Phosphodiesterases (PDEs) are enzymes that regulate the function of immune cells by hydrolyzing cyclic guanosine monophosphate/cGMP and cyclic adenosine monophosphate/cAMP. PDEs are divided into subfamilies (PDE3, PDE4, PDE5 and PDE7) which are mainly found in the respiratory tract[3]. IBMX is a broad-spectrum PDE inhibitor and its IC50 values for PDE3, 4 and 5 were 6.5 ± 1.2, 26.3 ± 3.9 and 31.7 ± 5.3 μM, respectively[4]. Human proximal tubular epithelial HK-2 cells were treated with different concentrations of IBMX for 24 h to elucidate the effect of IBMX on HIF-1 mRNA expression, IBMX reduced the mRNA levels in a dose dependant manner starting from 400 M concentration. HK-2 cells treated with or without IBMX were exposed to hypoxia for different durations, and cell viability was maintained in IBMX treated group at 24 h and 48 h, and the protective effect became significant at 48 h[5].
IBMX/3-异丁基-1-甲基黄嘌呤 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rat ventricular myocardium
30 µM
15 minutes
To study the effects of IBMX on the positive inotropic response to glucagon in rat ventricular myocardium. Results showed that IBMX enhanced the inotropic effect of glucagon and altered its EC50 value.
Cardiovasc Diabetol. 2023 May 30;22(1):128.
Nonfailing and failing human myocardial tissue
30 µM
15 minutes
To investigate the positive inotropic effects of IBMX on nonfailing and failing human myocardial tissues. Results showed that IBMX induced a marked inotropic response in atrial tissues from nonfailing hearts but no response in failing hearts. Ventricular tissues showed stronger responses in nonfailing hearts.
Cardiovasc Diabetol. 2023 May 30;22(1):128.
Mouse embryonic fibroblasts (MEFs)
500 µM
2 days
Induction of pre-adipocyte differentiation into adipocytes
Br J Pharmacol. 2012 Oct;167(3):561-75.
3T3-L1 pre-adipocytes
500 µM
2 days
Induction of pre-adipocyte differentiation into adipocytes
Br J Pharmacol. 2012 Oct;167(3):561-75.
Aged mouse right atrial tissue
100 µM
20 minutes
IBMXmax increased cAMP levels in both adult and aged atrial tissue by the same degree.
Geroscience. 2023 Feb;45(1):209-219.
Adult mouse right atrial tissue
5 µM
20 minutes
IBMX50 increased cAMP levels in both adult and aged atria, but to a greater magnitude in the former.
Geroscience. 2023 Feb;45(1):209-219.
Hepatocytes
0.5 mM
20 minutes
To investigate the effect of IBMX on mitochondrial respiratory chain complex I and CPS-I activity. Results showed that IBMX inhibited mitochondrial respiratory chain complex I and CPS-I activity.
J Biol Chem. 2008 May 30;283(22):15063-71.
Porcine oocytes
1.0 mM
24 hours
Inhibition of GVBD and increase in MIR21 abundance
Reprod Biol Endocrinol. 2020 May 11;18(1):39.
Mouse pancreatic acini
0.03-1.0 mM
30 min
IBMX potentiated amylase release stimulated by CCK, carbamylcholine, and the ionophore A23187 by mimicking the action of cyclic AMP.
J Physiol. 1984 Apr;349:475-82.
B16/F10 melanoma cells
100 mM
48 hours
To evaluate the melanogenic effect induced by IBMX, results showed IBMX treatment significantly increased melanin content
Nutrients. 2020 Mar 20;12(3):832.
Mesenchymal stem cells (MSCs)
100 µM
5 days
Induced neural-like differentiation of MSCs, including expression of neural markers and increased sensitivity to neurotransmitters
Sci Rep. 2019 Feb 27;9(1):2969.
Mouse PCLS
1 mM
50 minutes
Used as a positive control for maximal relaxation, compared with amitriptyline
Respir Res. 2023 Oct 31;24(1):262.
Rat PCLS
1 mM
50 minutes
Used as a positive control for maximal relaxation, compared with amitriptyline
Respir Res. 2023 Oct 31;24(1):262.
Colon fragments
100 µM
60 minutes
IBMX stimulation resulted in a 100% increase in GLP-1 release
Nat Commun. 2021 Jan 4;12(1):110.
Antral fragments
100 µM
60 minutes
IBMX stimulation resulted in an 80% increase in GLP-1 release
Nat Commun. 2021 Jan 4;12(1):110.
Fundus fragments
100 µM
60 minutes
IBMX stimulation resulted in a 70% increase in GLP-1 release
Nat Commun. 2021 Jan 4;12(1):110.
Gallbladder smooth muscle cells
100 µM
To investigate the effect of IBMX on cAMP levels in gallbladder smooth muscle cells and its role in gallbladder relaxation. Results showed that IBMX increased cAMP levels by inhibiting phosphodiesterase, leading to gallbladder smooth muscle relaxation.
Br J Pharmacol. 2004 Dec;143(8):994-1005.
Rat gastric mucosa parietal cells
1 µM-100 µM
IBMX caused concentration-dependent increases in acid output, unaffected by ranitidine, indicating direct action on parietal cells without histamine release.
Br J Pharmacol. 1996 Nov;119(5):905-10.
Mouse oviduct smooth muscle cells
10 µM
IBMX mimicked the effects of caffeine, causing membrane hyperpolarization and inhibition of slow wave activity, which were reversed by the KATP channel antagonist glibenclamide.
Br J Pharmacol. 2011 Jun;163(4):745-54.
Fischer rat thyroid (FRT) epithelial cells
100 µM
Activation of CFTR channel by increasing intracellular cAMP levels, used to study CFTR function
Int J Mol Sci. 2025 Jan 8;26(2):471.
Human nasal epithelial cells (HNEC)
100 µM
Activation of CFTR channel by increasing intracellular cAMP levels, used to study CFTR function
Int J Mol Sci. 2025 Jan 8;26(2):471.
IBMX/3-异丁基-1-甲基黄嘌呤 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Liver perfusion system
Perfusion
0.5 mM
45 minutes
To investigate the effect of IBMX on hepatic urea synthesis. Results showed that IBMX inhibited urea synthesis, and AGM reversed this inhibition.
J Biol Chem. 2008 May 30;283(22):15063-71.
Guinea-pigs
Gallbladder muscle strips
Organ bath
100 μM
Single administration
To study the relaxing effect of IBMX on gallbladder muscle strips. Results showed that IBMX caused gallbladder smooth muscle relaxation by increasing cAMP levels, with a relaxation amplitude of 6.4±1.1 mN.
Br J Pharmacol. 2004 Dec;143(8):994-1005.
Rat
Rat right atria
In vitro administration
30 µM
Single dose, 15 minutes
To investigate the effects of IBMX on the spontaneous beating rate of rat right atria. Results showed that IBMX increased the atrial rate but did not alter the chronotropic effect of glucagon.
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