Characterisation of leukotriene receptors on rat lung strip

Autor: Norman, Peter, Abram, Trevor S., Cuthbert, Nigel J., Tudhope, Stephen R., Gardiner, Phillip J.
Zdroj: European Journal of Pharmacology; December 1994, Vol. 271 Issue: 1 p73-78, 6p
Abstrakt: The leukotriene receptor(s) present on rat lung strip have been characterised using the natural agonists, a selective mimetic, and potent (cysLT1) selective leukotriene receptor antagonists. Leukotriene C4and leukotriene D4displayed comparable contractile potencies whilst leukotriene E4was less potent. However, both leukotriene D4and leukotriene E4were found to be partial agonists relative to leukotriene C4. Responses to all three leukotrienes were competitively antagonised by ICI 198615 (1-((2-methoxy-(4-phenylsulfonyl)-aminocarbonyl)-phenyl) methyl)-1H-indazol-6-yl) carbonic acid cyclopentyl ester), SK&F 104353 (2-(R)-hydroxy-3(S)-(2-carboxyethylthio)-3-(2-[8-phenyl)propanoic acid and MK 571 (±(E)-3-[3-[2-(7-chloro-2-quinolin-yl)ethenyl]-phenyl)- 3-oxopropyl]thio]methyl]thio]thio]propanoic acid) with comparable affinities irrespective of the agonist used. This indicates that rat lung contains a homogeneous population of leukotriene receptors and that they are of the CysLT1type.
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