TY - JOUR
T1 - Comparative biological activities of the four synthetic (5,6)-dihete isomers
AU - Muller, A.
AU - Rechencq, E.
AU - Kugel, C.
AU - Lellouche, J. P.
AU - Beaucourt, J. P.
AU - Niel, G.
AU - Girard, J. P.
AU - Rossi, J. C.
AU - Bonne, C.
PY - 1989/12
Y1 - 1989/12
N2 - (5,6)-dihydroxy-7,9-trans-11,14-cis-eicosatetraenoic acids ((5,6)-DiHETEs) were synthesized and separated into four pure diastereoisomers. They were tested for comparative binding affinities to leukotriene receptors (LTC4, LTD4, LTB4) in guinea pig ling membranes. Only (5S,6R)-DiHETE was recognized by the LTD4 receptor, the other receptors interacted with neither of the four isomers. (5S,6R)-DiHETE also contracted ileum in vitro and this effect was inihibited by the LTD4 receptor antagonists ICI 198,615 and SKF104,353. These data suggest that the biproduct (5S,6R)-DiHETE generated by enzymatic conversion of LTA4 could have some LTD4-like activity when produced in large concentrations.
AB - (5,6)-dihydroxy-7,9-trans-11,14-cis-eicosatetraenoic acids ((5,6)-DiHETEs) were synthesized and separated into four pure diastereoisomers. They were tested for comparative binding affinities to leukotriene receptors (LTC4, LTD4, LTB4) in guinea pig ling membranes. Only (5S,6R)-DiHETE was recognized by the LTD4 receptor, the other receptors interacted with neither of the four isomers. (5S,6R)-DiHETE also contracted ileum in vitro and this effect was inihibited by the LTD4 receptor antagonists ICI 198,615 and SKF104,353. These data suggest that the biproduct (5S,6R)-DiHETE generated by enzymatic conversion of LTA4 could have some LTD4-like activity when produced in large concentrations.
UR - http://www.scopus.com/inward/record.url?scp=0024826040&partnerID=8YFLogxK
U2 - 10.1016/0090-6980(89)90046-4
DO - 10.1016/0090-6980(89)90046-4
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C2 - 2633210
AN - SCOPUS:0024826040
SN - 0090-6980
VL - 38
SP - 635
EP - 644
JO - Prostaglandins
JF - Prostaglandins
IS - 6
ER -