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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
|
| pubmed:dateCreated |
1981-8-27
|
| pubmed:abstractText |
The serotonergic receptor antagonist 3-(2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl)-2,4-[1H,3H]quinazolinedione Ketanserin (R 41 468) caused a dose-dependent inhibition on the contractile responses to 5-hydroxytryptamine of isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, canine gastrosplenic veins (threshold 10(-10)-10(-9) M) and canine saphenous veins (threshold 10(-8) M). In concentrations up to 2.5 X 10(-5) M, it did not have agonistic properties. From 10(-8) M on, R 41 468 inhibited the contractions of rat caudal arteries and canine saphenous veins caused by postjunctional alpha adrenergic activation. In the rat caudal artery, R 41 468, in concentrations which did not affect the contractile response to norepinephrine, abolished the amplifying effect of low concentrations of 5-hydroxytryptamine on alpha adrenergic activation. In the canine saphenous vein, R 41 468 did not affect the prejunctional inhibitory effect of 5-hydroxytryptamine during sympathetic nerve stimulation. In the perfused guinea-pig stomach, R 41 468 depressed and in certain experiments reversed the vasoconstrictor response to 5-hydroxytryptamine. In isolated perfused kidneys from both normotensive and spontaneously hypertensive rats, R 41 468, in concentrations which did not depress vasoconstrictor responses to exogenous norepinephrine, inhibited those to 5-hydroxytryptamine. The compound caused a dose-related reduction in aortic blood pressure in unanesthetized spontaneously hypertensive rats, which was larger and occurred at lower concentrations, than in control animals. These results demonstrate that R 41 468 is a potent antagonist of the vasoconstrictor effects of 5-hydroxytryptamine, in particular of its amplifying effect on threshold amounts of norepinephrine, which may help explain its antihypertensive properties.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Ketanserin,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jul
|
| pubmed:issn |
0022-3565
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
218
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
217-30
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:6113280-Adrenergic alpha-Agonists,
pubmed-meshheading:6113280-Animals,
pubmed-meshheading:6113280-Arteries,
pubmed-meshheading:6113280-Blood Pressure,
pubmed-meshheading:6113280-Calcium,
pubmed-meshheading:6113280-Dogs,
pubmed-meshheading:6113280-Guinea Pigs,
pubmed-meshheading:6113280-Hypertension,
pubmed-meshheading:6113280-Ketanserin,
pubmed-meshheading:6113280-Kidney,
pubmed-meshheading:6113280-Male,
pubmed-meshheading:6113280-Muscle, Smooth, Vascular,
pubmed-meshheading:6113280-Norepinephrine,
pubmed-meshheading:6113280-Organ Specificity,
pubmed-meshheading:6113280-Piperidines,
pubmed-meshheading:6113280-Rats,
pubmed-meshheading:6113280-Serotonin Antagonists,
pubmed-meshheading:6113280-Species Specificity,
pubmed-meshheading:6113280-Stomach,
pubmed-meshheading:6113280-Vasoconstriction,
pubmed-meshheading:6113280-Veins
|
| pubmed:year |
1981
|
| pubmed:articleTitle |
Vascular effects of ketanserin (R 41 468), a novel antagonist of 5-HT2 serotonergic receptors.
|
| pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|