Identification

Name
Ibudilast
Accession Number
DB05266  (DB05066)
Type
Small Molecule
Groups
Approved, Investigational
Description

Ibudilast is an anti-inflammatory and neuroprotective oral agent which shows an excellent safety profile at 60 mg/day and provides significantly prolonged time-to-first relapse and attenuated brain volume shrinkage in patients with relapsing-remitting (RR) and/or secondary progressive (SP) multiple sclerosis (MS). Ibudilast is currently in development in the U.S. (codes: AV-411 or MN-166), but is approved for use as an antiinflammatory in Japan.

Structure
Thumb
Synonyms
  • Ibudilastum
External IDs
AV-411 / AV411 / BRN 0656579 / MN-166
International/Other Brands
Ke Tas / Ketas
Categories
UNII
M0TTH61XC5
CAS number
50847-11-5
Weight
Average: 230.3055
Monoisotopic: 230.141913208
Chemical Formula
C14H18N2O
InChI Key
ZJVFLBOZORBYFE-UHFFFAOYSA-N
InChI
InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3
IUPAC Name
2-methyl-1-[2-(propan-2-yl)pyrazolo[1,5-a]pyridin-3-yl]propan-1-one
SMILES
CC(C)C(=O)C1=C2C=CC=CN2N=C1C(C)C

Pharmacology

Indication

For the treatment of multiple sclerosis, asthma, and cerebrovascular disease.

Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action

Ibudilast has mechanisms that include anti-inflammatory effects, such as phosphodiesterase inhibition, and neuroprotective effects, such as inhibition of [nitric oxide] synthesis and reduction in reactive oxygen species.

TargetActionsOrganism
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A
inhibitor
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4B
inhibitor
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4C
inhibitor
Human
UcAMP-specific 3',5'-cyclic phosphodiesterase 4D
inhibitor
Human
UcGMP-inhibited 3',5'-cyclic phosphodiesterase A
inhibitor
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

19 hours

Clearance
Not Available
Toxicity

Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabIbudilast may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolIbudilast may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Ibudilast is combined with Acetylsalicylic acid.Approved, Vet Approved
AloxiprinThe risk or severity of adverse effects can be increased when Ibudilast is combined with Aloxiprin.Experimental
AlprostadilAlprostadil may increase the antiplatelet activities of Ibudilast.Approved, Investigational
AlteplaseIbudilast may increase the anticoagulant activities of Alteplase.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Ibudilast is combined with Aminosalicylic Acid.Approved
AnagrelideIbudilast may increase the anticoagulant activities of Anagrelide.Approved
AncrodIbudilast may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideIbudilast may increase the antiplatelet activities of Andrographolide.Investigational
AnistreplaseIbudilast may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanIbudilast may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Ibudilast is combined with Apixaban.Approved
ArdeparinIbudilast may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanIbudilast may increase the anticoagulant activities of Argatroban.Approved, Investigational
AstaxanthinIbudilast may increase the anticoagulant activities of Astaxanthin.Investigational
AzelastineAzelastine may increase the antiplatelet activities of Ibudilast.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Ibudilast is combined with Balsalazide.Approved, Investigational
BatroxobinIbudilast may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminIbudilast may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinIbudilast may increase the anticoagulant activities of Bemiparin.Approved, Investigational
BeraprostIbudilast may increase the anticoagulant activities of Beraprost.Investigational
BivalirudinIbudilast may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BrinaseIbudilast may increase the anticoagulant activities of Brinase.Experimental
BuflomedilIbudilast may increase the antiplatelet activities of Buflomedil.Experimental
ButylphthalideIbudilast may increase the antiplatelet activities of Butylphthalide.Investigational
CangrelorIbudilast may increase the anticoagulant activities of Cangrelor.Approved
CaplacizumabIbudilast may increase the anticoagulant activities of Caplacizumab.Investigational
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Ibudilast is combined with Carbaspirin calcium.Experimental, Investigational
CertoparinIbudilast may increase the anticoagulant activities of Certoparin.Approved, Investigational
CilostazolIbudilast may increase the anticoagulant activities of Cilostazol.Approved
Citric AcidIbudilast may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClopidogrelIbudilast may increase the anticoagulant activities of Clopidogrel.Approved
CloricromenIbudilast may increase the anticoagulant activities of Cloricromen.Experimental
ClorindioneIbudilast may increase the anticoagulant activities of Clorindione.Experimental
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Ibudilast is combined with Collagenase clostridium histolyticum.Approved, Investigational
Dabigatran etexilateIbudilast may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinIbudilast may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidIbudilast may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanIbudilast may increase the anticoagulant activities of Darexaban.Investigational
DasatinibDasatinib may increase the anticoagulant activities of Ibudilast.Approved, Investigational
DefibrotideIbudilast may increase the anticoagulant activities of Defibrotide.Approved, Investigational
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Ibudilast is combined with Deoxycholic Acid.Approved
DersalazineThe risk or severity of adverse effects can be increased when Ibudilast is combined with Dersalazine.Investigational
DesirudinIbudilast may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseIbudilast may increase the anticoagulant activities of Desmoteplase.Investigational
DextranIbudilast may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Ibudilast may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Ibudilast may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Ibudilast may increase the anticoagulant activities of Dextran 75.Approved
DicoumarolIbudilast may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Ibudilast is combined with Diflunisal.Approved
DiphenadioneIbudilast may increase the anticoagulant activities of Diphenadione.Experimental
DipyridamoleIbudilast may increase the anticoagulant activities of Dipyridamole.Approved
DitazoleIbudilast may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
Drotrecogin alfaIbudilast may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
Edetic AcidIbudilast may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanIbudilast may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinIbudilast may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the antiplatelet activities of Ibudilast.Approved, Investigational
EplivanserinIbudilast may increase the anticoagulant activities of Eplivanserin.Investigational
eplivanserineIbudilast may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Ibudilast.Approved
EptifibatideIbudilast may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
Ethyl biscoumacetateIbudilast may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ferulic acidIbudilast may increase the anticoagulant activities of Ferulic acid.Experimental
FibrinolysinIbudilast may increase the anticoagulant activities of Fibrinolysin.Investigational
FluindioneIbudilast may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxIbudilast may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumIbudilast may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateIbudilast may increase the anticoagulant activities of Gabexate.Investigational
GlucosamineGlucosamine may increase the antiplatelet activities of Ibudilast.Approved
GuacetisalThe risk or severity of adverse effects can be increased when Ibudilast is combined with Guacetisal.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Ibudilast is combined with Hemoglobin crosfumaril.Experimental
HeparinIbudilast may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineIbudilast may increase the anticoagulant activities of Higenamine.Investigational
HydroxytyrosolIbudilast may increase the antiplatelet activities of Hydroxytyrosol.Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ibudilast is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Ibudilast.Approved
Icosapent ethylIbudilast may increase the antiplatelet activities of Icosapent ethyl.Approved, Nutraceutical
IdraparinuxIbudilast may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIbudilast may increase the antiplatelet activities of Ifenprodil.Approved, Investigational, Withdrawn
IfetrobanIbudilast may increase the antiplatelet activities of Ifetroban.Investigational
IloprostIloprost may increase the antiplatelet activities of Ibudilast.Approved, Investigational
IndobufenIbudilast may increase the anticoagulant activities of Indobufen.Investigational
KetanserinIbudilast may increase the antiplatelet activities of Ketanserin.Investigational
LepirudinIbudilast may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanIbudilast may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostLimaprost may increase the antiplatelet activities of Ibudilast.Approved, Investigational
LinsidomineIbudilast may increase the antiplatelet activities of Linsidomine.Experimental
MelagatranIbudilast may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Ibudilast is combined with Mesalazine.Approved
Methyl salicylateThe risk or severity of adverse effects can be increased when Ibudilast is combined with Methyl salicylate.Approved, Vet Approved
MilrinoneMilrinone may increase the antiplatelet activities of Ibudilast.Approved
NadroparinIbudilast may increase the anticoagulant activities of Nadroparin.Approved
NafamostatIbudilast may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilIbudilast may increase the antiplatelet activities of Naftopidil.Investigational
NimesulideNimesulide may increase the antiplatelet activities of Ibudilast.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Ibudilast is combined with Nitroaspirin.Investigational
ObinutuzumabThe risk or severity of adverse effects can be increased when Ibudilast is combined with Obinutuzumab.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Ibudilast is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Ibudilast.Approved, Nutraceutical
OtamixabanIbudilast may increase the anticoagulant activities of Otamixaban.Investigational
OzagrelIbudilast may increase the anticoagulant activities of Ozagrel.Investigational
ParnaparinIbudilast may increase the anticoagulant activities of Parnaparin.Approved, Investigational
Pentaerythritol TetranitrateIbudilast may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Ibudilast.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Ibudilast.Approved, Investigational
PhenindioneIbudilast may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonIbudilast may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PicotamideIbudilast may increase the anticoagulant activities of Picotamide.Experimental
PrasugrelIbudilast may increase the anticoagulant activities of Prasugrel.Approved
Protein CIbudilast may increase the anticoagulant activities of Protein C.Approved
Protein S humanIbudilast may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeIbudilast may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanIbudilast may increase the antiplatelet activities of Ramatroban.Investigational
RelcovaptanIbudilast may increase the antiplatelet activities of Relcovaptan.Investigational
ResveratrolResveratrol may increase the antiplatelet activities of Ibudilast.Approved, Experimental, Investigational
ReteplaseIbudilast may increase the anticoagulant activities of Reteplase.Approved
ReviparinIbudilast may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelRidogrel may increase the antiplatelet activities of Ibudilast.Approved
RiociguatIbudilast may increase the hypotensive activities of Riociguat.Approved
RivaroxabanIbudilast may increase the anticoagulant activities of Rivaroxaban.Approved
RosiglitazoneIbudilast may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Ibudilast is combined with Salicylic acid.Approved, Vet Approved
SarpogrelateIbudilast may increase the anticoagulant activities of Sarpogrelate.Investigational
SaruplaseIbudilast may increase the anticoagulant activities of Saruplase.Experimental
SelexipagIbudilast may increase the anticoagulant activities of Selexipag.Approved
SevofluraneSevoflurane may increase the antiplatelet activities of Ibudilast.Approved, Vet Approved
SRT501SRT501 may increase the antiplatelet activities of Ibudilast.Investigational
StreptokinaseIbudilast may increase the anticoagulant activities of Streptokinase.Approved, Investigational
SulodexideIbudilast may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TenecteplaseIbudilast may increase the anticoagulant activities of Tenecteplase.Approved
TesmilifeneTesmilifene may increase the antiplatelet activities of Ibudilast.Investigational
TicagrelorIbudilast may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineIbudilast may increase the anticoagulant activities of Ticlopidine.Approved
TinzaparinIbudilast may increase the anticoagulant activities of Tinzaparin.Approved
TioclomarolIbudilast may increase the anticoagulant activities of Tioclomarol.Experimental
TipranavirTipranavir may increase the antiplatelet activities of Ibudilast.Approved, Investigational
TirofibanIbudilast may increase the anticoagulant activities of Tirofiban.Approved
TositumomabThe risk or severity of adverse effects can be increased when Ibudilast is combined with Tositumomab.Approved, Investigational
TranilastIbudilast may increase the antiplatelet activities of Tranilast.Approved, Investigational
TrapidilIbudilast may increase the antiplatelet activities of Trapidil.Approved
TreprostinilTreprostinil may increase the antiplatelet activities of Ibudilast.Approved, Investigational
TriflusalIbudilast may increase the anticoagulant activities of Triflusal.Approved, Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Ibudilast is combined with Trolamine salicylate.Approved
TroxerutinIbudilast may increase the anticoagulant activities of Troxerutin.Investigational
UrokinaseIbudilast may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
Vitamin EVitamin E may increase the antiplatelet activities of Ibudilast.Approved, Nutraceutical, Vet Approved
VorapaxarIbudilast may increase the anticoagulant activities of Vorapaxar.Approved
WarfarinIbudilast may increase the anticoagulant activities of Warfarin.Approved
XimelagatranIbudilast may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB15614
PubChem Compound
3671
PubChem Substance
99443231
ChemSpider
3543
BindingDB
50240404
ChEBI
31684
ChEMBL
CHEMBL19449
PharmGKB
PA165958351
HET
AVL
Wikipedia
Ibudilast
ATC Codes
R03DC04 — Ibudilast
PDB Entries
4grq

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableMethamphetamine-dependence / Substance Abuse1
1CompletedBasic ScienceMigrainous Headache1
1CompletedTreatmentAlcohol Use Disorders (AUD)1
1, 2CompletedTreatmentDiabetic Neuropathies1
1, 2RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS)1
1, 2Unknown StatusTreatmentMedication Overuse Headache1
2Active Not RecruitingNot AvailableOpioid Abuse / Opioid Dependence1
2Active Not RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS)1
2Active Not RecruitingTreatmentMultiple Sclerosis, Primary Progressive / Secondary Progressive Multiple Sclerosis (SPMS)1
2CompletedBasic ScienceOpioid-Related Disorders1
2Not Yet RecruitingTreatmentMethamphetamine Dependence in Remission1
2RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections / Methamphetamine Dependence1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.179 mg/mLALOGPS
logP3.36ALOGPS
logP3.68ChemAxon
logS-3.1ALOGPS
pKa (Strongest Acidic)16.12ChemAxon
pKa (Strongest Basic)1.86ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area34.37 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity79.38 m3·mol-1ChemAxon
Polarizability26.31 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9868
Caco-2 permeable+0.6112
P-glycoprotein substrateNon-substrate0.788
P-glycoprotein inhibitor IInhibitor0.5207
P-glycoprotein inhibitor IINon-inhibitor0.7071
Renal organic cation transporterNon-inhibitor0.8179
CYP450 2C9 substrateNon-substrate0.8076
CYP450 2D6 substrateNon-substrate0.793
CYP450 3A4 substrateSubstrate0.5476
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.6259
CYP450 2C19 inhibitorInhibitor0.8071
CYP450 3A4 inhibitorNon-inhibitor0.6338
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7965
Ames testNon AMES toxic0.7408
CarcinogenicityNon-carcinogens0.8482
BiodegradationNot ready biodegradable0.9838
Rat acute toxicity2.2040 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9554
hERG inhibition (predictor II)Non-inhibitor0.9088
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000w-3910000000-7c4d5c86420e4e74cdb1

Taxonomy

Description
This compound belongs to the class of organic compounds known as pyrazolopyridines. These are compounds containing a pyrazolopyridine skeleton, which consists of a pyrazole fused to a pyridine. Pyrazole is 5-membered ring consisting of three carbon atoms and two adjacent nitrogen centers. Pyridine is a 6-membered ring with four carbon and one nitrogen atoms.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyrazolopyridines
Sub Class
Not Available
Direct Parent
Pyrazolopyridines
Alternative Parents
Aryl alkyl ketones / Pyridines and derivatives / Vinylogous amides / Pyrazoles / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives
Substituents
Pyrazolopyridine / Aryl alkyl ketone / Aryl ketone / Pyridine / Azole / Pyrazole / Heteroaromatic compound / Vinylogous amide / Ketone / Azacycle
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name
PDE4A
Uniprot ID
P27815
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Molecular Weight
98142.155 Da
References
  1. Yagi K, Tada Y, Kitazato KT, Tamura T, Satomi J, Nagahiro S: Ibudilast inhibits cerebral aneurysms by down-regulating inflammation-related molecules in the vascular wall of rats. Neurosurgery. 2010 Mar;66(3):551-9; discussion 559. doi: 10.1227/01.NEU.0000365771.89576.77. [PubMed:20124930]
  2. Yamazaki T, Anraku T, Matsuzawa S: Ibudilast, a mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery. Eur J Pharmacol. 2011 Jan 15;650(2-3):605-11. doi: 10.1016/j.ejphar.2010.10.033. Epub 2010 Oct 29. [PubMed:21036126]
  3. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging f...
Gene Name
PDE4B
Uniprot ID
Q07343
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Molecular Weight
83342.695 Da
References
  1. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name
PDE4C
Uniprot ID
Q08493
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4C
Molecular Weight
79900.795 Da
References
  1. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Ubiquitin protein ligase binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name
PDE4D
Uniprot ID
Q08499
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
Molecular Weight
91114.1 Da
References
  1. Huang Z, Liu S, Zhang L, Salem M, Greig GM, Chan CC, Natsumeda Y, Noguchi K: Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sci. 2006 May 1;78(23):2663-8. Epub 2005 Nov 28. [PubMed:16313925]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
Gene Name
PDE3A
Uniprot ID
Q14432
Uniprot Name
cGMP-inhibited 3',5'-cyclic phosphodiesterase A
Molecular Weight
124978.06 Da
References
  1. Yamazaki T, Anraku T, Matsuzawa S: Ibudilast, a mixed PDE3/4 inhibitor, causes a selective and nitric oxide/cGMP-independent relaxation of the intracranial vertebrobasilar artery. Eur J Pharmacol. 2011 Jan 15;650(2-3):605-11. doi: 10.1016/j.ejphar.2010.10.033. Epub 2010 Oct 29. [PubMed:21036126]

Drug created on November 18, 2007 11:22 / Updated on November 09, 2017 03:51