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R- and S-terbutaline activate large conductance and Ca 2+ dependent K + (BK Ca ) channel through interacting with β 2 and M receptor respectively
- Source :
- Biochimica et Biophysica Acta (BBA) - Biomembranes. 1858:2745-2752
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- This study investigated the effect of the β2 receptor agonist terbutaline on the single channel activity of BKCa channel. The effects of racemate and two isomers of terbutaline were all assessed. β2 adrenoceptors were stably overexpressed on HEK293 cells by lentiviral transduction method and chicken BKCa channels were transiently expressed on normal HEK293 cell line or HEK293 cells overexpressing β2 receptors. Data showed that terbutaline significantly increased the single channel open probability of BKCa channel within 10min. The channel activating effects of terbutaline are stereoselective and mainly stay with the R-enantiomers. The opening probability of BKCa channel at 10min after drug application normalized to that just before drug application (Po10/Po0s) for R- and S-terbutaline were 7.85±3.20 and 1.06±0.45 respectively at 1μM concentration, corresponding to 28.37±9.96 and 2.68±1.09 at the higher concentration of 10μM. ICI 118551 blocked the effect of R- but not S-terbutaline (10μM), whereas atropine blocked the channel activating effects of S-terbutaline of higher concentration. In addition, the muscarinic receptor agonist carbachol increased the BKCa channel activity in an atropine-sensitive manner as an positive control experiment, which indicate the involvement of M receptor in the channel activating effect of S-terbutaline.
- Subjects :
- 0301 basic medicine
Agonist
BK channel
Carbachol
biology
medicine.drug_class
Chemistry
Terbutaline
HEK 293 cells
Biophysics
Cell Biology
Pharmacology
01 natural sciences
Biochemistry
03 medical and health sciences
Atropine
030104 developmental biology
0103 physical sciences
Muscarinic acetylcholine receptor
medicine
biology.protein
010306 general physics
Receptor
medicine.drug
Subjects
Details
- ISSN :
- 00052736
- Volume :
- 1858
- Database :
- OpenAIRE
- Journal :
- Biochimica et Biophysica Acta (BBA) - Biomembranes
- Accession number :
- edsair.doi...........197cfa3e3ba2a849e6f11f3447466c6c