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Bupivacaine inhibits large conductance, voltage- and $Ca^{2+}$- activated $K^{+}$channels in human umbilical artery smooth muscle cells
| Content Provider | Scilit |
|---|---|
| Author | Martín, Pedro Enrique, Nicolás Palomo, Ana R. Roldán Rebolledo, Alejandro Milesi, Veronica |
| Copyright Year | 2012 |
| Description | Bupivacaine is a local anesthetic compound belonging to the amino amide group. Its anesthetic effect is commonly related to its inhibitory effect on voltage-gated sodium channels. However, several studies have shown that this drug can also inhibit voltage-operated K(+) channels by a different blocking mechanism. This could explain the observed contractile effects of bupivacaine on blood vessels. Up to now, there were no previous reports in the literature about bupivacaine effects on large conductance voltage- and Ca(2+) -activated K(+) channels (BK(Ca)). Using the patch-clamp technique, it is shown that bupivacaine inhibits single-channel and whole-cell K(+) currents carried by BK(Ca) channels in smooth muscle cells isolated from human umbilical artery (HUA). At the single-channel level bupivacaine produced, in a concentration- and voltage-dependent manner (IC(50) 324 µM at +80 mV), a reduction of single-channel current amplitude and induced a flickery mode of the open channel state. Bupivacaine (300 µM) can also block whole-cell K(+) currents (~45% blockage) in which, under our working conditions, BK(Ca) is the main component. This study presents a new inhibitory effect of bupivacaine on an ion channel involved in different cell functions. Hence, the inhibitory effect of bupivacaine on BK(Ca) channel activity could affect different physiological functions where these channels are involved. Since bupivacaine is commonly used during labor and delivery, its effects on umbilical arteries, where this channel is highly expressed, should be taken into account. |
| Related Links | https://www.tandfonline.com/doi/pdf/10.4161/chan.20362?needAccess=true https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3431591/pdf |
| Ending Page | 180 |
| Page Count | 7 |
| Starting Page | 174 |
| ISSN | 19336950 |
| e-ISSN | 19336969 |
| DOI | 10.4161/chan.20362 |
| Journal | Channels |
| Issue Number | 3 |
| Volume Number | 6 |
| Language | English |
| Publisher | Informa UK Limited |
| Publisher Date | 2012-05-01 |
| Access Restriction | Open |
| Subject Keyword | Biophysics Physiology Bkca Channels Bupivacaine Human Umbilical Artery Patch Clamp Native Vascular Smooth Muscle |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Biochemistry Biophysics |
