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RGW2938

Names

[ CAS No. ]:
111786-07-3

[ Name ]:
RGW2938

[Synonym ]:
Prinoxodanum
RGW 2938
3,4-Dihydro-3-methyl-6-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2(1H)-quinazolinone
Prinoxodanum [INN-Latin]
Prinoxodano [INN-Spanish]
PRINOXODAN
2(1H)-Quinazolinone,3,4-dihydro-3-methyl-6-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)
Prinoxodano
RGW2938

Biological Activity

[Description]:

RGW2938 is a phosphodiesterase inhibitor.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Cardiovascular Disease

[Target]

Phosphodiesterase[1]


[In Vitro]

RGW2938 is an orally effective positive inotropic/vasodilator agent. RGW2938 is a new nonglycoside, noncatecholamine cardiotonic/vasodilator agent is examined in vitro in isolated guinea pig hearts; in the latter, RGW2938 5 nmol-5 μmol increases contractility in a dose-related fashion[2].

[In Vivo]

RGW2938 is a new nonglycoside, noncatecholamine cardiotonic/vasodilator agent is examined in vivo in anesthetized and conscious dogs. RGW2938 30-300 μg/kg administered intravenously (i.v.) to anesthetized dogs increases contractile force while decreasing arterial pressure and total peripheral resistance (TPR) in a dose-related manner. Heart rate (HR) is only slightly increased, and aortic flow is not appreciably altered. A single oral dose of RGW2938 0.3 mg/kg administered to conscious chronically instrumented dogs produces a marked and sustained increase in contractility 15-240 min after treatment while only slightly increasing HR. The effects of RGW2938 30-300 μg/kg, i.v. are studied in a mecamylamine-propranolol-induced model of heart failure. RGW2938 effectively reverses the drug-induced heart failure by increasing myocardial contractility and decreasing arterial pressure while only slightly affecting HR[2].

[References]

[1]. Artigou JY, et al. [Evaluation of a new cardiotonic agent on human isolated atrium]. Ann Cardiol Angeiol (Paris). 1993 Feb;42(2):79-82.

[2]. Barrett JA, et al. Pharmacology of RG W-2938: a cardiotonic agent with vasodilator activity. J Cardiovasc Pharmacol. 1990 Oct;16(4):537-45.


[Related Small Molecules]

3-Isobutyl-1-methylxanthine | rolipram | PF-04957325 | AN-2728 | GLPG1690 | BAY-60-7550 | Icariin | Ibudilast | PF-8380 | TAK-063 | Dipyridamole | Cilostazol | GSK256066 | Cialis | Pentoxifylline

Chemical & Physical Properties

[ Density]:
1.47g/cm3

[ Molecular Formula ]:
C13H13N4O2

[ Molecular Weight ]:
257.27

[ PSA ]:
73.80000

[ LogP ]:
1.11830

[ Index of Refraction ]:
1.724

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VA3144000
CHEMICAL NAME :
2(1H)-Quinazolinone, 3,4-dihydro-3-methyl-6-(1,4,5,6-tetrahydro-6-oxo-3-py ridazinyl)-
CAS REGISTRY NUMBER :
111786-07-3
LAST UPDATED :
199512
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C13-H14-N4-O2
MOLECULAR WEIGHT :
258.31

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>2 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,323,1990

Related Compounds

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