patients with heart failure (Loh E et al. Circulation 1999) also based on a hypothetical elevation of adenosine.

We hypothesize that:

The C34T-polymorphism of the enzyme AMP-deaminase leads to a decreased inflammatory respons and thereby a decrease of LPS-induced tissue damage.

A second hypothesis is based on the antagonism of the adenosine receptor, by caffeine;

Antagonism of the adenosine receptor by caffeine leads to an increased LPS-induced inflammatory reaction and an increase in (subclinical) tissue damage?

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
33
Inclusion Criteria
  • Healthy male volunteers
Exclusion Criteria
  • Drug-, nicotine-, alcohol abuses
  • Tendency towards fainting
  • Relevant medical history

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
1AMPD1 polymorphismEndotoxin and AMPD1 polymorphism
2Caffeine infusionEndotoxin and intervention with caffeine
3placeboEndotoxin combined with placebo
Primary Outcome Measures
NameTimeMethod
Hemodynamics; heart rate variability24 hrs after LPS administration
Markers of Inflammation24 hrs after LPS administration
Cytokines24 hrs after LPS administration
Sensitivity to norepinephrine24 hrs after LPS administration
Endothelial-dependent and independent vasorelaxation24 hrs after LPS administration
Mediators of Vascular reactivity24 hrs after LPS administration
Markers of endothelial damage and circulating endothelial cells24 hrs after LPS administration
Urinary excretion of markers of renal injury24 hrs after LPS administration
Neurologic testing24 hrs after LPS administration
Adenosine and related nucleotide concentrations.24 hrs after LPS administration
Additional blood samples will be drawn for measurement of: TLR-expression, Genetics; micro array analyses and determination of intercellular signalling pathways.24 hrs after LPS administration
Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

Radboud University Nijmegen Medical Centre

🇳🇱

Nijmegen, Gelderland, Netherlands

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