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Specific binding of leukotriene C4 to ileal segments and subcellular fractions of ileal smooth muscle cells.

Abstract：

:A specific high-affinity receptor for leukotriene C4 (LTC4) has been identified on segments of longitudinal smooth muscle from guinea pig ileum, in disrupted cells obtained from the ileal segments, and in subcellular fractions enriched for mitochondrial membranes and plasma membranes, respectively. Specific [3H]LTC4 binding at a fixed input at 4 degrees C reached a plateau at 60 min with each of the four preparations and was greater than 80% reversible after binding reached equilibrium by the introduction of excess unlabeled homoligand. LIGAND analysis demonstrated a single high-affinity receptor on the smooth muscle segments, the disrupted cells, and the subcellular fractions enriched for mitochondrial membranes and for plasma membranes with respective Kd values of 7.6 nM, 1.3 nM, 13 nM, and 8.5 nM. These Kd values overlap with the concentration of LTC4 known to elicit a spasmogenic response in the ileal muscle, indicating that the radioligand recognizes a receptor that mediates the biological response. Competition analysis with disrupted ileal cells and subcellular fractions with a fixed input of LTC4 radioligand and incremental concentrations of the natural sulfidopeptide leukotrienes demonstrated leukotriene D4 (LTD4) to be 1-3 logarithms less active than LTC4 and leukotriene E4 (LTE4) to be essentially inactive. Thus, ileal longitudinal smooth muscle cells possess a high-affinity receptor that is selective for LTC4 and that receptor exhibits both a plasma membrane and subcellular distribution.

journal_name

Proc Natl Acad Sci U S A

journal_title

Proceedings of the National Academy of Sciences of the United States of America

authors

Krilis S,Lewis RA,Corey EJ,Austen KF

doi

10.1073/pnas.81.14.4529

subject

Has Abstract

pub_date

1984-07-01 00:00:00

pages

4529-33

issue

14

eissn

0027-8424

issn

1091-6490

journal_volume

81

pub_type

杂志文章

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