Name | TRPV1 |
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Synonyms | Capsaicin receptor; OTRPC 1; Osm 9 like TRP channel 1; TRP vanilloid 1; TRPV 1; TRPV1; Transient receptor potential cation channel subfamily V member 1… |
Name | 4-aminopyridine |
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CAS | 4-pyridinamine |
PubMed | Abstract | RScore(About this table) | |
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18255104 | Guenthner CJ, McCaughey SA, Tordoff MG, Baird JP: Licking for taste solutions by Licking was unaffected by addition to NaCl of 200 muM amiloride, an epithelial Na (+) channel (ENaC) blocker, or 100 muM ruthenium red, a vanilloid receptor 1 (VR-1) antagonist, or by addition to KCl of 50 muM 4-aminopyridine, a K (+) channel blocker. |
-deprived rats: specificity and mechanisms. Physiol Behav. 2008 Mar 18;93(4-5):937-46. Epub 2007 Dec 26.81(1,1,1,1) | Details |
17295025 | Gupta S, Lozano-Cuenca J, Villalon CM, de Vries R, Garrelds IM, Avezaat CJ, van Kats JP, Saxena PR, MaassenVanDenBrink A: Pharmacological characterisation of a pungent constituent from red chilli peppers, activates sensory nerve fibres via transient receptor potential vanilloid receptors type 1 (TRPV1) to release neuropeptides like calcitonin gene-related peptide (CGRP) and substance P. Further, we also used the K+ channel inhibitors 4-aminopyridine (1 mM), charybdotoxin (0.5 microM) + apamin (0.1 microM) and iberiotoxin (0.5 microM) + apamin (0.1 microM). |
-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol. 2007 Mar;375(1):29-38. Epub 2007 Feb 13.2(0,0,0,2) | Details |
16360146 | Fujimoto S, Mori M, Tsushima H, Kunimatsu M: ileum. Eur J Pharmacol. 2006 Jan 13;530(1-2):144-51. Epub 2005 Dec 19. The mechanisms underlying transient receptor potential vanilloid receptor type 1 (TRPV1)-independent relaxation elicited by were studied by measuring isometric force and phosphorylation of 20-kDa regulatory light chain subunit of myosin (MLC (20)) in ileum longitudinal smooth muscles of guinea-pigs. The relaxant response was attenuated by 4-aminopyridine and high-KCl solution, but not by capsazepine, tetraethylammonium, Ba (2+), glibenclamide, charybdotoxin plus apamin nor antagonists of cannabinoid receptor type 1 and calcitonin-gene related peptide. |
-induced, capsazepine-insensitive relaxation of the guinea-pig 1(0,0,0,1) | Details |
12223577 | Bailey TW, Jin YH, Doyle MW, Andresen MC: Vanilloid-sensitive afferents activate neurons with prominent A-type currents in nucleus tractus solitarius. J Neurosci. 2002 Sep 15;22(18):8230-7. In horizontal brainstem slices, we used the vanilloid receptor 1 agonist (CAP; 100 nm) to identify CAP-sensitive and CAP-resistant ST afferent pathways to second-order NTS neurons and tested whether these two groups of neurons had similar intrinsic currents. Steady-state currents were similar in both groups. 4-Aminopyridine or depolarized conditioning blocked the TOC, but tetraethylammonium had no effect. |
1(0,0,0,1) | Details |
17673572 | Juvin V, Penna A, Chemin J, Lin YL, Rassendren FA: Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxydiphenyl borate. Mol Pharmacol. 2007 Nov;72(5):1258-68. Epub 2007 Aug 2. Despite its expression in different cell types, transient receptor potential V2 (TRPV2) is still the most cryptic members of the TRPV channel family. 2-Aminoethoxydiphenyl borate (2APB) has been shown to be a common activator of TRPV1, TRPV2, and TRPV3, but 2APB-triggered TRPV2 activation remains to be thoroughly characterized. Besides the classic TRP inhibitors ruthenium red (RR) and 1-(beta-[3-(4-methoxyphenyl) propoxy]-4-methoxyphenethyl)- hydrochloride (SKF96365), two potassium channel blockers, tetraethylammonium (TEA) and 4-aminopyridine, and an inhibitor of capacitative entry, 1-(2-(trifluoromethyl) phenyl) (TRIM), were found to inhibit TRPV2 activation by 100 microM 2APB. |
1(0,0,0,1) | Details |
15821751 | O'Sullivan SE, Kendall DA, Randall MD: The effects of Delta9-tetrahydrocannabinol in rat mesenteric vasculature, and its interactions with the endocannabinoid Br J Pharmacol. 2005 Jun;145(4):514-26. 1 Delta9-tetrahydrocannabinol (THC) produces varying effects in mesenteric arteries: vasorelaxation (third-order branches, G3), modest vasorelaxation (G2), no effect (G1) and vasoconstriction (the superior mesenteric artery, G0). 2 In G3, vasorelaxation to THC was inhibited by pertussis toxin, but was unaffected by the CB1 receptor antagonist, AM251 (1 microM), incubation with the TRPV1 receptor agonist (10 microM, 1 h), the TRPV1 receptor antagonist capsazepine (10 microM) or de-endothelialisation. 3 In G3, vasorelaxation to THC was inhibited by high K+ buffer, and by the following K+ channel inhibitors: charybdotoxin (100 nM), apamin (500 nM) and barium (30 microM), but not by 4-aminopyridine, glibenclamide or tertiapin. 4 In G3, THC (10 and 100 microM) inhibited the contractile response to Ca2+ in a Ca2+-free, high potassium buffer, indicating that THC blocks Ca2+ influx. 5 In G0, the vasoconstrictor responses to THC were inhibited by de-endothelialisation and SR141716A (100 nM), but not by the endothelin (ET (A)) receptor antagonist FR139317 (1 microM).THC (1 and 10 microM) antagonised vasorelaxation to in G3 but not G0. |
0(0,0,0,0) | Details |