High impact information on CYCLT1

• Flavones having CysLT1 receptor affinities of 10-30 nM were selected for determination of their inhibitory effects on the LTD4-induced contraction of guinea pig ileum in vitro [1].
• CysLT1 receptor affinities of the flavones (down to 11 nM) were determined by their ability to displace [3H]LTD4 from its receptor in guinea pig lung membranes [1].
• Neither theophylline nor the cysteinyl-leukotriene receptor antagonist attenuated the antigen-associated cell influx [2].
• Combination of BAY u9773 and ICI 198,615 did not produce additive inhibition, suggesting that the major part of the leukotriene D4 induced contraction in guinea pig lung parenchyma is mediated by a CysLT receptor with properties distinct from those of previously described CysLT1 and CysLT2 receptors [3].
• The CysLT1 receptor antagonist ICI 198,615 partly inhibited the contractile response to leukotriene D4 [3].

Biological context of CYCLT1

• Antagonism of LTD4-induced contraction of guinea pig ileum, the inhibition of antigen-induced contraction of guinea pig trachea in vitro, and the inhibition of LTD4-induced increase of vascular permeability in vivo are determined for chalcones with high CysLT1 receptor affinities (K(D) values below 0.1 microM) [4].

Anatomical context of CYCLT1

• The series contains several potent CysLT1 receptor antagonists, with K(D) values approaching the nanomolar range, as measured by the displacement of [3H]LTD4 from guinea pig lung membranes [4].

References