PENTIFYLLINE

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 Search

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

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Description
Sources: http://home.intekom.com/pharm/hmr/cosaldrt.html | https://www.ncbi.nlm.nih.gov/pubmed/170944 | https://www.ncbi.nlm.nih.gov/pubmed/227424

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 Target	Pharmacology	Potency
Phosphodiesterase 1 12 Target ID: CHEMBL2097166 Sources: https://www.ncbi.nlm.nih.gov/pubmed/170944	Inhibitor 8297	2.0 mM [IC50]
Phosphodiesterase 2A 7 Target ID: CHEMBL3477 Sources: https://www.ncbi.nlm.nih.gov/pubmed/170944	Inhibitor 8297	0.81 mM [IC50]
Brain ATPase (rat) 1 Target ID: Brain ATPase (rat) Sources: https://www.ncbi.nlm.nih.gov/pubmed/227424	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cerebral circulatory disorders 1 Sources: http://home.intekom.com/pharm/hmr/cosaldrt.html	Primary		Approved 8429	COSALDON Approved Use Indicated for the treatment of brain performance disorders in old age, degenerative vascular diseases in the eye.
Circulatory disorders of the eye 1 Sources: http://home.intekom.com/pharm/hmr/cosaldrt.html	Primary		Approved 8429	COSALDON Approved Use Indicated for the treatment of brain performance disorders in old age, degenerative vascular diseases in the eye.

PubMed

Title	Date	PubMed
[Cerebral sclerosis and its treatment with cosaldon].	1957 Jun 14	13451071
[Treatment of cerebral arteriosclerosis with cosaldon].	1960 May 6	13833290

Patents

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.

Name

Type

Language

PENTIFYLLINE

Official Name

English

1-HEXYLTHEOBROMINE

Systematic Name

English

PENTIFYLLINE [MART.]

Common Name

English

pentifylline [INN]

Common Name

English

PENTIFYLLINE [MI]

Common Name

English

Pentifylline [WHO-DD]

Common Name

English

1-HEXYL-3,7-DIMETHYLXANTHINE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1327