Linked Life Data

2515014

Source:http://linkedlifedata.com/resource/pubmed/id/2515014

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1990-3-15
pubmed:abstractText
1. The present study has examined the possibility that one or more metabolites of glyceryl trinitrate (GTN) (i.e. glyceryl-1,2- and -1,3-dinitrate and glyceryl-1- and -2-mononitrate) may be responsible for the second phase of the biphasic relaxant curve to GTN in phenylephrine-contracted rings of rat aorta. 2. The IC50 values for the two phases of the GTN curve were 0.1 mumol/L and 12 mumols/L with the initial phase eliciting 60% of the total relaxation response. The curves for glyceryl-1,2- and -1,3-dinitrate were monophasic with IC50 values of 248 mumols/L and 110 mumols/L, respectively. The mononitrate metabolites elicited relaxant effects at concentrations greater than or equal to 1 mmol/L. 3. The induction of tolerance to GTN or pretreatment with oxyhaemoglobin (5 mumol/L) resulted in a monophasic GTN curve with IC50 values of 16 mumol/L and 18 mumol/L respectively suggesting selective abolition of responses to low concentrations of GTN with little effect on responses to high concentrations of GTN. The relaxant effects of the -1,2- and -1,3-dinitrates, like that to GTN, were essentially unaltered by GTN tolerance or oxyhaemoglobin. 4. Thus while the relaxant effects of the dinitrate metabolites possess similar properties to that of the second phase of relaxation to GTN, a role for these metabolites is unlikely since their IC50 values are 9-20-fold greater than that for the second phase of relaxation to GTN. Whether these differences are due to the 8-10-fold lower lipophilicity of the dinitrates as compared with the parent compound requires further study.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0305-1870
pubmed:author
pubmed:issnType
Print
pubmed:volume
16
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
829-35
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1989
pubmed:articleTitle
Studies on the biphasic relaxant curve of glyceryl trinitrate in rat aorta: role of GTN metabolites.
pubmed:affiliation
School of Pharmacology, Victorian College of Pharmacy, Parkville, Victoria, Australia.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't