Name | adenylyl cyclase |
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Synonyms | ADCY 7; ATP pyrophosphate lyase; Adenylyl cyclase; ADCY7; ADCY7 protein; ATP pyrophosphate lyase 7; Adenylate cyclase 7; Adenylate cyclase type 7… |
Name | 4-aminopyridine |
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CAS | 4-pyridinamine |
PubMed | Abstract | RScore(About this table) | |
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12626609 | Jeong HJ, Jang IS, Nabekura J, Akaike N: Adenosine A1 receptor-mediated presynaptic inhibition of GABAergic transmission in immature rat hippocampal CA1 neurons. J Neurophysiol. 2003 Mar;89(3):1214-22. K (+) channel blockers, 4-aminopyridine (100 microM) and Ba (2+) (1 mM), had no effect on the inhibitory effect of CPA on GABAergic mIPSC frequency. Stimulation of adenylyl cyclase with forskolin (10 microM) prevented the CPA action on GABAergic mIPSC frequency. |
1(0,0,0,1) | Details |
18832757 | Heaps CL, Jeffery EC, Laine GA, Price EM, Bowles DK: Effects of exercise training and hypercholesterolemia on activation of voltage-dependent K+ channels in coronary arterioles. J Appl Physiol. 2008 Dec;105(6):1761-71. Epub 2008 Oct 2. For the present study, we tested the hypotheses that exercise training would correct impaired -induced dilatation in coronary arterioles from hypercholesterolemic pigs through restoration of activation of Kv channels and that vasodilatation to the receptor-independent adenylyl cyclase activator, forskolin, would also be attenuated in arterioles from hypercholesterolemic pigs. Arterioles ( approximately 150 mum) from both HC-Sed and HC-Ex pigs displayed impaired -mediated dilatation that was attributable to the elimination of 4-aminopyridine (4-AP; 1 mM)-sensitive Kv channel activation compared with NC counterparts. |
1(0,0,0,1) | Details |
11786491 | McGuire JJ, Hollenberg MD, Andrade-Gordon P, Triggle CR: Multiple mechanisms of vascular smooth muscle relaxation by the activation of proteinase-activated receptor 2 in mouse mesenteric arterioles. Br J Pharmacol. 2002 Jan;135(1):155-69. Activation of PAR2 in second-order mesenteric arteriole (MA) rings from C57BL/6J, NOS3 (-/-) and PAR2 (-/-) mice was assessed for the contributions of NO, cyclo-oxygenases, guanylyl cyclase, adenylyl cyclase, and of K (+) channel activation to vascular smooth muscle relaxation. 2. Tetraethylammonium (TEA), glibenclamide, tetrodotoxin, 17-octadecynoic acid, carboxy-2-phenyl-4,4,5,5,-tetramethyl-imidazoline-1-oxyl-3-oxide, SQ22536, carbenoxolone, arachidonyl trifluoromethyl ketone, 7-nitroindazole, N-(3-(aminomethyl) benzyl) acetamidine (1400W), N-(2-cyclohexyloxy- -methanesulfonamide (NS-398) and did not inhibit relaxation. 4-aminopyridine significantly increased the potency of SLIGRL-NH (2). |
1(0,0,0,1) | Details |
15066141 | Mei YA, Vaudry D, Basille M, Castel H, Fournier A, Vaudry H, Gonzalez BJ: PACAP inhibits delayed rectifier current via a cAMP/PKA transduction pathway: evidence for the involvement of I k in the anti-apoptotic action of PACAP. Eur J Neurosci. 2004 Mar;19(6):1446-58. Taken together, the present results demonstrate that, in rat cerebellar granule cells, PACAP reduces the delayed outward rectifier K (+) current by activating a type 1 PACAP (PAC1) receptor coupled to the adenylyl cyclase/protein kinase A pathway through a cholera toxin-sensitive Gs protein. |
1(0,0,0,1) | Details |
17606273 | Mato S, Lafourcade M, Robbe D, Bakiri Y, Manzoni OJ: Role of the cyclic-AMP/PKA cascade and of P/Q-type Ca++ channels in endocannabinoid-mediated long-term depression in the nucleus accumbens. Neuropharmacology. 2008 Jan;54(1):87-94. Epub 2007 May 5. In contrast, eCB-LTD was blocked by treatment of the slices with the adenylyl cyclase (AC) activator forskolin (10 microM), and with the protein kinase A (PKA) inhibitor KT5720 (1 microM) (fEPSP=108.9+/-5.7% in forskolin and 110.5+/-7.7% in KT5720, compared to 80.6+/-3.9% in control conditions). |
1(0,0,0,1) | Details |
16920098 | Jarajapu YP, Oomen C, Uteshev VV, Knot HJ: The dilation was not affected by iberiotoxin, barium and glibenclamide but was strongly antagonized by 4-aminopyridine (0.3 mM) and tetraethylammonium (10 mM) (pEC (50): control: 5.6+/-0.1, 4-aminopyridine: 4.1+/-0.1 (P <0.001); tetraethylammonium 3.2+/-0.2 (P <0.0001)). |
decreases myogenic tone in rat cerebral arteries by H2-receptor-mediated KV channel activation, independent of endothelium and cyclic AMP. Eur J Pharmacol. 2006 Oct 10;547(1-3):116-24. Epub 2006 Jul 27.0(0,0,0,0) | Details |
18493242 | Xu YC, Leung GP, Wong PY, Vanhoutte PM, Man RY: activated K+ (BKCa) channels in human umbilical vein endothelial cells via a cAMP/PKA-dependent pathway. Br J Pharmacol. 2008 Jul;154(6):1247-53. Epub 2008 May 19. This -induced current was abolished by large conductance Ca2+ -activated K+ (BKCa) channel blockers, such as iberiotoxin (IbTX) and charybdotoxin (ChTX), whereas the small conductance Ca2+ -activated K+ (SKCa) channel blocker, apamin, and the voltage-dependent K+ (KV) channel blocker, 4-aminopyridine, had no effect. |
stimulates large conductance Ca2+ -0(0,0,0,0) | Details |
12684454 | Dong Y, White FJ: receptors selectively modulate a slowly inactivating current in rat medial prefrontal cortex pyramidal neurons. J Neurosci. 2003 Apr 1;23(7):2686-95. Stimulation of DA D1Rs selectively suppressed I (D), an effect mimicked by the adenylyl cyclase activator forskolin, the active cAMP analog Sp-cAMP, and the protein phosphatase inhibitor okadaic acid. The A-type current (I (A)), with rapid activation and inactivation kinetics, was completely inactivated by prolonged holding of the membrane potential at -40 mV and was sensitive to the K (+) channel blocker 4-aminopyridine (4-AP) but not tetraethylammonium (TEA) or dendrotoxin (DTX). |
D1-class 1(0,0,0,1) | Details |
11219402 | Blandizzi C, Colucci R, Tognetti M, De Paolis B, Del Tacca M: H3 receptor-mediated inhibition of intestinal release: pharmacological characterization of signal transduction pathways. Naunyn Schmiedebergs Arch Pharmacol. 2001 Feb;363(2):193-202. Tetraethylammonium or 4-aminopyridine, acting as inhibitors of voltage-dependent K+ channels, enhanced the evoked tritium outflow when tested alone, and apparently counteracted the inhibitory effect of |
0(0,0,0,0) | Details |
11770009 | Yamaki F, Kaga M, Horinouchi T, Tanaka H, Koike K, Shigenobu K, Toro L, Tanaka Y: MaxiK channel-mediated relaxation of guinea-pig aorta following stimulation of IP receptor with beraprost via cyclic AMP-dependent and -independent mechanisms. Naunyn Schmiedebergs Arch Pharmacol. 2001 Dec;364(6):538-50. Moreover, cholera toxin (CTX, 1 microg/ml for 6 h), which activates the stimulatory G protein of adenylyl cyclase (Gs), significantly suppressed PGF2alpha-induced contraction both in the absence and presence of SQ 22,536 (10 (-4) M). The relaxation induced by beraprost was not significantly affected by other K+ channel blockers glibenclamide (10 (-6) M) or Ba2+ (10 (-5) M), but was slightly attenuated by 4-aminopyridine (10 (-4) M). |
1(0,0,0,1) | Details |
15973968 | Chai Q, Liu Z, Chen L: Effects of streptozotocin-induced diabetes on Kv channels in rat small coronary smooth muscle cells. Chin J Physiol. 2005 Mar 31;48(1):57-63. STZ-induced diabetes appeared to [corrected] reduce the vasodilation induced by beta-adrenoceptor agonist, isoproterenol (10 (-9)-10 (-5) mol/l), and adenylyl cyclase activator forskolin (10 (-9)-10 (-5) mol/l) respectively (isoproterenol: 44.2 +/- 6.7% vs. 82.5 +/- 4.8%, and forskolin: 54.4 +/- 4.5% vs. 94.3 +/- 2.4%). 4-AP, a Kv channel blocker of VSMC, further decreased dilation to isoproterenol (44.2 +/- 6.7% vs. 10.2 +/- 3.5%) and forskolin (54.4 +/- 4.5% vs. 13.8 +/- 11.0%) significantly. |
1(0,0,0,1) | Details |
12595962 | Horinouchi T, Tanaka Y, Koike K: Evidence for the primary role for 4-aminopyridine-sensitive K (v) channels in beta (3)-adrenoceptor-mediated, cyclic AMP-independent relaxations of guinea-pig gastrointestinal smooth muscles. Naunyn Schmiedebergs Arch Pharmacol. 2003 Feb;367(2):193-203. Epub 2003 Jan 14. The relaxations were unaffected by an adenylyl cyclase inhibitor, SQ-22536 (100 microM), which indicates their characteristic of cyclic AMP-independency. |
1(0,0,0,1) | Details |
15196683 | Borasio PG, Cervellati F, Pavan B, Pareschi MC: "Low" concentrations of inhibit neurotransmitter release from the guinea-pig superior cervical ganglion. Neurosci Lett. 2004 Jul 1;364(2):86-9. The electrically evoked (1 Hz, 5 min) [3H] release was inhibited by "low" F- concentrations (1-2.5 mM), by the adenylyl cyclase blocker MDL 12330A (10 microM), alone and in combination with 1 mM NaF, and increased by 0.5 mM 8Br-cAMP, 100 microM forskolin and 0.5 mM 3-isobutyl-1-methylxantine. -induced inhibition was counteracted by the G protein blocker sulmazole (1 mM), forskolin and alteration of influx by increasing [Ca2+] out from 2.2 to 6 mM, raising the rate of stimulation (10 Hz, 30 s), or broadening the presynaptic action potential with 10 microM 4-aminopyridine and 50 microM tetraethylammonium |
1(0,0,0,1) | Details |
17322023 | Moritz A, Gust R, Pertz HH: Characterization of the relaxant response to N,N'-dipropyl-1,2-bis (2,6-dichloro-4-hydroxyphenyl) ethylenediamine in porcine coronary arteries. J Pharmacol Exp Ther. 2007 May;321(2):699-706. Epub 2007 Feb 22. The relaxant response to 8 was unaffected by the estrogen receptor antagonist ICI 182,780 (7alpha-[9-[(4,4,5,5,5-pentafluoropentyl]-sulfinyl] nonyl]-estra-1,3,5 (10)- triene-3,17beta-diol) and K+ channel blockers, i.e., TEA, glibenclamide, and 4-aminopyridine. Furthermore, the vasodilatory effect of 8 was unaffected by the adenylyl cyclase inhibitor SQ 22536 [9-(tetrahydro-2-furanyl)- the guanylyl cyclase inhibitor ODQ [1H-[1,2,4] oxadiazolo [4,3-a] quinoxalin-1-one], the protein kinase A inhibitor KT 5720 [(9S,10S,12R)-2,3,9,10,11,12-hexahydro-10- -9-methyl-1-oxo-9,12-epox y-1H-diindolo [1,2,3-fg: 3',2',1'-kl] pyrrolo [3,4-i][1,6] benzodiazocine-10-carboxylic acid hexyl ester], the protein kinase G inhibitor KT 5823 [(9S,10R,12R)-2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl-1-oxo-9,12- epoxy-1H-diindolo [1,2,3-fg:3',2',1'-kl] pyrrolo [3,4-i][1,6] benzodiazocine-1 0-carboxylic acid methyl ester], and the p38 mitogen-activated protein kinase (MAPK) inhibitor SB 203580 [4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)- . |
1(0,0,0,1) | Details |
11374068 | Su J, Yu H, Lenka N, Hescheler J, Ullrich S: The expression and regulation of depolarization-activated K+ channels in the insulin-secreting cell line INS-1. Pflugers Arch. 2001 Apr;442(1):49-56. Outward currents were inhibited by 4-aminopyridine (4-AP, 10 mmol/l), tetraethylammonium (TEA, 10 mmol/l) and tetrapentylammonium (TPeA, 100 mumol/l) by 55.1 +/- 3.8% (n = 3), 78.1 +/- 3.2% (n = 6) and 98.7 +/- 0.8% (n = 5), respectively. |
0(0,0,0,0) | Details |
12668054 | Wang SJ, Sihra TS: Opposing facilitatory and inhibitory modulation of release elicited by cAMP production in cerebrocortical nerve terminals (synaptosomes). Neuropharmacology. 2003 Apr;44(5):686-97. The adenylyl cyclase (AC) activator, forskolin, failed to have any effect on 4-aminopyridine (4-AP)-evoked release, when added alone. |
0(0,0,0,0) | Details |
17435380 | Matsushita M, Tanaka Y, Koike K: Studies on the mechanisms underlying beta-adrenoceptor-mediated relaxation of rat abdominal aorta. J Smooth Muscle Res. 2006 Dec;42(6):217-25. Isoprenaline-induced relaxation in the presence of SQ 22,536 was significantly diminished by iberiotoxin (IbTx, 0.1 microM), but was not affected by 4-aminopyridine (4-AP, 3 mM). |
0(0,0,0,0) | Details |
16019148 | Han P, Lucero MT: Pituitary adenylate cyclase activating polypeptide reduces A-type K+ currents and caspase activity in cultured adult mouse olfactory neurons. Neuroscience. 2005;134(3):745-56. Interestingly, we found that the protective effects of pituitary adenylate cyclase activating polypeptide were related to the absence of a 4-aminopyridine (IC50=144 microM) sensitive rapidly inactivating current often referred to as A-type current. |
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-NOARG), indomethacin, N (2)-[(4R)-4- -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- -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 |
18643787 | Qu L, Leung LS: Mechanisms of hyperthermia-induced depression of GABAergic synaptic transmission in the immature rat hippocampus. J Neurochem. 2008 Sep;106(5):2158-69. Epub 2008 Jul 15. These results suggest that hyperthermia reduces release from pre-synaptic terminals, in part by blocking the adenylyl cyclase-protein kinase A signaling pathway and activating pre-synaptic 4-aminopyridine-sensitive K (+) channels. |
32(0,1,1,2) | Details |
15589969 | Lo YC, Tsou HH, Lin RJ, Wu DC, Wu BN, Lin YT, Chen IJ: Endothelium-dependent and -independent vasorelaxation by a derivative MCPT: roles of cyclic nucleotides, potassium channel opening and phosphodiesterase inhibition. Life Sci. 2005 Jan 7;76(8):931-44. This relaxation was also reduced by the presence of synthase inhibitor Nomega-nitro- methylester (L-NAME, 100 microM), soluble guanylyl cyclase (sGC) inhibitors methylene blue (10 microM), 1 H-[1,2,4] oxidazolol [4,3-a] quinoxalin-1-one (ODQ, 1 microM), adenylyl cyclase (AC) blocker SQ 22536 (100 microM), ATP-sensitive K+ channel blocker (KATP) glibenclamide (1 microM), a Ca2+ activated K+ channels blocker tetraethylammonium (TEA, 10 mM) and a voltage-dependent channels blocker 4-aminopyridine (4-AP, 100 microM). |
31(0,1,1,1) | Details |
18539401 | Lee J, Ueda A, Wu CF: Pre- and post-synaptic mechanisms of synaptic strength homeostasis revealed by slowpoke and shaker K+ channel mutations in Drosophila. Neuroscience. 2008 Jul 17;154(4):1283-96. Epub 2008 May 2. Removal of Sh current in slo mutants by 4-aminopyridine blockade or by combining slo with Sh mutations led to strikingly increased synaptic transmission, suggesting upregulation of presynaptic Sh current to limit excessive neurotransmitter release in the absence of Slo current. Such compensatory regulations were prevented by rutabaga (rut) adenylyl cyclase mutations in rut slo double mutants, demonstrating a novel role of rut in homeostatic plasticity, in addition to its well-established function in learning behavior. |
1(0,0,0,1) | Details |
14727522 | Horinouchi T, Tanaka Y, Koike K: [beta-adrenoceptor subtypes involved in relaxations of guinea-pig gastrointestinal smooth muscles: distribution and signaling pathway of beta 3-adrenoceptors]. Nippon Yakurigaku Zasshi. 2003 Nov;122 Suppl:54P-56P. This was strongly supported by molecular analyses with RT-PCR, showing the expression of beta 3-adrenoceptor mRNA in the four tissues. beta 3-Adrenoceptor-mediated relaxations were unaffected by both an adenylyl cyclase inhibitor, SQ-22,536 (100 microM), and a PKA inhibitor, H-89 (10 microM), in guinea-pig gastric fundus smooth muscle. Furthermore, in the presence of SQ-22,536 (100 microM), the stimulation of beta 3-adrenoceptors elicited relaxations without an elevation of cAMP, indicating the involvement of cAMP-independent mechanism (s). beta 3-Adrenoceptor-mediated, cAMP-independent relaxations were significantly diminished by a Kv channel blocker, 4-aminopyridine (3 mM). |
1(0,0,0,1) | Details |