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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1
|
| pubmed:dateCreated |
1998-3-11
|
| pubmed:abstractText |
Gamma-mangostin, purified from the fruit hull of the medicinal plant Garcinia mangostana caused a parallel rightwards shift of the concentration/response curve for the contraction elicited by 5-hydroxytryptamine (5-HT) in the rabbit aorta (pA2 = 8.2) without affecting the contractile responses to KCl, phenylephrine (alpha1) or histamine (H1). The perfusion pressure response of rat coronary artery to 5-HT (5-HT2A) was reduced concentration dependently by gamma-mangostin (IC50 = 0.32 microM). 5-HT amplified, ADP-induced aggregation of rabbit platelets (5-HT2A) was inhibited by gamma-mangostin (IC50 = 0.29 microM), whereas that induced by thrombin was not affected, nor did gamma-mangostin affect 5-HT-induced contraction of the guinea-pig ileum (5-HT3)in the presence of 5-HT1, 5-HT2 and 5-HT4 receptor antagonists. Furthermore, 5-HT-induced contraction of the rat fundus (5-HT2B) and 5-HT-induced relaxation of the rabbit aorta in the presence of ketanserin (5-HT1) and carbachol-induced contraction of the guinea-pig ileum (muscarinic M3) were not affected by gamma-mangostin (5 microM). Gamma-mangostin inhibited [3H]spiperone binding to cultured rat aortic myocytes (IC50 = 3.5 nM). The Kd for [3H]spiperone binding was increased by gamma-mangostin (3 nM) from 11.7 to 27.4 nM without affecting Bmax. These results suggest that gamma-mangostin is a novel competitive antagonist, free from a nitrogen atom, for the 5-HT2A receptors in vascular smooth muscles and platelets.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/HIV Protease Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Plant Extracts,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Aggregation Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Spiperone,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthenes,
http://linkedlifedata.com/resource/pubmed/chemical/Xanthones,
http://linkedlifedata.com/resource/pubmed/chemical/gamma-mangostin
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jan
|
| pubmed:issn |
0028-1298
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
357
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
25-31
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:9459569-Animals,
pubmed-meshheading:9459569-Binding, Competitive,
pubmed-meshheading:9459569-Dose-Response Relationship, Drug,
pubmed-meshheading:9459569-Guinea Pigs,
pubmed-meshheading:9459569-HIV Protease Inhibitors,
pubmed-meshheading:9459569-Male,
pubmed-meshheading:9459569-Muscle, Smooth,
pubmed-meshheading:9459569-Muscle, Smooth, Vascular,
pubmed-meshheading:9459569-Muscle Contraction,
pubmed-meshheading:9459569-Perfusion,
pubmed-meshheading:9459569-Plant Extracts,
pubmed-meshheading:9459569-Platelet Aggregation Inhibitors,
pubmed-meshheading:9459569-Rabbits,
pubmed-meshheading:9459569-Rats,
pubmed-meshheading:9459569-Rats, Wistar,
pubmed-meshheading:9459569-Receptor, Serotonin, 5-HT2A,
pubmed-meshheading:9459569-Receptors, Serotonin,
pubmed-meshheading:9459569-Serotonin Antagonists,
pubmed-meshheading:9459569-Spiperone,
pubmed-meshheading:9459569-Xanthenes,
pubmed-meshheading:9459569-Xanthones
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Gamma-mangostin, a novel type of 5-hydroxytryptamine 2A receptor antagonist.
|
| pubmed:affiliation |
Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
|
| pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|