Linked Life Data

10510460

Source:http://linkedlifedata.com/resource/pubmed/id/10510460

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2000-1-4
pubmed:abstractText
1 Endomorphin-1 and -2 (E-1/E-2) have been proposed as endogenous ligands for the mu-opioid receptor. The aims of this study are to characterize the binding of E-1/E-2 and the subsequent effects on cyclic AMP formation and [Ca2+]i levels in SH-SY5Y and Chinese hamster ovary (CHO) cells expressing endogenous and recombinant mu-opioid receptors. 2 E-1 displaced [3H]-diprenorphine ([3H]-DPN) binding in CHO micro and SH-SY5Y membranes with pKi values of 8.02+/-0.09 and 8.54+/-0.13 respectively. E-2 displaced [3H]-DPN binding in CHOmu and SH-SY5Y cells with pKi values of 7.82+/-0.11 and 8.43+/-0.13 respectively. E-1/E-2 bound weakly to CHOdelta and CHOkappa membranes, with IC50 values of greater than 10 microM. 3 In CHOmu cells, E-1/E-2 inhibited forskolin (1 microM) stimulated cyclic AMP formation with pIC50 values of 8.03+/-0.16 (Imax = 53.0+/-9. 3%) and 8.15+/-0.24 (Imax = 56.3+/-3.8%) respectively. In SH-SY5Y cells E1/E2 inhibited forskolin stimulated cyclic AMP formation with pIC50 values of 7.72+/-0.13 (Imax=46.9+/-5.6%) and 8.11+/-0.31 (Imax = 40.2+/-2.8%) respectively. 4 E-1/E-2 (1 microM) increased [Ca2+]i in fura-2 loaded CHOmu cell suspensions in a thapsigargin sensitive and naloxone reversible manner. Mean increases observed were 106+/-28 and 69+/-6.7 nM respectively. In single adherent cells E-1/E-2 (1 microM) increased [Ca2+]i with a mean 340/380 ratio change of 0.81+/-0.09 and 0.40+/-0.08 ratio units respectively. E-1/E-2 failed to increase intracellular calcium in CHOdelta, CHOkappa and SH-SY5Y cells. 5 These data show that E-1/E-2 bind with high affinity and selectivity to mu-opioid receptors and modulate signal transduction pathways typical of opioids. This provides further evidence that these two peptides may be endogenous ligands at the mu-opioid receptor.
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-1207728, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-1264258, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-1334555, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-1335167, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-1851914, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-2155471, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-230519, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-2679954, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-3838314, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-7519024, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-7737460, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-7786304, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8216364, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8240812, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8382479, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8393575, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8756186, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8789387, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-8813369, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9087409, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9134231, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9331928, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9353135, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9392842, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9422796, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9437727, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9437728, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9512376, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9519803, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9523574, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9537802, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9544801, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9601662, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9617760, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9622031, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9622032, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9655870, http://linkedlifedata.com/resource/pubmed/commentcorrection/10510460-9694962
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0007-1188
pubmed:author
pubmed:issnType
Print
pubmed:volume
128
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
472-8
pubmed:dateRevised
2009-11-18
pubmed:meshHeading
pubmed:year
1999
pubmed:articleTitle
The effects of endomorphin-1 and endomorphin-2 in CHO cells expressing recombinant mu-opioid receptors and SH-SY5Y cells.
pubmed:affiliation
University Department of Anaesthesia, Leicester Royal Infirmary, Leicester LE1 5WW.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't