Protein Information

Name protein kinase A (protein family or complex)
Synonyms Protein kinase A; cAMP dependent protein kinase; cAMP dependent protein kinases

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
15680943 Zsombok A, Schrofner S, Hermann A, Kerschbaum HH: A cGMP-dependent cascade enhances an L-type-like Ca2+ current in identified snail neurons. Brain Res. 2005 Jan 25;1032(1-2):70-6.

Blockade of protein kinase activity with 1-[5-isoquinolinesulfonyl]-2 methyl piperazine (H 7), a nonselective protein kinase inhibitor, or Rp-8-pCPT-cGMP, a selective protein kinase G (PKG) inhibitor, decreased, whereas Rp-cAMP, a selective protein kinase A (PKA) inhibitor, increased the Ba (2+) current upon application of cGMP analogues or SNP.
31(0,1,1,1) Details
12211084 Thumen A, Qadri F, Sarkar R, Moser A: GBR-12909 effect on dopamine outflow depends on phosphorylation in the caudate nucleus of the rat. Synapse. 2002 Nov;46(2):72-8.

Activation of protein kinase A and C markedly enhanced the effect of GBR-12909, whereas protein kinase inhibition by H7 reduced the GBR-12909 effect.
These results suggest a complex and strong influence of phosphorylation on GBR-12909 effects on calcium channel-dependent DA outflow at low-affinity piperazine binding sites in slices of the rat caudate nucleus in vitro.
1(0,0,0,1) Details
17141281 Dong LY, Cheng ZX, Fu YM, Wang ZM, Zhu YH, Sun JL, Dong Y, Zheng P: Neurosteroid dehydroepiandrosterone sulfate enhances spontaneous glutamate release in rat prelimbic cortex through activation of dopamine D1 and sigma-1 receptor. Neuropharmacology. 2007 Mar;52(3):966-74. Epub 2006 Nov 30.


The results showed that dehydroepiandrosterone sulfate increased the frequency of miniature excitatory postsynaptic currents in the prelimbic cortex and hippocampus; sigma-1 receptor antagonist partially blocked the effect of dehydroepiandrosterone sulfate in the prelimbic cortex, but completely blocked it in the hippocampus; D1 receptor antagonist, adenylyl cyclase inhibitor and protein kinase A inhibitor completely blocked the effect of dehydroepiandrosterone sulfate in the prelimbic cortex; dehydroepiandrosterone sulfate increased the activity of protein kinase A in the prelimbic cortex and hippocampus; the effect of dehydroepiandrosterone sulfate on protein kinase A was completely blocked by sigma-1 receptor antagonist in the hippocampus, but was partially blocked in the prelimbic cortex; interestingly, here again, the effect of dehydroepiandrosterone sulfate on protein kinase A was completely blocked by D1 receptor antagonist in the prelimbic cortex.
1(0,0,0,1) Details
20164327 Zhang J, Huang XY, Ye ML, Luo CX, Wu HY, Hu Y, Zhou QG, Wu DL, Zhu LJ, Zhu DY: Neuronal nitric oxide synthase alteration accounts for the role of 5-HT1A receptor in modulating anxiety-related behaviors. J Neurosci. 2010 Feb 17;30(7):2433-41.


Blockade of hippocampal CREB phosphorylation by microinjection of H89 (5.19 microg/1.0 microl), a PKA (protein kinase A) inhibitor, abolished the anxiolytic-like effects of 7-NI (i.p., 30 mg/kg/d for 21 d).
1(0,0,0,1) Details
12417643 Wang X, Zhong P, Yan Z: Dopamine D4 receptors modulate GABAergic signaling in pyramidal neurons of prefrontal cortex. J Neurosci. 2002 Nov 1;22(21):9185-93.

To understand the cellular mechanisms and functional implications of D4 receptors, we examined the impact of D4 receptors in PFC pyramidal neurons on GABAergic inhibition, a key element in the regulation of "working memory." Application of the D4 agonist N-(methyl)-4-(2-cyanophenyl) piperazinyl-3-methylbenzamide maleate caused a reversible decrease in postsynaptic GABA (A) receptor currents; this effect was blocked by the D4 antagonist 3-[(4-[4-chlorophenyl] piperazine-1-yl) methyl]-[1H]-pyrrolo [2,3-b] pyridine but not by the D2 antagonist sulpiride, suggesting mediation by D4 receptors.
The D4 modulation of GABA (A) receptor currents was blocked by protein kinase A (PKA) activation and occluded by PKA inhibition.
1(0,0,0,1) Details
15456534 Zhang XF, Guo SZ, Lu KH, Li HY, Li XD, Zhang LX, Yang L: Different roles of PKC and PKA in effect of interferon-gamma on proliferation and collagen synthesis of fibroblasts. Acta Pharmacol Sin. 2004 Oct;25(10):1320-6.

The proliferation and collagen synthesis were enhanced by PKC activator (containing phosphatidylserine, diacylglycerol and Ca2+) and PKA inhibitor [H (7) 250 micromol/L, 1-(5-isoquinolinylsulfonyl)-2-methyl piperazine], and inhibited by PKC inhibitor (GF109 250 micromol/L) and PKA activator (cAMP 25 micromol/L) (P <0.01).
AIM: To study the signal roles of protein kinase C (PKC) and protein kinase A (PKA) in the influence of interferon-gamma (IFN-gamma) on proliferation and collagen synthesis of fibroblasts derived from hypertrophic scar (HS-FB) and normal skin (NS-FB).
1(0,0,0,1) Details
12466248 Wang SJ, Coutinho V, Sihra TS: Presynaptic cross-talk of beta-adrenoreceptor and 5-hydroxytryptamine receptor signalling in the modulation of glutamate release from cerebrocortical nerve terminals. Br J Pharmacol. 2002 Dec;137(8):1371-9.

The presynaptic interactions between facilitatory beta-adrenoreceptors and inhibitory 5-hydroxytryptamine (5-HT) receptors modulating glutamate release from cerebrocortical nerve terminals were examined. 2. 4-aminopyridine (4-AP, 1 mM)-evoked glutamate release was facilitated by the membrane permeant cyclic-3',5'-adenosine monophosphate (cAMP) analogue, 8-bromo-cAMP (8-Br-cAMP), used to directly activate cAMP-dependent protein kinase (PKA). 3.
The inhibitory effect of 5-HT could be mimicked by the selective 5-HT (1A) receptor agonist, 8-hydroxy-dipropylaminotetralin (8-OH-DPAT) and antagonized by 1-(2-methoxyphenyl)-4-(4-phthalimidobutyl) piperazine (NAN-190). 5.
1(0,0,0,1) Details
16682960 Kim HW, Kwon YB, Roh DH, Yoon SY, Han HJ, Kim KW, Beitz AJ, Lee JH: Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice. Br J Pharmacol. 2006 Jun;148(4):490-8. Epub 2006 May 8.


I.t. injection of BD-1047 also reduced formalin-evoked Fos expression and pNR1 at the protein kinase C-dependent site, serine-896 (Ser896) and the protein kinase A-dependent site, serine-897 (Ser897) in spinal dorsal horn.i.t.
1(0,0,0,1) Details
17392733 Lee JJ, Hahm ET, Lee CH, Cho YW: Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons. Neuropsychopharmacology. 2008 Jan;33(2):340-52. Epub 2007 Mar 28.

H-89, a selective protein kinase A (PKA) inhibitor, decreased the frequencies of GABAergic mIPSCs and glutamatergic mEPSCs, and blocked their reduction by 5-HT.
Serotonergic inhibition of mIPSC frequency was mimicked by (+/-)-8-hydroxy-2-dipropylaminotetralin hydrobromide, a specific 5-HT (1A) receptor agonist, and blocked by 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide, a specific 5-HT (1A) receptor antagonist. 6-Cyano-7-nitroquinoxaline-2,3-dione completely blocked spontaneous glutamatergic miniature excitatory postsynaptic currents (mEPSCs) in the MPOA.
1(0,0,0,1) Details