| Name | TREK 1 |
|---|---|
| Synonyms | KCNK 2; KCNK2; Outward rectifying potassium channel protein TREK 1; Potassium channel subfamily K member 2; Potassium inwardly rectifying channel subfamily K member 2; TPKC 1; TPKC1; TREK… |
| Name | 4-aminopyridine |
|---|---|
| CAS | 4-pyridinamine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15608074 | Tertyshnikova S, Knox RJ, Plym MJ, Thalody G, Griffin C, Neelands T, Harden DG, Signor L, Weaver D, Myers RA, Lodge NJ: BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine] : a putative potassium channel opener with bladder-relaxant properties. J Pharmacol Exp Ther. 2005 Apr;313(1):250-9. Epub 2004 Dec 17. A survey of channels exhibiting sensitivity to extracellular Ba2+ at millimolar concentration revealed that the expression of the K2P2.1 (TREK-1) channel was relatively high in human bladder cells versus human aortic cells, suggesting this channel as a possible candidate target for BL-1249. The BL-1249-evoked outward K+ current was insensitive to blockade by glyburide, tetraethylammonium, iberiotoxin, 4-aminopyridine, apamin, or Mg2+. |
1(0,0,0,1) | Details |
| 16565299 | Bryan RM Jr, You J, Phillips SC, Andresen JJ, Lloyd EE, Rogers PA, Dryer SE, Marrelli SP: Evidence for two-pore domain channels in rat cerebral arteries. Am J Physiol Heart Circ Physiol. 2006 Aug;291(2):H770-80. Epub 2006 Mar 24. RT-PCR revealed message for the following AA-sensitive K (2P) channels in rat MCA: tandem of P domains in weak inward rectifier K+ (TWIK-2), TWIK-related K+ (TREK-1 and TREK-2), TWIK-related AA-stimulated K+ (TRAAK), and TWIK-related halothane-inhibited K+ (THIK-1) channels. AA-induced dilation was not affected by inhibition of cyclooxygenase, epoxygenase, or lipoxygenase or inhibition of classical K+ channels with 10 mM TEA, 3 mM 4-aminopyridine, 10 microM glibenclamide, or 100 microM Ba2+. |
1(0,0,0,1) | Details |
| 12680846 | Aimond F, Fauconnier J, Donadille D, Vassort G: The p42/44mitogen-activated protein kinase inhibitor PD 98059, but not U 0126, increases a K+ current in cardiomyocytes. Clin Exp Pharmacol Physiol. 2003 Apr;30(4):273-7. These observations indicate that PD 98059 activates a TREK-1 like current. |
1(0,0,0,1) | Details |
| 17828284 | Westphalen RI, Krivitski M, Amarosa A, Guy N, Hemmings HC Jr: Reduced inhibition of cortical and release by halothane in mice lacking the K+ channel, TREK-1. Br J Pharmacol. 2007 Nov;152(6):939-45. Epub 2007 Sep 10. KEY RESULTS: Deletion of TREK-1 significantly reduced the potency of halothane inhibition of 4-aminopyridine-evoked release of both and without affecting control evoked release or the selective inhibition of vs release. |
93(1,1,2,8) | Details |
| 17659475 | Mathie A, Veale EL: Therapeutic potential of neuronal two-pore domain potassium-channel modulators. Curr Opin Investig Drugs. 2007 Jul;8(7):555-62. Although not inhibited by classical potassium channel-blocking drugs, such as tetraethylammonium and 4-aminopyridine, K2P channels are regulated by a diverse array of pharmacological mediators. There are six main families of K2P channels and among these certain members of the TREK family (ie, TREK-1 and TREK-2) are activated by general anesthetic agents such as halothane, xenon and nitrous oxide. |
3(0,0,0,3) | Details |
| 15066906 | Gardener MJ, Johnson IT, Burnham MP, Edwards G, Heagerty AM, Weston AH: Functional evidence of a role for two-pore domain channels in rat mesenteric and pulmonary arteries. Br J Pharmacol. 2004 May;142(1):192-202. Epub 2004 Apr 5. RT-PCR demonstrated the expression of TASK-1, TASK-2, THIK-1, TRAAK, TREK-1, TWIK-1 and TWIK-2 in mesenteric arteries and TASK-1, TASK-2, THIK-1, TREK-2 and TWIK-2 in pulmonary arteries. K (+) channel blockade by 4-aminopyridine (4-AP) (5 mm), tetraethylammonium (TEA) (10 mm), Ba (2+) (30 microm) and glibenclamide (10 microm) depolarised the pulmonary artery. |
2(0,0,0,2) | Details |
| 12559116 | Lesage F: Pharmacology of neuronal background channels. Neuropharmacology. 2003 Jan;44(1):1-7. In the nervous system, the main representatives of this family are the TASK and TREK channels. They are relatively insensitive to the broad-spectrum K (+) channel blockers tetraethylammonium (TEA), 4-aminopyridine (4-AP), Cs (+), and Ba (2+). |
2(0,0,0,2) | Details |