rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1984-2-24
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pubmed:abstractText |
The selectivity of 4-methylhistamine (4-MH) as an agonist at histamine H1- and H2-receptors has been evaluated in the guinea-pig isolated ileum. The EC50 values of 4-MH on H1- and H2-receptors that mediate contractile responses were determined. The EC50 at H1-receptors was estimated after selective blockade of H2-receptors by tiotidine and the EC50 at H2-receptors estimated after selective blockade of H1-receptors by mepyramine. The -log EC50 values at H1- and at H2-receptors were 4.57 and 5.23, respectively. The dissociation constants for the interaction of 4-MH with H1- and H2-receptors were determined. The -log KD values at H1- and H2-receptors were 3.55 and 4.27, respectively. These results suggest that 4-MH is only about 5 times as potent at H2- as it is at H1-receptors in the guinea-pig ileum and that 4-MH should be used with caution to discriminate between H1- and H2-receptors.
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pubmed:grant |
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pubmed:commentsCorrections |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/4-methylhistamine,
http://linkedlifedata.com/resource/pubmed/chemical/Dibenzylchlorethamine,
http://linkedlifedata.com/resource/pubmed/chemical/Dimaprit,
http://linkedlifedata.com/resource/pubmed/chemical/Methylhistamines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine H1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Histamine H2,
http://linkedlifedata.com/resource/pubmed/chemical/Thiourea
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0007-1188
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:volume |
80
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
65-71
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:6228278-Animals,
pubmed-meshheading:6228278-Dibenzylchlorethamine,
pubmed-meshheading:6228278-Dimaprit,
pubmed-meshheading:6228278-Drug Interactions,
pubmed-meshheading:6228278-Female,
pubmed-meshheading:6228278-Guinea Pigs,
pubmed-meshheading:6228278-Ileum,
pubmed-meshheading:6228278-Male,
pubmed-meshheading:6228278-Methylhistamines,
pubmed-meshheading:6228278-Muscle, Smooth,
pubmed-meshheading:6228278-Muscle Contraction,
pubmed-meshheading:6228278-Receptors, Histamine,
pubmed-meshheading:6228278-Receptors, Histamine H1,
pubmed-meshheading:6228278-Receptors, Histamine H2,
pubmed-meshheading:6228278-Thiourea
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pubmed:year |
1983
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pubmed:articleTitle |
Selectivity of 4-methylhistamine at H1- and H2-receptors in the guinea-pig isolated ileum.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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