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Details

Stereochemistry ACHIRAL
Molecular Formula C13H20N4O2
Molecular Weight 264.3235
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PENTIFYLLINE

SMILES

CCCCCCN1C(=O)N(C)C2=C(N(C)C=N2)C1=O

InChI

InChIKey=MRWQRJMESRRJJB-UHFFFAOYSA-N
InChI=1S/C13H20N4O2/c1-4-5-6-7-8-17-12(18)10-11(14-9-15(10)2)16(3)13(17)19/h9H,4-8H2,1-3H3

HIDE SMILES / InChI

Description

Pentifylline is an active vasodilating substance which does not affect blood sugar levels. Pentifylline inhibits the soluble and the particulate cyclic AMP phosphodiesterases from bovine platelets and rat brain ATPase. The inhibition of ATPase by pentifylline was not influenced by the change in Na /K ratio. Pentifylline in combination with Nicotinic acid indicated for the treatment of Cerebral circulatory disorders and Circulatory disorders of the eye. Pentifylline is well tolerated but it is recommended that blood pressure be monitored and if there is a severe drop in blood pressure, a drip infusion of plasma expander be administered. Coagulation states should also be closely watched.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
2.0 mM [IC50]
0.81 mM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
COSALDON
Primary
COSALDON

OverviewOther

Other InhibitorOther SubstrateOther Inducer


Drug as perpetrator​

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Cerebral and peripheral circulatory disorders: 400 mg one tablet twice daily (Initial and normal dose) or 400 mg tablet daily for as long as necessary (Maintenance dose). Circulatory disorders of the eye: 400 mg two or three times daily (Initial and normal dose) or 400 mg once or twice daily for as long as necessary (Maintenance dose).
Route of Administration: Oral
In Vitro Use Guide
The secretion of type-I collagen COOH-terminal peptide (PIP) into the culture medium in the presence of pentifylline (PTF) was significantly lower than that in the presence of pentoxifylline (PTX) at concentrations of 10-1000 ug/ml; its level in cell lysate in the presence of PTX at concentrations of 10-100 ug/ml.