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编 号：F016263
分子式：C27H34N2O7
分子量：498.57
分子式：C27H34N2O7
分子量：498.57
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CAS No: 103775-10-6
产品详情
生物活性：
Moexipril is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril exhibits antihypertensive and neuroprotective effects-.
体内研究：
Moexipril can not cross the blood-brain barrier.Moexipril (3 mg/kg, 30 mg/kg and 10 mg/kg; p.o.; once daily; 5 days) exhibits a dose-dependent and antihypertensive effects in renal hypertensive rats, spontaneously hypertensive rats and perinephritic hypertensive dogs, respectively.Moexipril (0.3 mg/kg, i.p.) significantly reduces the infarct area on the mouse brain surface in NMRI mice.Moexipril (0.1 mg/kg, i.p.) significantly attenuates the cortical infarct volume in Long-Evans rats.Animal Model:Spontaneously hypertensive rats
Dosage:30 mg/kg
Administration:Oral gavage; once daily; 5 days
Result:Caused a progressive lowering of mean blood pressure from pretreatment values of 180 +/- 7 mmHg to a trough on day 4 of 127 +/- 4 mmHg.Dose-dependently decreased arterial blood pressure, and inhibited plasma and tissue ACE activity.
Animal Model:Renal hypertensive rats
Dosage:0.03-10 mg/kg
Administration:Oral gavage; once daily; 5 days
Result:Caused a dose-dependent decrease in blood pressure with a threshold dose of 0.3 mg/kg. Lowered mean blood pressure by about 70 mmHg of 3 mg/kg.
Animal Model:Perinephritic hypertensive dogs
Dosage:10 mg/kg
Administration:Oral gavage; once daily; 5 days
Result:Caused a drop of mean blood pressure by 25 mmHg from pre-treatment control, which persisted for 24 h, by a rapid onset and a long duration of action.
Animal Model:NMRI mice (male, Permanent focal ischemia)
Dosage:0, 0.03, 0.3, and 3 mg/kg
Administration:Intraperitoneal injection (1 h before middle cerebral artery occlusion)
Result:Significantly reduced the infarct area on the mouse brain surface with a dose of 0.3 mg/kg, and other doses were not effective.
Animal Model:Long-Evans rats (male, Permanent focal ischemia)
Dosage:0, 0.01, 0.1 mg/kg
Administration:Intraperitoneal injection (1 h before middle cerebral artery occlusion)
Result:Significantly attenuated the cortical infarct volume from 114.4 to 98.2 mm as compared to non-treated animals in a dose of 0.01 mg/kg, without reducing the infarct volume of the rat brain at dosages >0.01 mg/kg.
体外研究：
Moexipril is devoid of anti-inflammatory properties and has no effect on platelet function.Moexipril hydrolyzes to Moexiprilat, and Moexiprilat inhibits ACE in guinea pig serum as well as on purified ACE from rabbit lung with IC50s of 2.6 nM and 4.9 nM, respectively.Moexipril (0.01 nM-0.1 mM) exhibits high potency against both ACE in rats plasma and purified ACE from rabbit lung, with IC50s of 1.75 nM and 2.1 nM, respectively.Moexipril (0-100 μM, 24 h) significantly reduced the percentage of damaged neurons in a dose-dependent manner.Moexipril (0-100 μM, 24 h) significantly attenuates Fe2+/3+-induced neurotoxicity.Moexipril dose not cause significant changes in the percentage of apoptotic neurons.
Moexipril is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril exhibits antihypertensive and neuroprotective effects-.
体内研究：
Moexipril can not cross the blood-brain barrier.Moexipril (3 mg/kg, 30 mg/kg and 10 mg/kg; p.o.; once daily; 5 days) exhibits a dose-dependent and antihypertensive effects in renal hypertensive rats, spontaneously hypertensive rats and perinephritic hypertensive dogs, respectively.Moexipril (0.3 mg/kg, i.p.) significantly reduces the infarct area on the mouse brain surface in NMRI mice.Moexipril (0.1 mg/kg, i.p.) significantly attenuates the cortical infarct volume in Long-Evans rats.Animal Model:Spontaneously hypertensive rats
Dosage:30 mg/kg
Administration:Oral gavage; once daily; 5 days
Result:Caused a progressive lowering of mean blood pressure from pretreatment values of 180 +/- 7 mmHg to a trough on day 4 of 127 +/- 4 mmHg.Dose-dependently decreased arterial blood pressure, and inhibited plasma and tissue ACE activity.
Animal Model:Renal hypertensive rats
Dosage:0.03-10 mg/kg
Administration:Oral gavage; once daily; 5 days
Result:Caused a dose-dependent decrease in blood pressure with a threshold dose of 0.3 mg/kg. Lowered mean blood pressure by about 70 mmHg of 3 mg/kg.
Animal Model:Perinephritic hypertensive dogs
Dosage:10 mg/kg
Administration:Oral gavage; once daily; 5 days
Result:Caused a drop of mean blood pressure by 25 mmHg from pre-treatment control, which persisted for 24 h, by a rapid onset and a long duration of action.
Animal Model:NMRI mice (male, Permanent focal ischemia)
Dosage:0, 0.03, 0.3, and 3 mg/kg
Administration:Intraperitoneal injection (1 h before middle cerebral artery occlusion)
Result:Significantly reduced the infarct area on the mouse brain surface with a dose of 0.3 mg/kg, and other doses were not effective.
Animal Model:Long-Evans rats (male, Permanent focal ischemia)
Dosage:0, 0.01, 0.1 mg/kg
Administration:Intraperitoneal injection (1 h before middle cerebral artery occlusion)
Result:Significantly attenuated the cortical infarct volume from 114.4 to 98.2 mm as compared to non-treated animals in a dose of 0.01 mg/kg, without reducing the infarct volume of the rat brain at dosages >0.01 mg/kg.
体外研究：
Moexipril is devoid of anti-inflammatory properties and has no effect on platelet function.Moexipril hydrolyzes to Moexiprilat, and Moexiprilat inhibits ACE in guinea pig serum as well as on purified ACE from rabbit lung with IC50s of 2.6 nM and 4.9 nM, respectively.Moexipril (0.01 nM-0.1 mM) exhibits high potency against both ACE in rats plasma and purified ACE from rabbit lung, with IC50s of 1.75 nM and 2.1 nM, respectively.Moexipril (0-100 μM, 24 h) significantly reduced the percentage of damaged neurons in a dose-dependent manner.Moexipril (0-100 μM, 24 h) significantly attenuates Fe2+/3+-induced neurotoxicity.Moexipril dose not cause significant changes in the percentage of apoptotic neurons.
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