Words similar to blocker
Example sentences for: blocker
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Tetraethylammonium is known as a pore-occluding blocker of voltage-gated potassium channels [ 1 ] , but it also blocks other cationic channels such as calcium-dependent K +channels [ 2 3 ] and the nicotinic acetylcholine receptor [ 4 ] . TEA at 0.1 to 10 mM also inhibits osmotic water flux through human AQP1 channels expressed in Xenopus oocytes, decreasing the net swelling rate in hypotonic saline by 30-40% as compared to AQP1-expressing oocytes not treated with TEA [ 5 ] . This blocking effect on osmotic water flux was demonstrated to involve AQP1 channels specifically by using site-directed mutagenesis (tyrosine 186 to phenylalanine) to generate a Y186F AQP1 channel that is insensitive to block by TEA, but retains sensitivity to block by mercury.
Expression of AQP1 channels in bilayers has shown that the water permeability but not the ionic conductance is blocked by p-chloromethylbenzenesulfonate, indicating that the two fluxes may involve distinct pathways [ 12 ] . Work presented here provides an additional line of evidence that the pathways for water and ions in AQP1 can be distinguished pharmacologically, using the blocker TEA as a probe.
The blocking effect of mercury in AQP1 channels is dependent on a neighboring residue, cysteine 189 [ 6 ] . TEA offers attractive advantages over mercury as a reversible and less toxic blocker for AQP1 channels in experimental analyses of water channel function; however, the relevance of TEA as a blocker for AQP1 channels outside the Xenopus expression system has not been examined previously.
These four transcripts are considered to be biomarkers of the SU5416 administration regimen rather than activity of SU5416 specifically; with the available samples we could not exclude the possibility that altered gene expression resulted from exposure to the administration vehicle (Cremophor) or the concomitant premedications (dexamethasone and H1- and H2-blocker antihistamines) rather than SU5416.
The sections were treated for 5 min with 3% H 2 O 2 , followed by a 10 min incubation with the universal blocker, Cas-block (Zymed).
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