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Identification
NameAV411
Accession NumberDB05066
TypeSmall Molecule
GroupsInvestigational
Description

AV411 is an orally bioavailable, centrally acting molecule that Avigen has identified as having potential utility for the treatment of neuropathic pain and other neurological indications, including opiate withdrawal. The active pharmaceutical ingredient in AV411 is ibudilast.

Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Taxonomy
ClassificationNot classified
Pharmacology
IndicationInvestigated for use/treatment in neuropathy (diabetic) and pain (acute or chronic).
PharmacodynamicsRelease of factors such as substance P, chemokines such as fractalkine, and cytokines including IL-1 and TNF╬▒ play a role in amplifying afferent sensory input and causing or exacerbating painful sensations. AV411 has been found to suppress the production of pro-inflammatory cytokines (IL-1beta, TNF-alpha , IL-6), and may enhance the production of the anti-inflammatory cytokine IL-10, and upregulate release of neurotrophic factors (NGF, GDNF, NT-4).
Mechanism of actionAV411 suppresses the production of pro-inflammatory cytokines (IL-1beta, TNF-alpha , IL-6), and may enhance the production of the anti-inflammatory cytokine IL-10, and upregulate release of neurotrophic factors (NGF, GDNF, NT-4).
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein domain specific binding
Specific Function:
Potent proinflammatory cytokine. Initially discovered as the major endogenous pyrogen, induces prostaglandin synthesis, neutrophil influx and activation, T-cell activation and cytokine production, B-cell activation and antibody production, and fibroblast proliferation and collagen production. Promotes Th17 differentiation of T-cells.
Gene Name:
IL1B
Uniprot ID:
P01584
Molecular Weight:
30747.7 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Tumor necrosis factor receptor binding
Specific Function:
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs ...
Gene Name:
TNF
Uniprot ID:
P01375
Molecular Weight:
25644.15 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Interleukin-6 receptor binding
Specific Function:
Cytokine with a wide variety of biological functions. It is a potent inducer of the acute phase response. Plays an essential role in the final differentiation of B-cells into Ig-secreting cells Involved in lymphocyte and monocyte differentiation. Acts on B-cells, T-cells, hepatocytes, hematopoietic progenitor cells and cells of the CNS. Required for the generation of T(H)17 cells. Also acts as ...
Gene Name:
IL6
Uniprot ID:
P05231
Molecular Weight:
23717.965 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Interleukin-10 receptor binding
Specific Function:
Inhibits the synthesis of a number of cytokines, including IFN-gamma, IL-2, IL-3, TNF and GM-CSF produced by activated macrophages and by helper T-cells.
Gene Name:
IL10
Uniprot ID:
P22301
Molecular Weight:
20516.585 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor binding
Specific Function:
Seems to promote the survival of visceral and proprioceptive sensory neurons.
Gene Name:
NTF3
Uniprot ID:
P20783
Molecular Weight:
29354.29 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor binding
Specific Function:
Neurotrophic factor that enhances survival and morphological differentiation of dopaminergic neurons and increases their high-affinity dopamine uptake.
Gene Name:
GDNF
Uniprot ID:
P39905
Molecular Weight:
23719.85 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Growth factor activity
Specific Function:
Target-derived survival factor for peripheral sensory sympathetic neurons.
Gene Name:
NTF4
Uniprot ID:
P34130
Molecular Weight:
22426.435 Da
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Drug created on October 21, 2007 16:23 / Updated on September 13, 2013 11:58