Olprinone (Hydrochloride)

Modify Date: 2024-01-07 16:06:30

Olprinone (Hydrochloride) Structure
Olprinone (Hydrochloride) structure
Common Name Olprinone (Hydrochloride)
CAS Number 119615-63-3 Molecular Weight 286.72
Density 1.34g/cm3 Boiling Point N/A
Molecular Formula C14H11ClN4O Melting Point >300ºC
MSDS USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of Olprinone (Hydrochloride)


Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.

 Names

Name 5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-1H-pyridine-3-carbonitrile,hydrochloride
Synonym More Synonyms

 Olprinone (Hydrochloride) Biological Activity

Description Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor. IC50 value:Target: PDE3Olprinone is used as cardiotonic agent with positive inotropic and vasodilating effects. Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB). Olprinone was infused at a rate of 0.2 μg/kg/min when weaning from CPB was started. Olprinone has also shown potent antioxidative and anti-inflammatory effects in the meconium-induced oxidative lung injury.
Related Catalog
References

[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 & Physical Properties

Density 1.34g/cm3
Melting Point >300ºC
Molecular Formula C14H11ClN4O
Molecular Weight 286.72
PSA 83.18000
LogP 2.60738
Storage condition 2-8℃

 Toxicological Information

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

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi: Irritant;
Risk Phrases R36/37/38
Safety Phrases S26
RIDADR NONH for all modes of transport
RTECS US4201450

 Articles25

More Articles
Anti-inflammatory treatment in dysfunction of pulmonary surfactant in meconium-induced acute lung injury.

Adv. Exp. Med. Biol. 756 , 189-96, (2013)

Inflammation, oxidation, lung edema, and other factors participate in surfactant dysfunction in meconium aspiration syndrome (MAS). Therefore, we hypothesized that anti-inflammatory treatment may reve...

Olprinone attenuates the development of ischemia/reperfusion injury of the gut.

Intensive Care Med. 36(7) , 1235-47, (2010)

Splanchnic artery occlusion (SAO) shock is a severe form of circulatory shock produced by ischemia and reperfusion of the splanchnic organs. The occlusion and reperfusion of the splanchnic arteries ca...

Olprinone, a specific phosphodiesterase (PDE)-III inhibitor, reduces the development of multiple organ dysfunction syndrome in mice.

Pharmacol. Res. 64(1) , 68-79, (2011)

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...

 Synonyms

E 1020
pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile hydrochloride
Olprinone hydrochloride
Olprinone (Hydrochloride)
1,2-dihydro-5-imidazo<1,2-a>pyridin-6-yl-6-methyl-2-oxo-3-pyridine carbonitrile hydrochloride
1,2-dihydro-6-methyl-2-oxo-5-(imidazo[1,2-a]pyridin-6-yl)-3-pyridine carbonitrile hydrochloride
MFCD01749474
Loprinone hydrochloride
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