| pubmed-article:8636420 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:8636420 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
| pubmed-article:8636420 | lifeskim:mentions | umls-concept:C0003062 | lld:lifeskim |
| pubmed-article:8636420 | lifeskim:mentions | umls-concept:C0003842 | lld:lifeskim |
| pubmed-article:8636420 | lifeskim:mentions | umls-concept:C0042396 | lld:lifeskim |
| pubmed-article:8636420 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:8636420 | pubmed:issue | 10 | lld:pubmed |
| pubmed-article:8636420 | pubmed:dateCreated | 1996-7-11 | lld:pubmed |
| pubmed-article:8636420 | pubmed:abstractText | Recent studies have suggested that nonsterol, mevalonate-derived metabolites are implicated in the control of vascular tone and blood pressure. Because of the metabolic importance of farnesyl pyrophosphate, a 15-carbon (C15) intermediate of the cholesterol pathway, the vasoactive properties of the farnesyl motif were investigated. Two farnesyl analogues were used: farnesol, the natural dephosphorylated form of farnesyl pyrophosphate, and N-acetyl-S-trans,trans-farnesyl-L-cysteine (AFC), a synthetic mimic of the carboxyl terminus of farnesylated proteins. Both compounds inhibited NE-induced vasoconstriction in rat aortic rings at micromolar concentration. Their action was rapid, dose dependent, and reversible. Shorter (C10) and longer (C20) isoprenols as well as N-acetyl-S-geranyl-L-cysteine (C10) did not inhibit the response to NE. In contrast, N-acetyl-S-geranylgeranyl-L-cysteine (C20), exhibited vasoactive properties similar to AFC. It was further demonstrated that AFC and farnesol inhibited KCl and NaF-induced contractions, suggesting a complex action on Ca2+ channels and G protein-dependent pathways. Finally, the effect of farnesol and AFC on the NE response was reproduced in human resistance arteries. In conclusion, mevalonate-derived farnesyl analogues are potent inhibitors of vasoconstriction. The study suggests that farnesyl cellular availability is an important determinant of vascular tone in animals and humans, and provides a basis for exploring farnesyl metabolism in humans with compromised vascular function as well as for using farnesyl analogues as regulators of arterial tone in vivo. | lld:pubmed |
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| pubmed-article:8636420 | pubmed:language | eng | lld:pubmed |
| pubmed-article:8636420 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8636420 | pubmed:citationSubset | AIM | lld:pubmed |
| pubmed-article:8636420 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:8636420 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:8636420 | pubmed:month | May | lld:pubmed |
| pubmed-article:8636420 | pubmed:issn | 0021-9738 | lld:pubmed |
| pubmed-article:8636420 | pubmed:author | pubmed-author:ChapmanJJ | lld:pubmed |
| pubmed-article:8636420 | pubmed:author | pubmed-author:McCarronD ADA | lld:pubmed |
| pubmed-article:8636420 | pubmed:author | pubmed-author:RoulletJ BJB | lld:pubmed |
| pubmed-article:8636420 | pubmed:author | pubmed-author:XueHH | lld:pubmed |
| pubmed-article:8636420 | pubmed:author | pubmed-author:RoulletC MCM | lld:pubmed |
| pubmed-article:8636420 | pubmed:author | pubmed-author:McDougalPP | lld:pubmed |
| pubmed-article:8636420 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:8636420 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:8636420 | pubmed:volume | 97 | lld:pubmed |
| pubmed-article:8636420 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:8636420 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:8636420 | pubmed:pagination | 2384-90 | lld:pubmed |
| pubmed-article:8636420 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:8636420 | pubmed:meshHeading | pubmed-meshheading:8636420-... | lld:pubmed |
| pubmed-article:8636420 | pubmed:year | 1996 | lld:pubmed |
| pubmed-article:8636420 | pubmed:articleTitle | Farnesyl analogues inhibit vasoconstriction in animal and human arteries. | lld:pubmed |
| pubmed-article:8636420 | pubmed:affiliation | Department of Nephrology, Hypertension and Clinical Pharmacology, Oregon Health Sciences University, Portland 97201, USA. | lld:pubmed |
| pubmed-article:8636420 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:8636420 | pubmed:publicationType | In Vitro | lld:pubmed |
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