Protein Information

Name calcitonin gene related peptide
Synonyms Alpha type CGRP; CT; CGRP; CALC 1; CALC1; CALCA; CGRP 1; CGRP I…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
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).
5(0,0,0,5) Details
15790910 Boussery K, Delaey C, Van de Voorde J: The vasorelaxing effect of CGRP and natriuretic peptides in isolated bovine retinal arteries. Invest Ophthalmol Vis Sci. 2005 Apr;46(4):1420-7.

The nonselective K (+) channel blocker tetraethylammoniumchloride (TEA) and the voltage-dependent K (+) channel blocker 4-aminopyridine significantly reduced the CGRP response, whereas the Ca (2+) activated K (+) channel blockers apamin plus charybdotoxin, the inward rectifier K (+) channel blocker Ba (2+), and the adenosine triphosphate (ATP)-sensitive K (+) channel blocker glibenclamide had no effect.
4(0,0,0,4) Details
17379634 Tan JH, Al Abed A, Brock JA: Inhibition of KATP channels in the rat tail artery by neurally released noradrenaline acting on postjunctional alpha2-adrenoceptors. J Physiol. 2007 Jun 1;581(Pt 2):757-65. Epub 2007 Mar 22.

A high concentration of Ba (2+)(1 mM), which would be expected to block K (ATP) channels, abolished the NAD, whereas teteraethylammonium (1 mM) and 4-aminopyridine (1 mM) increased its amplitude.
Activation of K (ATP) channels with calcitonin gene-related peptide (CGRP; 10 nM) also hyperpolarized the smooth muscle and decreased membrane resistance.
3(0,0,0,3) Details
18692643 Zulli A, Ye B, Wookey PJ, Buxton BF, Hare DL: Calcitonin gene-related peptide inhibits angiotensin II-mediated vasoconstriction in human radial arteries: role of the Kir channel. J Thorac Cardiovasc Surg. 2008 Aug;136(2):370-5. Epub 2008 Jun 19.

N-nitro-L-arginine methyl ester, 4-aminopyridine, charybdotoxin, and apamin had no effect on calcitonin gene-related peptide relaxation, but Ba (2+) impaired the effects of alpha-calcitonin gene-related peptide.
8(0,0,0,8) Details
17533425 Nguyen DT, Lang RJ, Exintaris B: K+ channel modulation of slow wave activity in the guinea-pig prostate. . Br J Pharmacol. 2007 Jul;151(6):828-36. Epub 2007 May 29.

KEY RESULTS: Tetraethylammonium (TEA 300 micro M and 1 mM), iberiotoxin (150 nM) and 4-aminopyridine (4-AP 1 mM) increased the frequency of slow wave discharge.
Lemakalim (1 micro M) and PCO-400 (1 micro M) abolished the slow waves, as did sodium nitroprusside (SNP 10 micro M) and calcitonin gene-related peptide (CGRP 100 nM).
3(0,0,0,3) Details
14976323 Erdos B, Simandle SA, Snipes JA, Miller AW, Busija DW: Potassium channel dysfunction in cerebral arteries of insulin-resistant rats is mediated by reactive oxygen species. Stroke. 2004 Apr;35(4):964-9. Epub 2004 Feb 19.

Blockade of the K (ir) and K (v) channels with Ba2+ and 4-aminopyridine, respectively, constricted the MCAs in both experimental groups with no significant difference.
IR also reduced the K (ATP) channel-dependent component in calcitonin gene-related peptide-induced dilation; however, the magnitude of the relaxation remained unchanged in IR because of a nonspecified K+ channel-mediated compensatory mechanism.
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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 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.
0(0,0,0,0) Details
10611463 Andre E, Malheiros A, Cechinel-Filho V, Yunes RA, Calixto JB: Mechanisms underlying the relaxation caused by the sesquiterpene polygodial in vessels from rabbit and guinea-pig. Eur J Pharmacol. 1999 Dec 10;386(1):47-53.


In contrast, N (omega)-nitro-D-arginine (D-NOARG), indomethacin, N (2)-[(4R)-4-hydroxy-1-(1methyl-1H-indol-3yl) carbonyl-L-prol yl]-N-met hyl-N-phenylmethyl-3-(2-naphthyl)-L-alaninamide (FK 888), (S)-N-methyl-N [4-(4-acetylamino-4-phenylpiperidino)-2-(3, 4-dichlorophenyl) butyl] benzamide (SR 48968), (8R,9S, 11S)-(-)-9-hydroxy-9-n-hexyloxy-carbonyl-8-methyl-2,3,9, 20-tetrahydro-8,11-epoxy-1H,8H,11H-2,7b,11a-triaqzadibenzo [a, g] cycloocta [c,d,e]-trinden-1-one (KT 5720), calcitocin gene-related peptide receptor antagonist (CGRP-(8-37), apamin, charybdotoxin and 4-aminopyridine had no effect on polygodial action.
0(0,0,0,0) Details