Protein Information

Name TRPV1
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…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
18255104 Guenthner CJ, McCaughey SA, Tordoff MG, Baird JP: Licking for taste solutions by potassium-deprived rats: specificity and mechanisms. Physiol Behav. 2008 Mar 18;93(4-5):937-46. Epub 2007 Dec 26.

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.
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 capsaicin-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol. 2007 Mar;375(1):29-38. Epub 2007 Feb 13.

Capsaicin, 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).
2(0,0,0,2) Details
16360146 Fujimoto S, Mori M, Tsushima H, Kunimatsu M: Capsaicin-induced, capsazepine-insensitive relaxation of the guinea-pig 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 capsaicin 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.
1(0,0,0,1) Details
12223577 Bailey TW, Jin YH, Doyle MW, Andresen MC: Vanilloid-sensitive afferents activate neurons with prominent A-type potassium 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 capsaicin (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 potassium 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)-1H-imidazole hydrochloride (SKF96365), two potassium channel blockers, tetraethylammonium (TEA) and 4-aminopyridine, and an inhibitor of capacitative calcium entry, 1-(2-(trifluoromethyl) phenyl) imidazole (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 anandamide. 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 capsaicin (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 chloride (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 anandamide in G3 but not G0.
0(0,0,0,0) Details