| pubmed-article:1320207 | rdf:type | pubmed:Citation | lld:pubmed |
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| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0039259 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0036751 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0021467 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0021469 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0243076 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C1709059 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0679932 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0065357 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0752969 | lld:lifeskim |
| pubmed-article:1320207 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
| pubmed-article:1320207 | pubmed:issue | 4 | lld:pubmed |
| pubmed-article:1320207 | pubmed:dateCreated | 1992-7-31 | lld:pubmed |
| pubmed-article:1320207 | pubmed:abstractText | Twelve ergolines (O-acylated lysergol and dihydrolysergol-I derivatives) were synthesized to study their antagonism of 5-HT responses in comparison with methylsergide and LY 53857 [6-methyl-1-(1-methylethyl)-8 beta-ergoline carboxylic acid 2-hydroxy-1-methylpropyl-ester hydrogen maleate] in cylindrical segments of the isolated rat tail artery. With regard to (9.10-didehydro-6-methyl-8 beta-ergoline)methyl R,S-2-methylbutyrate, the most potent new ergoline derivative, we examined the phenomenon of insurmountable antagonism to 5-HT by methylsergide. O-Acylated lysergol and dihydrolysergol-I derivatives competitively antagonized 5-HT-induced contractions with calculated pA2 values of 7.30 +/- 0.42 for the weakest and 8.42 +/- 0.35 for the most potent ergoline derivative in this series. N1-isopropyl substitution did not generally enhance 5-HT2 receptor affinities but lowered affinities for alpha 1 adrenoceptors in rat aorta. Methysergide and LY 53857 were insurmountable antagonists of 5-HT in rat tail artery. Preincubation with (9.10-didehydro-6-methyl-8 beta-ergoline)methyl R,S-2-methylbutyrate (1 mumol/l) partially prevented the depression of 5-HT-induced contractions caused by methysergide (1-10 nmol/l). Methysergide (100 nmol/l) abolished the protective effect of (9.10-didehydro-6-methyl-8 beta-ergoline)methyl R,S-2-methylbutyrate. (9.10-Didehydro-6-methyl-8 beta-ergoline)methyl R,S-2-methylbutyrate (1 mumol/l), concomitantly incubated with methysergide (30 nmol/l), partially restored the maximum response to 5-HT that had been depressed by methysergide (30 nmol/l). Partial restoration could not be mimicked by washout of methysergide.(ABSTRACT TRUNCATED AT 250 WORDS) | lld:pubmed |
| pubmed-article:1320207 | pubmed:language | eng | lld:pubmed |
| pubmed-article:1320207 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1320207 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:1320207 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:1320207 | pubmed:issn | 0028-1298 | lld:pubmed |
| pubmed-article:1320207 | pubmed:author | pubmed-author:HORNJ EJE | lld:pubmed |
| pubmed-article:1320207 | pubmed:author | pubmed-author:PertzHH | lld:pubmed |
| pubmed-article:1320207 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:1320207 | pubmed:volume | 345 | lld:pubmed |
| pubmed-article:1320207 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:1320207 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:1320207 | pubmed:pagination | 394-401 | lld:pubmed |
| pubmed-article:1320207 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
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| pubmed-article:1320207 | pubmed:meshHeading | pubmed-meshheading:1320207-... | lld:pubmed |
| pubmed-article:1320207 | pubmed:year | 1992 | lld:pubmed |
| pubmed-article:1320207 | pubmed:articleTitle | O-acylated lysergol and dihydrolysergol-I derivatives as competitive antagonists of 5-HT at 5-HT2 receptors of rat tail artery. Allosteric modulation instead of pseudoirreversible inhibition. | lld:pubmed |
| pubmed-article:1320207 | pubmed:affiliation | Fachbereich Pharmazie, Freie Universität Berlin, Federal Republic of Germany. | lld:pubmed |
| pubmed-article:1320207 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:1320207 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:1320207 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
