Protein Information

Name calcineurin inhibitors
Synonyms CABIN 1; CAIN; CABIN1; Calcineurin binding protein 1; Calcineurin binding protein cabin 1; Calcineurin inhibitor; Calcineurin binding protein 1s; Calcineurin binding protein cabin 1s…

Compound Information

Name deltamethrin
CAS

Reference List

PubMed Abstract RScore(About this table)
9037753 Robello M, Amico C, Cupello A: A dual mechanism for impairment of GABAA receptor activity by NMDA receptor activation in rat cerebellum granule cells. Eur Biophys J. 1997;25(3):181-7.

The NMDA effect was reduced by including adenosine-5'-O-3-thiophosphate (ATP-gamma-S) in the internal solution and there was a reduction in the NMDA effect caused by deltamethrin, a calcineurin inhibitor.
81(1,1,1,1) Details
18611438 Ranta F, Dufer M, Stork B, Wesselborg S, Drews G, Haring HU, Lang F, Ullrich S: Regulation of calcineurin activity in insulin-secreting cells: stimulation by Hsp90 during glucocorticoid-induced apoptosis. Cell Signal. 2008 Oct;20(10):1780-6. Epub 2008 Jun 18.

Previously, we described that apoptotic cell death induced by the synthetic glucocorticoid dexamethasone (dex) is inhibited by calcineurin inhibitors, FK506 and deltamethrin, in insulin-secreting cells.
31(0,1,1,1) Details
7531976 Richter A, Davies DE, Alexander P: Growth inhibitory effects of FK506 and cyclosporin A independent of inhibition of calcineurin. Biochem Pharmacol. 1995 Jan 31;49(3):367-73.

The role of calcineurin in CyA- or FK506-induced growth inhibition was investigated using the synthetic pyrethroid insecticides: cypermethrin, deltamethrin and fenvalerate, which are known calcineurin inhibitors.
31(0,1,1,1) Details
9379408 Traynelis SF, Wahl P: Control of rat GluR6 glutamate receptor open probability by protein kinase A and calcineurin. J Physiol. 1997 Sep 15;503 ( Pt 3):513-31.

The calcineurin-stimulated decrease of Po,peak in cells co-transfected with C alpha-PKA is blocked by 800 nM deltamethrin, a calcineurin inhibitor.
31(0,1,1,1) Details
8948591 Carrera A, Moos J, Ning XP, Gerton GL, Tesarik J, Kopf GS, Moss SB: Regulation of protein tyrosine phosphorylation in human sperm by a calcium/calmodulin-dependent mechanism: identification of A kinase anchor proteins as major substrates for tyrosine phosphorylation. Dev Biol. 1996 Nov 25;180(1):284-96.

In this regard, the calcineurin inhibitor deltamethrin inhibited the Ca2+ ionophore-induced dephosphorylation.
31(0,1,1,1) Details
16317049 MacDonald PE, Eliasson L, Rorsman P: Calcium increases endocytotic vesicle size and accelerates membrane fission in insulin-secreting INS-1 cells. J Cell Sci. 2005 Dec 15;118(Pt 24):5911-20. Epub 2005 Nov 29.

Similar results were obtained upon direct application of 100 nM and 0.5 mM Ca2+ to the intracellular surface of inside-out excised membrane patches, and in these experiments the increase in vesicle capacitance was prevented by the calcineurin inhibitor deltamethrin.
6(0,0,1,1) Details
16644695 Ranta F, Avram D, Berchtold S, Dufer M, Drews G, Lang F, Ullrich S: Dexamethasone induces cell death in insulin-secreting cells, an effect reversed by exendin-4. Diabetes. 2006 May;55(5):1380-90.

FK506 (0.1 micromol/l) and another calcineurin inhibitor, deltamethrin (1 micromol/l), attenuated dexamethasone-induced cell death.
6(0,0,1,1) Details
10794729 Bandyopadhyay A, Shin DW, Kim DH: Regulation of ATP-induced calcium release in COS-7 cells by calcineurin. . Biochem J. 2000 May 15;348 Pt 1:173-81.

Treatment of the cells with calcineurin inhibitors such as cyclosporin A (CsA), deltamethrin and FK506 resulted in an enhancement of ATP-induced intracellular Ca (2+) release.
6(0,0,1,1) Details
9572286 Matsuda T, Takuma K, Asano S, Kishida Y, Nakamura H, Mori K, Maeda S, Baba A: Involvement of calcineurin in Ca2+ paradox-like injury of cultured rat astrocytes. J Neurochem. 1998 May;70(5):2004-11.

Deltamethrin (20 nM), another calcineurin inhibitor, had a similar protective effect, whereas okadaic acid did not.
6(0,0,1,1) Details
16678970 Wu ZZ, Chen SR, Pan HL: Signaling mechanisms of down-regulation of voltage-activated Ca2+ channels by transient receptor potential vanilloid type 1 stimulation with olvanil in primary sensory neurons. Neuroscience. 2006 Aug 11;141(1):407-19. Epub 2006 May 6.

Furthermore, calcineurin (protein phosphatase 2B) inhibitors (deltamethrin and FK-506) eliminated the effect of olvanil on voltage-activated Ca (2+) channel current.
Notably, 1,2-bis (2-aminophenoxy) ethane-N,N,N',N'-tetraacetic acid, calmodulin antagonists, and calcineurin inhibitors each alone significantly increased the amplitude of voltage-activated Ca (2+) channel current.
1(0,0,0,1) Details
11062058 Bandyopadhyay A, Shin DW, Ahn JO, Kim DH: Calcineurin regulates ryanodine receptor/Ca (2+)-release channels in rat heart. Biochem J. 2000 Nov 15;352 Pt 1:61-70.

Effects of calcineurin inhibitors were tested on neonatal-rat-heart cardiomyocytes.
Treatment of neonatal cardiomyocytes with 20 microM deltamethrin, 10 microM cyclosporin A (CsA), or 10 mciroM FK506 led to Ca (2+) oscillations in originally quiescent cardiomyocytes.
1(0,0,0,1) Details
10575025 Liu Q, Berg DK: Actin filaments and the opposing actions of CaM kinase II and calcineurin in regulating alpha7-containing nicotinic receptors on chick ciliary ganglion neurons. J Neurosci. 1999 Dec 1;19(23):10280-8.

A membrane-permeable calcineurin inhibitor, however, still decreases the nicotinic response in a calcium-dependent manner, confirming that calcium-dependent phosphoregulation of alpha7-containing receptors occurs in the intact cell.
Blockade of calmodulin by calmidazolium or blockade of CaM kinase II with either KN93 or autocamtide-2-related inhibitory peptide each prevents the rundown; blockade of the phosphatase calcineurin with either cyclosporin A or deltamethrin increases the rundown.
1(0,0,0,1) Details
17551263 Martin C, Jacobi JS, Nava G, Jeziorski MC, Clapp C, Martinez de la Escalera G: GABA inhibition of cyclic AMP production in immortalized GnRH neurons is mediated by calcineurin-dependent dephosphorylation of adenylyl cyclase 9. Neuroendocrinology. 2007;85(4):257-66. Epub 2007 Jun 4.

Finally, GABA increased phosphatase activity in a calcium-dependent manner, an effect blocked by calcineurin inhibitors.
Furthermore, blocking calcineurin with deltamethrin, FK-506 or cyclosporin A blocked the inhibitory effect of GABA on [cAMP] i, supporting the involvement of AC9 in this effect.
1(0,0,0,1) Details
15337272 Choi JS, Soderlund DM: Cyclosporin A and deltamethrin block the downregulation of Nav1.8 sodium channels expressed in Xenopus oocytes. Neurosci Lett. 2004 Sep 9;367(3):389-93.

The use of a calcineurin inhibitor such as cyclosporin A provides an effective means of stabilizing the expression of Nav1.8 sodium channels in oocytes for functional and pharmacological studies.
1(0,0,0,1) Details
10844399 Kampermann J, Herbst M, Ullrich S: Effects of adrenaline and tolbutamide on insulin secretion in INS-1 cells under voltage control. Cell Physiol Biochem. 2000;10(1-2):81-90.


After incubation of the cells with deltamethrin, a calcineurin inhibitor, the stimulation of secretion was attenuated, but the adrenaline-induced inhibition was not affected.
0(0,0,0,0) Details
11562451 Dufer M, Krippeit-Drews P, Lembert N, Idahl LA, Drews G: Diabetogenic effect of cyclosporin A is mediated by interference with mitochondrial function of pancreatic B-cells. Mol Pharmacol. 2001 Oct;60(4):873-9.


This effect is not due to an inhibition of calcineurin, which mediates the immunosuppressive effect of CsA, because other calcineurin inhibitors, deltamethrin and tacrolimus, did not affect the oscillations in [Ca (2+)](c) of the B-cells.
0(0,0,0,0) Details
10807662 Wirkner K, Assmann H, Koles L, Gerevich Z, Franke H, Norenberg W, Boehm R, Illes P: Inhibition by adenosine A (2A) receptors of NMDA but not AMPA currents in rat neostriatal neurons. Br J Pharmacol. 2000 May;130(2):259-69.


The calcineurin inhibitor deltamethrin did not interfere with CGS 21680.
0(0,0,0,0) Details
8985861 Hardwick JC, Parsons RL: Activation of the protein phosphatase calcineurin during carbachol exposure decreases the extent of recovery from end-plate desensitization. J Neurophysiol. 1996 Dec;76(6):3609-16.


This staurosporine-induced decrease in ACh sensitivity could be prevented by pretreatment with the protein phosphatase 2B (calcineurin) inhibitor deltamethrin (0.5 microM), whereas okadaic acid (5 microM) and calyculin A (0.5 microM), inhibitors of protein phosphatases 1 and 2A, had no effect. 3.
0(0,0,0,0) Details