PROXYPHYLLINE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C10H14N4O3
Molecular Weight	238.2432
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(O)CN1C=NC2=C1C(=O)N(C)C(=O)N2C

InChI

InChIKey=KYHQZNGJUGFTGR-UHFFFAOYSA-N

InChI=1S/C10H14N4O3/c1-6(15)4-14-5-11-8-7(14)9(16)13(3)10(17)12(8)2/h5-6,15H,4H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C10H14N4O3
Molecular Weight	238.2432
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Proxyphylline is a xanthine derivative that acts as a cardiac stimulant, vasodilator and bronchodilator. In combination with ephedrine it’s used for relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema. Proxyphylline is readily absorbed from the gastrointestinal tract and it’s not converted to theophylline in the body. The clinical studies are agreed with the property of proxyphylline to inhibit the cyclic nucleotide phosphodiesterases.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
3',5'-cyclic phosphodiesterase 5	Inhibitor 8,297

Conditions

Condition	Modality	Highest Phase	Product
Obstructive airways disease 1	Secondary	Approved 8,429	Novofilin
Asthma 241	Secondary	Approved 8,429	Unknown
Bronchial disorders 1	Secondary	Approved 8,429	Unknown

PubMed

Show entries

Title	Date	PubMed
[Effectiveness of proxyphylline in chronic obstructive pulmonary disease (author's transl)].	1980 Jun 20	7408664
Antianaphylactic and antiasthmatic properties of new piperazinyl 7-(beta-hydroxypropyl)-theophylline derivatives in guinea pigs.	2001 Mar-Apr	11787952
Application of micellar electrokinetic chromatography to the quality control of a pharmaceutical preparation containing three bronchodilators.	2002 Feb	11870768
Polymer particle erosion controlling drug release. II. Swelling investigations to clarify the release mechanism.	2002 Oct 24	12429482
The role of the discriminant factor in the assessment and treatment of alcoholic hepatitis.	2004 May-Jun	15100527

Showing 1 to 5 of 8 entries

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Patents

Sample Use Guides

In Vivo Use Guide

intravenous: 29 mumol/kg single oral: 21 mumol/kg and multiple oral: 21 mumol/kg three times a day

Route of Administration: Other

In Vitro Use Guide

Inhibition of cAMP and cGMP hydrolysis in human lung tissue by proxyphylline and its main metabolite 1-methyl-7-(beta-hydroxypropyl)xanthine was compared with theophylline and its metabolite 3-methylxanthine. The Inhibition constant of proxyphylline was 0.06-0.7 mmol/l at low cAMP concentrations and at low and high cGMP concentrations, while it was 1.0 mmol/l at high cAMP concentrations