Source:http://linkedlifedata.com/resource/pubmed/id/12023327
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
Pt 6
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pubmed:dateCreated |
2002-5-22
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pubmed:abstractText |
There is a considerable literature to suggest that adenosine A1 receptor agonists may have anti-nociceptive effects, and we sought to explore the role of adenosine A1 receptors in a model of trigeminovascular nociceptive transmission. Cats were anaesthetized (alpha-chloralose 60 mg/kg, intraperitoneally), and prepared for physiological monitoring. The superior sagittal sinus (SSS) was stimulated electrically, and linked units were recorded in the trigeminocervical complex. Post-stimulus histograms were constructed to analyse the responses and the effect of drug administration. Blood was sampled from the external jugular vein to determine levels of calcitonin gene-related peptide (CGRP) release before and after drug administration. Intravenous administration of the highly selective adenosine A1 receptor agonist, GR79236 (3-100 microg/kg) had a dose-dependent inhibitory effect on SSS-evoked trigeminal activity. The maximal effect (80 +/- 6% reduction in probability of firing) was seen at 100 microg/kg. The neuronal inhibitory effect of GR79236 could be inhibited by the selective adenosine A1 receptor antagonist DPCPX (300 microg/kg; P < 0.05). SSS stimulation increased cranial CGRP levels from 33 +/- 2 pmol/l (n = 6) to 64 +/- 3 pmol/l, an effect substantially reduced by pre-treatment with GR79236 (30 microg/kg; P < 0.01). The selective low efficacy adenosine A1 receptor agonist, GR190178 (30-1000 microg/kg i.v.), also inhibited SSS-evoked neuronal activity in a dose-dependent fashion. In this model of trigeminovascular nociception, adenosine A1 receptor activation leads to neuronal inhibition without concomitant vasoconstriction, suggesting a novel avenue for the treatment of migraine and cluster headache.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
AIM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/1,3-dipropyl-8-cyclopentylxanthine,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine,
http://linkedlifedata.com/resource/pubmed/chemical/N-((1S,trans)-2-hydroxycyclopentyl)a...,
http://linkedlifedata.com/resource/pubmed/chemical/Purinergic P1 Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Purinergic P1 Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Purinergic P1,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthines
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0006-8950
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
125
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1392-401
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:12023327-Adenosine,
pubmed-meshheading:12023327-Animals,
pubmed-meshheading:12023327-Blood Pressure,
pubmed-meshheading:12023327-Cats,
pubmed-meshheading:12023327-Dose-Response Relationship, Drug,
pubmed-meshheading:12023327-Heart Rate,
pubmed-meshheading:12023327-Neural Inhibition,
pubmed-meshheading:12023327-Pain Measurement,
pubmed-meshheading:12023327-Purinergic P1 Receptor Agonists,
pubmed-meshheading:12023327-Purinergic P1 Receptor Antagonists,
pubmed-meshheading:12023327-Receptors, Purinergic P1,
pubmed-meshheading:12023327-Synaptic Transmission,
pubmed-meshheading:12023327-Trigeminal Nuclei,
pubmed-meshheading:12023327-Xanthines
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pubmed:year |
2002
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pubmed:articleTitle |
Adenosine A1 receptor agonists inhibit trigeminovascular nociceptive transmission.
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pubmed:affiliation |
Headache Group, Institute of Neurology, Queen Square, London, UK. peterg@ion.ucl.ac.uk
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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