Differential effects of the BKCa channel openers NS004 and NS1608 in porcine coronary arterial cells
| Autor: | Cynthia A. Fink, Shiling Hu, Helen S. Kim |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
Agonist
Patch-Clamp Techniques Potassium Channels Swine medicine.drug_class chemistry.chemical_element In Vitro Techniques Calcium Muscle Smooth Vascular Membrane Potentials Bkca channel medicine Animals Patch clamp Mode of action Pharmacology Phenylurea Compounds Coronary Vessels In vitro chemistry Mechanism of action Anesthesia Circulatory system Biophysics Benzimidazoles medicine.symptom Chlorophenols |
| Zdroj: | European Journal of Pharmacology. 294:357-360 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/0014-2999(95)00744-x |
| Popis: | The effects of newly claimed BKCa channel openers NS004 (5-trifluoromethyl-(5-chloro-2-hydroxyphenyl)-1,3-dihydro-2H-benzimidazo le-2- one) and NS1608 (N-(3-(trifluoromethyl)phenyl)-N'-(2-hydroxy-5-chlorophenyl)urea) were investigated on whole-cell K+ current (IK) in enzymatically isolated porcine coronary arterial cells using patch-clamp technique with a double holding potential protocol. When cells were held at 0 mV, IK was augmented by NS004 in a concentration-dependent manner. With a holding potential of -60 mV, however, IK was moderately inhibited by NS004 between 0.5 and 10 microM, but robustly stimulated by 50 microM NS004 at highly depolarized potentials. The effects of NS1608 on IK did not differ due to change in holding potential. At -60 mV and 0 mV, NS1608 activated IK with bell-shaped concentration-response curves peaked between 5 and 10 microM. The differential mode of action of the two compounds suggested an involvement of mechanism(s) other than an opening of BKCa channel. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect