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[3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel?
Eur J Pharmacol. 2001 Feb 02; 412(3):203-12.EJ

Abstract

The pharmacological characteristics of [3H]dofetilide binding in SHSY5Y, HEK293 and CHO-K1 cells were examined, and in parallel whole cell recordings used to characterise HERG-like K+ currents. Dofetilide affinity was similar in the human cell lines, SHSY5Y (Kd=99.6 nM) and HEK293 (Kd=102.9 nM), but 10 times lower in CHO-K1 cells (Kd=1200 nM). In contrast, clofilium and E4031 had a similar affinity in all three cell lines, whereas WAY 123,398 had no effect. Electrophysiological studies showed that SHSY5Y cells contained a HERG-like K+ current blocked by application of dofetilide to either side of the membrane. Block was faster when dofetilide was applied intracellularly. In contrast, HEK293 and CHO-K1 cells contained no such current, despite the presence of a partial cDNA for HERG in the former. That [3H]dofetilide is specific for I(Kr)/HERG may be questionable, as HEK293 and CHO-K1 cells contain no such functional K+ current.

Authors+Show Affiliations

Fujisawa Institute of Neuroscience, Department of Neuroscience, University of Edinburgh, 1 George Square, EH8 9JZ, Edinburgh, UK. Keith.Finlayson@ed.ac.ukNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

11166283

Citation

Finlayson, K, et al. "[3H]dofetilide Binding in SHSY5Y and HEK293 Cells Expressing a HERG-like K+ Channel?" European Journal of Pharmacology, vol. 412, no. 3, 2001, pp. 203-12.
Finlayson K, Pennington AJ, Kelly JS. [3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel? Eur J Pharmacol. 2001;412(3):203-12.
Finlayson, K., Pennington, A. J., & Kelly, J. S. (2001). [3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel? European Journal of Pharmacology, 412(3), 203-12.
Finlayson K, Pennington AJ, Kelly JS. [3H]dofetilide Binding in SHSY5Y and HEK293 Cells Expressing a HERG-like K+ Channel. Eur J Pharmacol. 2001 Feb 2;412(3):203-12. PubMed PMID: 11166283.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel? AU - Finlayson,K, AU - Pennington,A J, AU - Kelly,J S, PY - 2001/2/13/pubmed PY - 2001/5/22/medline PY - 2001/2/13/entrez SP - 203 EP - 12 JF - European journal of pharmacology JO - Eur. J. Pharmacol. VL - 412 IS - 3 N2 - The pharmacological characteristics of [3H]dofetilide binding in SHSY5Y, HEK293 and CHO-K1 cells were examined, and in parallel whole cell recordings used to characterise HERG-like K+ currents. Dofetilide affinity was similar in the human cell lines, SHSY5Y (Kd=99.6 nM) and HEK293 (Kd=102.9 nM), but 10 times lower in CHO-K1 cells (Kd=1200 nM). In contrast, clofilium and E4031 had a similar affinity in all three cell lines, whereas WAY 123,398 had no effect. Electrophysiological studies showed that SHSY5Y cells contained a HERG-like K+ current blocked by application of dofetilide to either side of the membrane. Block was faster when dofetilide was applied intracellularly. In contrast, HEK293 and CHO-K1 cells contained no such current, despite the presence of a partial cDNA for HERG in the former. That [3H]dofetilide is specific for I(Kr)/HERG may be questionable, as HEK293 and CHO-K1 cells contain no such functional K+ current. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/11166283/[3H]dofetilide_binding_in_SHSY5Y_and_HEK293_cells_expressing_a_HERG_like_K+_channel L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014299901007312 DB - PRIME DP - Unbound Medicine ER -