BAY-60-7550 is a potent Type 2 cyclic nucleotide phosphodiesterases (PDE2) inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). BAY-60-7550 is an analog of EHNA, which is more than 100-fold more potent and is highly selective for PDE2A.
|Cell lines||human distal pulmonary artery smooth muscle cells|
|Preparation method||Cell proliferation.
Growth of human distal pulmonary artery smooth muscle cells isolated from patients with idiopathic pulmonary arterial hypertension (IPAH) or control cells from adults undergoing transplant or lung resection for suspected malignancy, were monitored as we have described previously 29 following treatment with BAY 60-7550 (1μmol/L), ANP (1μmol/L), DETA-NONOate (10μmol/L), or treprostinil (1μmol/L), alone or in combination.
|Animal models||Oxidative Stress on Behavior in mice|
|Formulation||dissolved in 50% dimethyl sulfoxide (Fisher Scientific Co., Pittsburgh, PA)|
|Dosages||3 mg/kg; given 30 min before each BSO treatment|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Inhibition of phosphodiesterase 2 augments cGMP and cAMP signaling to ameliorate pulmonary hypertension.
Bubb KJ, et al. Circulation. 2014 Aug 5;130(6):496-507. PMID: 24899690.
Phosphodiesterase-2 inhibitor reverses corticosterone-induced neurotoxicity and related behavioural changes via cGMP/PKG dependent pathway.
Xu et al. Int J Neuropsychopharmacol. 2012 Jul 31;1-13. PMID: 22850435.
Mechanisms of carbon monoxide attenuation of tubuloglomerular feedback.
Ren et al. Hypertension. 2012 Jun;59(6):1139-44. PMID: 22508834.
Selective phosphodiesterase inhibitors improve performance on the ED/ID cognitive task in rats
Rodefer et al. Neuropharmacology. 2012 Mar;62(3):1182-90. PMID: 21856317.
PDE5A suppression of acute beta-adrenergic activation requires modulation of myocyte beta-3 signaling coupled to PKG-mediated troponin I phosphorylation.
Lee et al. Basic Res Cardiol. 2010 May;105(3):337-47. PMID: 20107996.
Reversal of oxidative stress-induced anxiety by inhibition of phosphodiesterase-2 in mice.
Masood A, et al. J Pharmacol Exp Ther. 2008 Aug;326(2):369-79. PMID: 18456873.
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