Pub. Date : 1999 Nov
PMID : 10556945
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Effects of rupatadine, a new dual antagonist of histamine and platelet-activating factor receptors, on human cardiac kv1.5 channels. | rupatadine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 2 | The effects of rupatadine, a new dual antagonist of both histamine H1 and platelet-activating factor receptors, were studied on human cloned hKv1.5 channels expressed in Ltk- cells using the whole-cell patch-clamp technique. | rupatadine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 3 | Rupatadine produced a use- and concentration-dependent block of hKv1.5 channels (KD=2.4+/-0.7 micronM) and slowed the deactivation of the tail currents, thus inducing the "crossover" phenomenon. | rupatadine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 4 | Moreover, rupatadine also modified the voltage-dependence of hKv1.5 channel activation, which exhibited two components, the midpoint of the steeper component averaging -25. | rupatadine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |
| 5 | All these results suggest that rupatadine blocks hKv1.5 channels binding to an external and to an internal binding site but only at concentrations much higher than therapeutic plasma levels in man. | rupatadine | potassium voltage-gated channel subfamily A member 5 | Homo sapiens |