MOXAVERINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H21NO2
Molecular Weight	307.3862
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCC1=NC(CC2=CC=CC=C2)=C3C=C(OC)C(OC)=CC3=C1

InChI

InChIKey=MYCMTMIGRXJNSO-UHFFFAOYSA-N

InChI=1S/C20H21NO2/c1-4-16-11-15-12-19(22-2)20(23-3)13-17(15)18(21-16)10-14-8-6-5-7-9-14/h5-9,11-13H,4,10H2,1-3H3

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23203292 | https://clinicaltrials.gov/ct2/show/NCT00709449

Moxaverine, a derivative of papaverine, is a phosphodiesterase inhibitor. Moxaverine has been studied in phase III of a clinical trial for the treatment of ocular blood flow in patients with age- related macular degeneration and primary open angle glaucoma. In addition, it has been studied in phase II of the clinical trial for the treatment of ischemia. This compound is prohibited by FEI (International Federation of equine).

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Phosphodiesterase 4 52 Target ID: CHEMBL2093863 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2854468	Inhibitor 8297

Conditions

Condition	Modality	Highest Phase	Product
Macular degeneration 4 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20456253	Primary	Phase III 656	Unknown Approved Use Unknown
Glaucoma 57 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20456253	Primary	Phase III 656	Unknown Approved Use Unknown
Ischemia 16 Sources: https://clinicaltrials.gov/ct2/show/NCT00569621	Primary	Phase II 1132	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Construction and validation of a microprocessor controlled extracorporal circuit in rats for the optimization of isolated limb perfusion.	2004 Dec	15597400
Tissue distribution of moxaverine-hydrochloride in the rabbit eye and plasma.	2005 Jun	15969638
Effect of systemic moxaverine on ocular blood flow in humans.	2009 Nov	18778333

Patents

Sample Use Guides

In Vivo Use Guide

intravenous infusion of 150 mg in 250 ml NaCl, applied over 30 minutes.

Route of Administration: Intravenous

In Vitro Use Guide

Using a combination of techniques to assess quantitatively the shape and the filterability of red blood cells (RBC) after exposure to stress conditions (400 mosmol/l, lactacidosis, pH 6.8), the effects of 1-benzyl-3-ethyl-6,7-dimethoxy-isoquinoline hydrochloride (moxaverine-HCl, Kollateral) were tested. The shape of freely suspended RBC was quantified using the tangent count procedure. Moxaverine, when present in doses between 10(-5) und 10(-2) mol/l while the RBC are stressed, restored both the normal discoid red cell configuration and the microrheological performance when tested under low shear stresses. The data showed that moxaverine exerted protective effects on RBC membrane curvature and whole cell microrheological behavior (performance).

Name

Type

Language

MOXAVERINE

Official Name

English

Moxaverine [WHO-DD]

Common Name

English

1-BENZYL-3-ETHYL-6,7-DIMETHOXYISOQUINOLINE

Systematic Name

English

MOXAVERINE [MI]

Common Name

English

moxaverine [INN]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QA03AD30