hERG (the human Ether-à-go-go-Related Gene) is a gene (KCNH2) that codes for a protein known as Kv11.1, the alpha subunit of a potassium ion channel. This...
20 KB (2,339 words) - 21:31, 21 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
117 KB (11,215 words) - 22:00, 20 December 2024
Orphenadrine (category HERG blocker)
dopamine reuptake inhibitor) Nav1.7, Nav1.8, and Nav1.9 sodium channel blocker HERG potassium channel blocker George Rieveschl was a professor of chemistry at...
18 KB (1,550 words) - 02:58, 26 October 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
80 KB (8,640 words) - 19:58, 16 December 2024
Terfenadine (category HERG blocker)
effects, also acts as a potassium channel blocker (Kv11.1 encoded by the gene hERG). Since its active metabolite is not a potassium channel blocker, no cardiotoxicity...
9 KB (782 words) - 21:56, 16 September 2024
JJC8-088 (category HERG blocker)
Reduced hERG Activity". ACS Pharmacol Transl Sci. 7 (2): 515–532. doi:10.1021/acsptsci.3c00322. PMID 38357284. Furutani K. Facilitation of hERG Activation...
8 KB (715 words) - 08:30, 18 October 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
13 KB (1,082 words) - 16:34, 19 December 2024
by chance. Among the best-known and most significant antitargets are the hERG channel and the 5-HT2B receptor, both of which cause long-term problems with...
7 KB (777 words) - 19:11, 19 April 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
62 KB (5,859 words) - 20:35, 30 November 2024
Methadone (category HERG blocker)
other cardiotoxic drugs, methadone blocks the hERG K+ channel. The two enantiomers of methadone inhibit hERG channels with different potency. Dextromethadone...
77 KB (7,720 words) - 00:03, 10 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
44 KB (3,871 words) - 02:50, 13 November 2024
model for the channel dynamics of larger eukaryotic K+ channels, including hERG. The structure of KcsA is that of an inverted cone, with a central pore running...
28 KB (3,465 words) - 13:06, 1 August 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
96 KB (9,511 words) - 09:42, 22 December 2024
Suessbrich H, Waldegger S, Lang F, Busch AE (April 1996). "Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists...
22 KB (1,762 words) - 07:49, 22 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
182 KB (19,658 words) - 01:43, 10 December 2024
from outside). Kvα11.x - ether-a-go-go potassium channels: Kv11.1 (KCNH2) - hERG, Kv11.2 (KCNH6), Kv11.3 (KCNH7) Kvα12.x: Kv12.1 (KCNH8), Kv12.2 (KCNH3),...
17 KB (1,772 words) - 00:46, 21 December 2024
JJC8-016 is blocking a specific protein (hERG) that can lead to heart problems (potent inhibition of the hERG antitarget and predicted cardiotoxicity)...
37 KB (3,544 words) - 04:47, 8 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
45 KB (4,739 words) - 19:13, 18 December 2024
Quinidine (category HERG blocker)
also blocks certain voltage-gated potassium channels (e.g., Kv1.4, Kv4.2, hERG, among others), acts as an antimuscarinic and alpha-1 blocker, and is an...
19 KB (1,911 words) - 19:11, 13 December 2024
not exhibit anticholinergic effects. It shows negligible inhibition of the hERG channel (IC50Tooltip half-maximal inhibitory concentration > 30 μM) and no...
36 KB (3,344 words) - 08:22, 30 November 2024
JJC8-016 (category HERG blocker)
~2-fold lower affinity for the hERG. Newer related modafinil analogues and DRIs with further reduced affinity for the hERG were also subsequently developed...
11 KB (1,041 words) - 01:49, 19 November 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
107 KB (10,914 words) - 19:11, 21 December 2024
Noribogaine (category HERG blocker)
does ibogaine. Noribogaine is a hERG inhibitor and appears at least as potent as ibogaine. The inhibition of the hERG potassium channel delays the repolarization...
10 KB (879 words) - 18:04, 21 October 2024
voltage-gated potassium channels Kv7.2/ Kv7.3, Kv7.1, Kv7.1/KCNE1, and hERG. Inhibition of serotonin and norepinephrine transporters by amitriptyline...
93 KB (8,733 words) - 03:33, 16 December 2024
Astemizole (category HERG blocker)
fatal side effects (QTc interval prolongation and related arrhythmias due to hERG channel blockade). Astemizole is a histamine H1-receptor antagonist. It has...
7 KB (522 words) - 16:34, 23 September 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
97 KB (10,572 words) - 06:06, 10 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
73 KB (8,203 words) - 16:33, 21 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
34 KB (3,220 words) - 08:27, 22 December 2024
Quinidine ShK-186 Sotalol Tedisamil Terikalant Tetraethylammonium Vernakalant hERG (KCNH2, Kv11.1)-specific: Ajmaline Amiodarone AmmTX3 Astemizole Azaspiracid...
51 KB (4,686 words) - 22:41, 9 December 2024
scorpion Centruroides margaritatus. It blocks human ether-a-go-go-Related gene (hERG) potassium channels, which are important for cardiac action potential repolarization...
8 KB (1,043 words) - 20:09, 8 September 2024