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[3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen.
Eur J Pharmacol. 2001 Oct 26; 430(1):147-8.EJ

Abstract

The pharmacological characteristics of [3H]dofetilide binding were examined in membranes prepared from human embryonic kidney (HEK293) cells stably expressing human ether-á-go-go related gene (HERG) K+ channels. The classIII antiarrhythmic compounds dofetilide, clofilium, 4'-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidyl]carbonyl]methanesulfonanilide (E-4031), N-methyl-N-[2-[methyl-(1-methyl-1H-benzimidazol-2-yl)amino]ethyl]-4-[(methylsulfonyl)amino]benzene-sulfonamide (WAY-123,398) and d-sotalol all inhibited [3H]dofetilide binding. In addition, the structurally unrelated compounds pimozide, terfenadine and haloperidol, all of which prolong the QT interval in man, also inhibited binding. These data indicate that a [3H]dofetilide binding assay using HERG membranes may help identify compounds that prolong the QT interval.

Authors+Show Affiliations

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

Pub Type(s)

Journal Article

Language

eng

PubMed ID

11698075

Citation

Finlayson, K, et al. "[3H]dofetilide Binding to HERG Transfected Membranes: a Potential High Throughput Preclinical Screen." European Journal of Pharmacology, vol. 430, no. 1, 2001, pp. 147-8.
Finlayson K, Turnbull L, January CT, et al. [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur J Pharmacol. 2001;430(1):147-8.
Finlayson, K., Turnbull, L., January, C. T., Sharkey, J., & Kelly, J. S. (2001). [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. European Journal of Pharmacology, 430(1), 147-8.
Finlayson K, et al. [3H]dofetilide Binding to HERG Transfected Membranes: a Potential High Throughput Preclinical Screen. Eur J Pharmacol. 2001 Oct 26;430(1):147-8. PubMed PMID: 11698075.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. AU - Finlayson,K, AU - Turnbull,L, AU - January,C T, AU - Sharkey,J, AU - Kelly,J S, PY - 2001/11/8/pubmed PY - 2002/1/5/medline PY - 2001/11/8/entrez SP - 147 EP - 8 JF - European journal of pharmacology JO - Eur. J. Pharmacol. VL - 430 IS - 1 N2 - The pharmacological characteristics of [3H]dofetilide binding were examined in membranes prepared from human embryonic kidney (HEK293) cells stably expressing human ether-á-go-go related gene (HERG) K+ channels. The classIII antiarrhythmic compounds dofetilide, clofilium, 4'-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidyl]carbonyl]methanesulfonanilide (E-4031), N-methyl-N-[2-[methyl-(1-methyl-1H-benzimidazol-2-yl)amino]ethyl]-4-[(methylsulfonyl)amino]benzene-sulfonamide (WAY-123,398) and d-sotalol all inhibited [3H]dofetilide binding. In addition, the structurally unrelated compounds pimozide, terfenadine and haloperidol, all of which prolong the QT interval in man, also inhibited binding. These data indicate that a [3H]dofetilide binding assay using HERG membranes may help identify compounds that prolong the QT interval. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/11698075/[3H]dofetilide_binding_to_HERG_transfected_membranes:_a_potential_high_throughput_preclinical_screen_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014299901013620 DB - PRIME DP - Unbound Medicine ER -