Linked Life Data

3580709

Source:http://linkedlifedata.com/resource/pubmed/id/3580709

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1987-6-26
pubmed:abstractText
Isopolar methylene phosphonate analogues of adenosine triphosphate (ATP) were synthesized and tested on the guinea-pig isolated taenia coli (where ATP causes relaxation) and urinary bladder (where ATP causes contraction), to see if restoration of the electronegativity of the methylene linkage would enhance pharmacological potency. The compounds used were the dichloromethylene and difluoromethylene analogues of adenosine 5'-(beta,gamma-methylene)triphosphonate (AMP-PCP), L-adenosine 5'-(beta,gamma-methylene)triphosphonate (L-AMP-PCP) and 2-methylthioadenosine 5'-(beta,gamma-methylene)-triphosphonate (2-methylthio-AMP-PCP). The order of potency of the analogues depended on the tissue, and was independent of the nature of the purine or ribose moieties. None of the analogues was degraded by ectonucleotidases on either tissue. In the taenia coli the order of potency for relaxation was difluoromethylene greater than or equal to dichloromethylene greater than methylene, and this reflected the order of electronegativity of the analogues. The isopolar analogues of L-AMP-PCP were inactive in the taenia coli. In the bladder the order of potency for contraction was difluoromethylene greater than or equal to methylene greater than dichloromethylene, suggesting that electronegativity is of lesser importance here. The isopolar analogues of L-AMP-PCP were active in this tissue. The differences between the two tissues in the order of potency for these non-degradable analogues supports suggestions that P2-purinoceptors in the taenia coli (P2Y) are different from those in the bladder (P2X). The isopolar analogues of L-AMP-PCP, like L-AMP-PCP itself, were selective agonists at the P2X-purinoceptor.
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-1195136, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-2984024, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-2996968, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-3006665, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-3023103, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-3816951, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-5787092, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-6312968, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-6317121, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-6547360, http://linkedlifedata.com/resource/pubmed/commentcorrection/3580709-760894
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0007-1188
pubmed:author
pubmed:issnType
Print
pubmed:volume
90
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
791-5
pubmed:dateRevised
2009-11-18
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Pharmacological effects of isopolar phosphonate analogues of ATP on P2-purinoceptors in guinea-pig taenia coli and urinary bladder.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't