Piclamilast

Piclamilast Structure
Piclamilast structure
Common Name Piclamilast
CAS Number 144035-83-6 Molecular Weight 381.253
Density 1.4±0.1 g/cm3 Boiling Point 447.8±45.0 °C at 760 mmHg
Molecular Formula C18H18Cl2N2O3 Melting Point N/A
MSDS Chinese USA Flash Point 224.6±28.7 °C
Symbol GHS07
GHS07
Signal Word Warning

Phosphodiesterase IV inhibition by piclamilast potentiates the cytodifferentiating action of retinoids in myeloid leukemia cells. Cross-talk between the cAMP and the retinoic acid signaling pathways.

J. Biol. Chem. 279(40) , 42026-40, (2004)

Inhibition of phosphodiesterase IV by N-(3,5-dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide (piclamilast) enhances the myeloid differentiation induced by all-trans-retinoic acid (ATRA), retinoic acid receptor alpha (RARalpha), or retinoic acid recept...

Potential role of phosphodiesterase 7 in human T cell function: comparative effects of two phosphodiesterase inhibitors.

Clin. Exp. Immunol. 128(3) , 460-6, (2002)

Even though the existence of phosphodiesterase (PDE) 7 in T cells has been proved, the lack of a selective PDE7 inhibitor has confounded an accurate assessment of PDE7 function in such cells. In order to elucidate the role of PDE7 in human T cell function, th...

The differential impact of PDE4 subtypes in human lung fibroblasts on cytokine-induced proliferation and myofibroblast conversion.

J. Cell Physiol. 226(8) , 1970-80, (2011)

Lung fibroblast proliferation and differentiation into myofibroblasts are pathological key events during development of lung fibrosis. Cyclic nucleotide signaling is described as a negative modulator of these cellular processes, and cyclic nucleotide degradin...

Correlation between emetic effect of phosphodiesterase 4 inhibitors and their occupation of the high-affinity rolipram binding site in Suncus murinus brain.

Eur. J. Pharmacol. 573(1-3) , 93-9, (2007)

We employed an ex vivo [(3)H]rolipram binding experiment to elucidate the mechanism of emetic activity of phosphodiesterase 4 inhibitors. In Suncus murinus (an insectivore used for evaluation of emesis), emetic potential as well as ability to occupy the high-...

Selective inhibition of purified human phosphodiesterase 4A expressed in yeast cell GL62 by ciclamilast, piclamilast, and rolipram.

Acta Pharmacol. Sin. 25(9) , 1171-5, (2004)

To improve the specific activity of human phosphodiesterase 4A (PDE4A) expressed in yeast cell GL62 and investigate the effects of selective phosphodiesterase 4 (PDE4) inhibitors (ciclamilast, piclamilast, and rolipram), selective phosphodiesterase 5 (PDE5) i...

Evaluating the significance of cyclic adenosine monophosphate-mediated signaling in human prostate: a functional and biochemical study.

Urology 80(4) , 952.e9-14, (2012)

To investigate further the potential significance of the cyclic adenosine monophosphate (cAMP) pathway in the control of prostate smooth muscle. The cAMP pathway has been assumed to be an alternative pharmacologic target to treat dysfunctions of the human low...

Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H(2)O(2) via mechanisms involving AP-1 activation.

Free Radic. Res. 46(5) , 690-9, (2012)

Reactive oxygen species (ROS) are involved in the pathogenesis of many inflammatory diseases such as chronic obstructive pulmonary disease (COPD). They can alter the expression of genes involved in cellular damage by activating transcription factors, includin...

Effects of piclamilast, a selective phosphodiesterase-4 inhibitor, on oxidative burst of sputum cells from mild asthmatics and stable COPD patients.

Lung 182(6) , 369-77, (2004)

Oxidative stress associated with increased presence of neutrophils is an important feature of inflammatory airways diseases like asthma or chronic obstructive pulmonary disease. We studied the in vitro effect of piclamilast (RP73401), a selective phosphodiest...

Phosphodiesterase 4 inhibition attenuates persistent heart and lung injury by neonatal hyperoxia in rats.

Am. J. Physiol. Lung Cell. Mol. Physiol. 302(1) , L56-67, (2012)

Phosphodiesterase (PDE) 4 inhibitors are potent anti-inflammatory drugs with antihypertensive properties, and their therapeutic role in bronchopulmonary dysplasia (BPD) is still controversial. We studied the role of PDE4 inhibition with piclamilast on normal ...

Phosphodiesterase-4 inhibition attenuates pulmonary inflammation in neonatal lung injury.

Eur. Respir. J. 31(3) , 633-44, (2008)

Phosphodiesterase-4 (PDE4) inhibitors may offer novel therapeutic strategies in respiratory diseases, including asthma and chronic obstructive pulmonary disease. Therefore, selective PDE4 inhibitors may also provide a therapeutic option for very pre-term infa...