CAS 119615-63-3|Olprinone (Hydrochloride)

[1]. Tsubokawa T, Ishizuka S, Fukumoto K, et al. The effect of hemodilution by cardiopulmonary bypass on protein binding of olprinone. J Anesth. 2012 .

[2]. Mokra D, Drgova A, Pullmann R Sr, et al. Selective phosphodiesterase 3 inhibitor olprinone attenuates meconium-induced oxidative lung injury. Pulm Pharmacol Ther. 2012 Jun;25(3):216-22.

[3]. Yamanaka H, Hayashi Y, Kamibayashi T, Mashimo T. Effect of olprinone, a phosphodiesterase III inhibitor, on balance of cerebral oxygen supply and demand during cardiopulmonary bypass. J Cardiovasc Pharmacol. 2011 May;57(5):579-83.

[4]. Mazzon E, Esposito E, Di Paola R, et al. Olprinone, a specific phosphodiesterase (PDE)-III inhibitor, reduces the development of multiple organ dysfunction syndrome in mice. Pharmacol Res. 2011 Jul;64(1):68-79.

CHEMICAL IDENTIFICATION

RTECS NUMBER :

US4201450

CHEMICAL NAME :

3-Pyridinecarbonitrile, 1,2-dihydro-5-(imidazo(1,2-a)pyridin-6-yl)-6-methyl-2 -oxo-, monohydrochloride, monohydrate

CAS REGISTRY NUMBER :

119615-63-3

LAST UPDATED :

199703

DATA ITEMS CITED :

13

MOLECULAR FORMULA :

C14-H10-N4-O.Cl-H.H2-O

MOLECULAR WEIGHT :

304.76

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

7804 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - lacrimation Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

2133 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Skin and Appendages - hair

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

176 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>10 gm/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - tremor

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

3898 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - ptosis Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

242 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

>100 mg/kg

TOXIC EFFECTS :

Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Gastrointestinal - nausea or vomiting

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

175 mg/kg/4W-I

TOXIC EFFECTS :

Behavioral - fluid intake Cardiac - EKG changes not diagnostic of specified effects Kidney, Ureter, Bladder - urine volume increased

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

DOSE :

11 mg/kg

SEX/DURATION :

female 7-17 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

DOSE :

130 mg/kg

SEX/DURATION :

female 6-18 day(s) after conception

TOXIC EFFECTS :

Reproductive - Maternal Effects - other effects Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :

Micronucleus test

TYPE OF TEST :

Micronucleus test

MUTATION DATA

TYPE OF TEST :

Cytogenetic analysis

TEST SYSTEM :

Rodent - hamster Lung

DOSE/DURATION :

1200 mg/L

REFERENCE :

KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,77,1993

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Olprinone is a specific phosphodiesterase (PDE)-III inhibitor, which has been found to have anti-inflammatory effects in addition to its main inotropic and peripheral vasodilatory effects. In the pres...