Three-dimensional quantitative structure-activity relationship for inhibition of human ether-a-go-go-related gene potassium channel

Journal of Pharmacology and Experimental Therapeutics

Volumn 301, Issue 2, 2002, Pages 427-434

  Ekins, Sean ^a,b,c   Crumb, William J ^a,b   Dustan Sarazan, R ^a,b   Wikel, James H ^a,b   Wrighton, Steven A ^a,b  

^a ELI LILLY AND COMPANY   (United States)

^b TULANE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c Concurrent Pharmaceuticals Inc ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [2 (6 METHYL 2 PYRIDYL)ETHYL] 4 (4 METHYLSULFONYLAMINOBENZOYL)PIPERIDINE; ALOSETRON; AMITRIPTYLINE; CHLORPROMAZINE; CISAPRIDE; CLOZAPINE; CLOZAPINE N OXIDE; DESIPRAMINE; DILTIAZEM; HALOPERIDOL; IMIPRAMINE; KETOCONAZOLE; MESORIDAZINE; NEUROLEPTIC AGENT; NICOTINE; NORCLOZAPINE; OLANZAPINE; PALIPERIDONE; PERHEXILINE; PIMOZIDE; PIPERANOMETOZINE; POTASSIUM CHANNEL; QUINIDINE; RISPERIDONE; SERTINDOLE; SILDENAFIL; TERFENADINE; THIORIDAZINE; UNINDEXED DRUG; VERAPAMIL; ZIPRASIDONE;

ARTICLE; HEART ARRHYTHMIA; HUMAN; HUMAN CELL; HYDROPHOBICITY; IC 50; PHARMACOPHORE; PRIORITY JOURNAL; QUANTITATIVE STRUCTURE ACTIVITY RELATION; THREE DIMENSIONAL IMAGING;

ANTIPSYCHOTIC AGENTS; CELLS, CULTURED; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; IMAGING, THREE-DIMENSIONAL; ISOXAZOLES; MODELS, MOLECULAR; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS; POTASSIUM CHANNELS, VOLTAGE-GATED; PROTEIN CONFORMATION; PYRIMIDINES; REPRODUCIBILITY OF RESULTS; STRUCTURE-ACTIVITY RELATIONSHIP; TERFENADINE;

EID: 0036229805     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.301.2.427     Document Type: Article

References (30)

1. QT interval prolongation by non-cardiovascular drugs: Issues and solutions for novel drug development
2. +channels in human heart: Comparison with terfenadine under physiological conditions
3. hERG block by antipsychotic drugs: A relationship between QT prolongation and ion channel blockade
4. A molecular basis for the cardiac arrhythmia: HERG mutations cause long QT syndrome
5. QT-interval prolongation by noncardiac drugs: Lessons to be learned from recent experience
6. Blockade of HERG and Kv1.5 by keteconazole
7. Predicting drug-drug interactions in silico using pharmacophores: A paradigm for the next millennium
8. In silico ADME/TOX The state of the art at the 220th ACS meeting
9. Progress in predicting human ADME parameters in silico
10. Sildenafil (Viagra) prolongs cardiac repolarization by blocking the rapid component of the delayed rectifier potassium current
11. + channel HERG
12. Inhibitory effects of vesnarinone on cloned cardiac delayed rectifier K(+) channels expressed in a mammalian cell line
13. Interactions of the 5-hydroxytryptamine 3 antagonist class of antiemetic drugs with human cardiac ion channels
14. A structural basis for the drug-induced log QT syndrome
15. Blockage of the HERG human cardiac K+ channel by the gastrointestinal prokinetic agent cisapride
16. Modulation of HERG potassium channels by extracellular magnesium and quinidine
17. A mechanism for the proarrhythmic effects of cisapride (Prepulsid): High affinity blockade of the human cardiac potassium channel HERG
18. Which cardiac potassium channel subtype is the preferable target for suppression of ventricular arrhythmias?
19. A mechanistic link between an inherited and an acquired cardiac arrhythmia: HERG encodes the IKr potassium channel
20. A common polymorphism associated with antibiotic-induced cardiac arrhythmia
21. The inward rectification mechanism of the HERG cardiac potassium channel
22. The inhibitory effect of the antipsychotic drug haloperidol on HERG potassium channels expressed in Xenopus oocytes
23. + channels as pharmacological targets
24. Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline
25. Inhibition of HERG potassium channels by the antimalarial agent halofantrine
26. Inhibition of the human ether-a-go-go-related gene (HERG) potassium channel by cisapride: Affinity for open and inactivated states
27. Inhibition of HERG channels stably expressed in a mammalian cell line by the antianginal agent perhexiline maleate
28. Inactivation gating determines nicotine blockade of human HERG channels
29. Mechanism of cocaine block of HERG potassium channels
30. Mechanism of block and identification of the verapamil binding domain to HERG potassium channels