Protein Information

Name adenylate cyclase
Synonyms AH related protein; HCA2; ATP pyrophosphate lyase; Adenylate cyclase; Adenylyl cyclase soluble; HCA 2; RP1 313L4.2; SAC…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
15034129 Daniel H, Rancillac A, Crepel F: Mechanisms underlying cannabinoid inhibition of presynaptic Ca2+ influx at parallel fibre synapses of the rat cerebellum. J Physiol. 2004 May 15;557(Pt 1):159-74. Epub 2004 Mar 19.

The present study demonstrates that the molecular mechanisms underlying the CB1 inhibitory effect involve the activation of the PTX-sensitive G (i)/G (o) subclass of G proteins, independently of any direct effect on presynaptic Ca (2+) channels (N, P/Q and R (SNX-482-sensitive) types) or on adenylate cyclase or MAPK activity, but do require the activation of G protein-gated inwardly rectifying (Ba (2+)- and tertiapin Q-sensitive) K (+) channels, in addition to 4-aminopyridine-sensitive K (+) channels.
82(1,1,1,2) Details
16234412 Lin RJ, Wu BN, Lo YC, An LM, Dai ZK, Lin YT, Tang CS, Chen IJ: A xanthine-based epithelium-dependent airway relaxant KMUP-3 (7-[2-[4-(4-nitrobenzene) piperazinyl] ethyl]-1,3-dimethylxanthine) increases respiratory performance and protects against tumor necrosis factor-alpha-induced tracheal contraction, involving nitric oxide release and expression of cGMP and protein kinase G. J Pharmacol Exp Ther. 2006 Feb;316(2):709-17. Epub 2005 Oct 18.

In isolated trachea precontracted with carbachol, KMUP-3 (10-100 microM)-caused relaxations were attenuated by epithelium removal and by pretreatments with an inhibitor of K (+) channel, tetraethylammonium (10 mm); K (ATP) channel, glibenclamide (1 microM); voltage-dependent K (+) channel, 4-aminopyridine (100 microM); Ca (2+)-dependent K (+) channel, charybdotoxin (0.1 microM) or apamin (1 microM); soluble guanylate cyclase (sGC), 1H-[1,2,4] oxadiazolo [4,3-a] quinoxalin-1one (ODQ, 1 microM); nitric-oxide (NO) synthase, N (omega)-nitro-L-arginine methyl ester (L-NAME, 100 microM); and adenylate cyclase, SQ 22536 [9-(terahydro-2-furanyl)-9H-purin-6-amine] (100 microM).
31(0,1,1,1) Details
15237094 Wu BN, Lin RJ, Lo YC, Shen KP, Wang CC, Lin YT, Chen IJ: KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. Epub 2004 Jul 5.

Tracheal relaxation induced by KMUP-1 was attenuated by epithelium removal and by pretreatment with inhibitors of soluble guanylate cyclase (sGC) (1H-[1,2,4] oxadiazolo [4,3-a] quinoxalin-1-one (ODQ), 1 microm), nitric oxide synthase (Nomega-nitro-L-arginine methyl ester, 100 microm), K+ channels (tetraethylammonium, 10 mm), KATP channels (glibenclamide, 1 microm), voltage-dependent K+ channels (4-aminopyridine, 100 microm) and Ca2+-dependent K+ channels (charybdotoxin, 0.1 microm or apamin, 1 microm).
These increases in cyclic AMP and cyclic GMP were abolished in the presence of an adenylate cyclase inhibitor SQ 22536 (100 microm) and an sGC inhibitor ODQ (10 microm), respectively.
1(0,0,0,1) Details
16436472 Xu F, Xu J, Tse FW, Tse A: Adenosine stimulates depolarization and rise in cytoplasmic [Ca2+] in type I cells of rat carotid bodies. Am J Physiol Cell Physiol. 2006 Jun;290(6):C1592-8. Epub 2006 Jan 25.

Our results suggest that adenosine, acting via the adenylate cyclase and PKA pathways, inhibits the TASK-1 K+ channels.
Although adenosine was reported to inhibit a 4-aminopyridine (4-AP)-sensitive K+ current, 4-AP failed to trigger any [Ca2+] i rise, or to attenuate the adenosine response.
1(0,0,0,1) Details
11801366 Doi A, Ishibashi H, Jinno S, Kosaka T, Akaike N: Presynaptic inhibition of GABAergic miniature currents by metabotropic glutamate receptor in the rat CNS. Neuroscience. 2002;109(2):299-311.

The application of K+ channel blockers such as 4-aminopyridine, Cs+, Ba2+ or tetraethylammonium increased the mIPSC frequency, but failed to inhibit the tACPD action on mIPSC.
Forskolin, an activator of adenylate cyclase, facilitated the mIPSC frequency in a concentration-dependent manner and inhibited the tACPD-induced suppression of mIPSC frequency. 8-Br-cAMP, a membrane permeable analog of cAMP, also prevented the inhibitory action of tACPD.
1(0,0,0,1) Details
16153635 Zhang Y, Pertens E, Janssen LJ: 8-isoprostaglandin E (2) activates Ca (2+)-dependent K (+) current via cyclic AMP signaling pathway in murine renal artery. Eur J Pharmacol. 2005 Sep 27;520(1-3):22-8.

This augmentation was observed in the presence of 4-aminopyridine (4-AP, 10 (-3) M) but not that of charybdotoxin (Ch Tx, 10 (-7) M).
The isoprostane-induced augmentation was prevented by the ryanodine receptor blocker ruthenium red (10 (-5) M) or the adenylate cyclase blocker SQ 22536 (10 (-4) M).
1(0,0,0,1) Details
11284450 Tanaka Y, Mitani A, Igarashi T, Someya S, Otsuka K, Imai T, Yamaki F, Tanaka H, Saitoh M, Nakazawa T, Noguchi K, Hashimoto K, Shigenobu K: HNS-32, a novel azulene-1-carboxamidine derivative, inhibits nifedipine-sensitive and -insensitive contraction of the isolated rabbit aorta. Naunyn Schmiedebergs Arch Pharmacol. 2001 Mar;363(3):344-52.


Relaxation elicited by HNS-32 was not affected by the adenylate cyclase inhibitor, 9-(tetrahydro-2'-furyl) adenine (SQ 22,536, 10 (-4) M), the soluble guanylate cyclase inhibitor, 1H-(1,2,4)-oxadiazolo-(4,3-a)-quinoxalin-1-one (ODQ, 10 (-5) M) or a cocktail of K+ channel blockers (glybenclamide 10 (-6) M, tetraethylammonium 2x10 (-3) M, apamin 10 (-7) M, 4-aminopyridine 10 (-4) M and Ba2+ 10 (-5) M).
0(0,0,0,0) Details
19919833 Dhaese I, Van Colen I, Lefebvre RA: Mechanisms of action of hydrogen sulfide in relaxation of mouse distal colonic smooth muscle. Eur J Pharmacol. 2010 Feb 25;628(1-3):179-86. Epub 2009 Nov 15.


The NaHS-induced relaxation was not influenced by the K (+) channels blockers glibenclamide, apamin, charybdotoxin, barium chloride and 4-aminopyridine.
0(0,0,0,0) Details
16151435 Wu BN, Tu HF, Welsh DG, Chen IJ: KMUP-1 activates BKCa channels in basilar artery myocytes via cyclic nucleotide-dependent protein kinases. Br J Pharmacol. 2005 Nov;146(6):862-71.


BKCa current activation by KMUP-1 was markedly inhibited by a soluble guanylate cyclase inhibitor (ODQ 10 microM), an adenylate cyclase inhibitor (SQ 22536 10 microM), competitive antagonists of cGMP and cAMP (Rp-cGMP, 100 microM and Rp-cAMP, 100 microM), and cGMP- and cAMP-dependent protein kinase inhibitors (KT5823, 300 nM and KT5720, 300 nM).
1(0,0,0,1) Details
15201307 Yang K, Fujita T, Kumamoto E: Adenosine inhibits GABAergic and glycinergic transmission in adult rat substantia gelatinosa neurons. J Neurophysiol. 2004 Nov;92(5):2867-77. Epub 2004 Jun 16.


This reduction in frequency disappeared in the presence of a K+ -channel blocker (4-aminopyridine) but not in the absence of Ca2+.
0(0,0,0,0) Details
11150326 Robbe D, Alonso G, Duchamp F, Bockaert J, Manzoni OJ: Localization and mechanisms of action of cannabinoid receptors at the glutamatergic synapses of the mouse nucleus accumbens. J Neurosci. 2001 Jan 1;21(1):109-16.


The K (+) channel blockers 4-aminopyridine (100 micrometer) and BaCl (2) (300 micrometer) each reduced by 40-50% the inhibitory actions of WIN-2, and their effects were additive.
0(0,0,0,0) Details
12548092 Andre E, Malheiros A, Cechinel-Filho V, Yunes RA, Calixto JB: Role of nitric oxide and K+ channels in relaxation induced by polygodial in rabbit corpus cavernosum in vitro. J Cardiovasc Pharmacol. 2003 Feb;41(2):300-6.


In contrast, apamin, charybdotoxin, and 4-aminopyridine or the protein kinase A inhibitor KT 5720 all failed to affect either polygodial or ACh-mediated relaxation in these preparations.
0(0,0,0,0) Details
12491798 Horinouchi T, Tanaka Y, Koike K: [Beta 3-adrenoceptor-mediated relaxation of guinea-pig gastric funds smooth muscle: cAMP-independent characteristics and a primary role of 4-aminopyridine-sensitive voltage-dependent K+ (Kv) channels]. Nippon Yakurigaku Zasshi. 2002 Nov;120(1):109P-111P.

0(0,0,0,0) Details