Captopril是一种具有口服活性的血管紧张素转化酶（ACE）抑制剂，IC50值为0.025μM。
Cas No.:62571-86-2
Sample solution is provided at 25 µL, 10mM.
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Captopril is an orally active angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 0.025μM[1]. Captopril exerts its effects by blocking the conversion of angiotensin I to angiotensin II, thereby achieving vasodilation, lowering blood pressure, and reducing cardiac workload[2]. Captopril is commonly used in the treatment and research of hypertension, heart failure, and diabetic nephropathy[3,4].
In vitro, BV2 microglial cells were incubated with Captopril (0.1, 0.3, 1, and 3mM) and lipopolysaccharide (LPS, 7ng/mL) for 24h. Low concentrations of Captopril (0.3, 1mM) enhanced LPS-induced NO production, whereas a high concentration of Captopril (3mM) inhibited LPS-induced NO production[5].
In vivo, normal ICR mice were treated with Captopril (10mg/kg) by gavage for 8 weeks, resulting in decreased mean arterial pressure and serum calcium levels, as well as increased urinary calcium excretion[6]. BALB-c mice were pretreated with Captopril (25, 50mg/kg) via intraperitoneal injection for 7 days. On day 7, 30min after the last dose, pentylenetetrazole (PTZ, 60mg/kg) was injected to induce epileptic seizures. Captopril treatment significantly reduced the formation of dark neurons in the hippocampal CA1, CA2, CA3 regions and the dentate gyrus (DG)[7].
References:
[1] Afrin S, Rakib M A, Kim B H, et al. Eritadenine from edible mushrooms inhibits activity of angiotensin converting enzyme in vitro[J]. Journal of Agricultural and Food Chemistry, 2016, 64(11): 2263-2268.
[2] Bolterman R J, Manriquez M C, Ruiz M C O, et al. Effects of captopril on the renin angiotensin system, oxidative stress, and endothelin in normal and hypertensive rats[J]. Hypertension, 2005, 46(4): 943-947.
[3] Atkinson A B, Robertson J I S. Captopril in the treatment of clinical hypertension and cardiac failure[J]. The Lancet, 1979, 314(8147): 836-839.
[4] Heel R C, Brogden R N, Speight T M, et al. Captopril: a preliminary review of its pharmacological properties and therapeutic efficacy[J]. Drugs, 1980, 20(6): 409-452.
[5] Asraf K, Torika N, Apte R N, et al. Microglial activation is modulated by captopril: in vitro and in vivo studies[J]. Frontiers in Cellular Neuroscience, 2018, 12: 116.
[6] Yang M, Xia C, Song Y, et al. Impairing effects of angiotensin-converting enzyme inhibitor captopril on bone of normal mice[J]. European Journal of Pharmacology, 2016, 771: 40-47.
[7] Tastemur Y, Gumus E, Ergul M, et al. Positive effects of angiotensin-converting enzyme (ACE) inhibitor, captopril, on pentylenetetrazole-induced epileptic seizures in mice[J]. Tropical Journal of Pharmaceutical Research, 2020, 19(3): 637-643.
Captopril是一种具有口服活性的血管紧张素转化酶（ACE）抑制剂，IC50值为0.025μM[1]。Captopril通过阻断血管紧张素I转化为血管紧张素II，达到舒张血管、降低血压和减轻心脏负荷的效果[2]，通常用于高血压、心力衰竭及糖尿病肾病等的治疗和研究[3,4]。
在体外，Captopril（0.1, 0.3, 1, and 3mM）和脂多糖（LPS, 7ng/mL）与小胶质细胞BV2共培养24h，低浓度Captopril（0.3, 1mM）增强LPS诱导的NO产生，而高浓度Captopril（3mM）抑制LPS诱导的NO产生[5]。
在体内，Captopril（10mg/kg）通过灌胃处理正常ICR小鼠8周，小鼠平均动脉压和血清钙降低，尿钙增加[6]。Captopril（25, 50mg/kg）通过腹腔注射预处理BALB-c小鼠7天，第7天给药30min后注射pentylenetetrazole（PTZ, 60mg/kg）诱导癫痫发作，Captopril处理可显著减少海马CA1、CA2、CA3区和齿状回（DG）的暗神经元形成[7]。
| Cell experiment [1]: | |
Cell lines | BV2 microglia |
Preparation Method | BV2 microglia were incubated in 24-well plates in the presence of 7ng/ml LPS with Captopril (0.1, 0.3, 1 or 3mM) for 24h. Thereafter, supernatants were analyzed for nitrite levels using the Griess reaction. Nitrite levels were normalized to cell counts. |
Reaction Conditions | 0.1, 0.3, 1, and 3mM; 24h |
Applications | Treatment of BV2 cells with 7ng/ml LPS and low doses of Captopril (0.3 and 1mM) resulted in 50% and 45% increased NO production, respectively, as compared to cells induced with LPS alone. Higher dose of Captopril (3mM) reduced LPS-induced NO levels in the BV2 microglial cell line by more than 40%. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | Mice were pretreated with Captopril (25 or 50mg/kg; i.p.) for 7 days, then received PTZ (60mg/kg, i.p.) 30min after the last dose. The animals were sacrificed 4h later, and brain sections were stained with Toluidine blue to assess dark neurons in hippocampal regions. |
Dosage form | 25, 50mg/kg; 7 days; i.p. |
Applications | Both the 25 mg/kg and 50 mg/kg doses of Captopril significantly prevented dark neuron formation in CA1, CA2, and CA3 regions of the hippocampus and DG after PTZ induced seizures. |
References: | |
| Cas No. | 62571-86-2 | SDF | |
| 别名 | 卡托普利; SQ 14225 | ||
| 化学名 | (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid | ||
| Canonical SMILES | CC(CS)C(=O)N1CCCC1C(=O)[O-] | ||
| 分子式 | C9H15NO3S | 分子量 | 217.3 |
| 溶解度 | ≥ 21.7 mg/mL in DMSO, ≥ 105.2 mg/mL in EtOH with ultrasonic, ≥ 48.6 mg/mL in Water with ultrasonic | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.6019 mL | 23.0097 mL | 46.0193 mL |
| 5 mM | 920.4 μL | 4.6019 mL | 9.2039 mL |
| 10 mM | 460.2 μL | 2.301 mL | 4.6019 mL |
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