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Olprinone Hydrochloride

Olprinone Hydrochloride用途

Olprinone(Loprinone)盐酸盐是磷酸二酯酶3(PDE3)抑制剂。

Olprinone Hydrochloride名称

[ CAS 号 ]:
119615-63-3

[ 中文名 ]:
1,2-二氢-5-咪唑并[1,2-a]吡啶-6-基-6-甲基-2-氧代-3-吡啶甲腈盐酸盐

[ 英文名 ]:
Olprinone (Hydrochloride)

[英文别名 ]:

E 1020
Olprinone hydrochloride
Olprinone (Hydrochloride)
MFCD01749474
Loprinone hydrochloride

Olprinone Hydrochloride生物活性

[ 描述 ]:

Olprinone(Loprinone)盐酸盐是磷酸二酯酶3(PDE3)抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 心血管疾病

[参考文献]

[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.

[相关活性小分子]

Olprinone Hydrochloride物理化学性质

[ 密度 ]:
1.34g/cm3

[ 熔点 ]:
>300ºC

[ 分子式 ]:
C₁₄H₁₁ClN₄O

[ 分子量 ]:
286.72

[ PSA ]:
83.18000

[ LogP ]:
2.60738

[ 储存条件 ]:
2-8℃

Olprinone HydrochlorideMSDS

详细MSDS(安全技术说明书)

Olprinone Hydrochloride毒性和生态

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

Olprinone Hydrochloride安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
US4201450

Olprinone Hydrochloride文献

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...

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