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编 号：F437962
分子式：C16H22N2O3
分子量：290.36
分子式：C16H22N2O3
分子量：290.36
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CAS No: 72332-33-3
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生物活性：
Procaterol is an oral selective β2 adrenergic receptor agonist. Procaterol inhibits eosinophil migration and the release of eosinophil chemotactic factor from BEAS-2B cells through a cyclic AMP-dependent mechanism. Procaterol has a large dose difference existing between the bronchodilator effect and the anabolic effect in rat, can be used for asthma research in athletes.
体内研究：
Procaterol (0.03-1 mg/kg, inhalation 3 times a day, 14 days) 大鼠腓肠肌的重量或体重增加没有明显变化。Procaterol (1 mg/kg, inhalation 3 times a day, 14 days) 显著地增加了提肛肌的重量，有合成代谢作用。Procaterol (1 mg/kg, inhalation 3 times a day, 14 days) 增加腹侧前列腺重量与药物对组织中b2肾上腺素受体的刺激有关。Procaterol (1 mg/kg, inhalation 3 times a day, 14 days) 的支气管扩张作用与合成代谢作用的剂量差异大于 30 倍，小于100 倍。Procaterol (0.1, 1, 10 mg/kg, orally, before ovalbumin (HY-W250978) (OVA) inhalation) 吸入不会增强气道高反应性、气道壁炎症或气道壁增厚，并能减少嗜酸性粒细胞的数量。Animal Model:Six-week-old rats were castrated on Day – 5, except for a normal group of 6 rats
Dosage:0.03, 0.1, 0.3, 1 mg/mL
Administration:in-halation 3 times a day (09 : 00, 12 : 00, 16 : 00) for 14 days from Day 0 to Day 13.
Result:No significant changed in weight or body weight gain in rat gastrocnemius muscle. Significantly increased the weight of the levator ani muscle. Increasd in ventral prostate weight.
Animal Model:Mice immunized with ovalbumin (HY-W250978) (OVA, inhalation of 20 mg/mL OVA for 10 minutes every other day, total 7 times) + alum
Dosage:0.1, 1, 10 mg/kg
Administration:orally, before ovalbumin (HY-W250978) (OVA) inhalation
Result:Inhalation did not enhance airway hyperresponsiveness, airway wall inflammation, or airway wall thickening after OVA inhalation.Reduced the number of eosinophils in BALF mice.
体外研究：
Procatero (10-1000 ng/mL, 12, 24, 48 h, BEAS-2B) 通过环 AMP 依赖性机制直接抑制嗜酸性粒细胞迁移和 BEAS-2B 细胞中嗜酸性粒细胞趋化因子的释放。Procaterol (10-1000 ng/mL, 12, 24, 48 h, BEAS-2B) 剂量依赖性抑制 BEAS-2B 细胞单层对 IL-1b 和 TNF-a 反应的 RANTES 释放, 在 IL-1b 作用下增强 GM-CSF mRNA 的表达。Procaterol (0.1 μM, 72 h, Human tracheal surface epithelial cells) 可降低鼻病毒滴度和 RNA、细胞因子浓度、鼻病毒感染易感性、14 型鼻病毒受体细胞间粘附分子-1 (ICAM-1) 的表达以及鼻病毒 RNA 进入细胞质的细胞内酸性内体的数量。Procaterol (10 nM, one time, Lung ephelial cells) 通过 cAMP 以剂量依赖的方式增加 ciliary bend amplitude (CBA) 和 ciliary beating frequency (CBF)。
Procaterol is an oral selective β2 adrenergic receptor agonist. Procaterol inhibits eosinophil migration and the release of eosinophil chemotactic factor from BEAS-2B cells through a cyclic AMP-dependent mechanism. Procaterol has a large dose difference existing between the bronchodilator effect and the anabolic effect in rat, can be used for asthma research in athletes.
体内研究：
Procaterol (0.03-1 mg/kg, inhalation 3 times a day, 14 days) 大鼠腓肠肌的重量或体重增加没有明显变化。Procaterol (1 mg/kg, inhalation 3 times a day, 14 days) 显著地增加了提肛肌的重量，有合成代谢作用。Procaterol (1 mg/kg, inhalation 3 times a day, 14 days) 增加腹侧前列腺重量与药物对组织中b2肾上腺素受体的刺激有关。Procaterol (1 mg/kg, inhalation 3 times a day, 14 days) 的支气管扩张作用与合成代谢作用的剂量差异大于 30 倍，小于100 倍。Procaterol (0.1, 1, 10 mg/kg, orally, before ovalbumin (HY-W250978) (OVA) inhalation) 吸入不会增强气道高反应性、气道壁炎症或气道壁增厚，并能减少嗜酸性粒细胞的数量。Animal Model:Six-week-old rats were castrated on Day – 5, except for a normal group of 6 rats
Dosage:0.03, 0.1, 0.3, 1 mg/mL
Administration:in-halation 3 times a day (09 : 00, 12 : 00, 16 : 00) for 14 days from Day 0 to Day 13.
Result:No significant changed in weight or body weight gain in rat gastrocnemius muscle. Significantly increased the weight of the levator ani muscle. Increasd in ventral prostate weight.
Animal Model:Mice immunized with ovalbumin (HY-W250978) (OVA, inhalation of 20 mg/mL OVA for 10 minutes every other day, total 7 times) + alum
Dosage:0.1, 1, 10 mg/kg
Administration:orally, before ovalbumin (HY-W250978) (OVA) inhalation
Result:Inhalation did not enhance airway hyperresponsiveness, airway wall inflammation, or airway wall thickening after OVA inhalation.Reduced the number of eosinophils in BALF mice.
体外研究：
Procatero (10-1000 ng/mL, 12, 24, 48 h, BEAS-2B) 通过环 AMP 依赖性机制直接抑制嗜酸性粒细胞迁移和 BEAS-2B 细胞中嗜酸性粒细胞趋化因子的释放。Procaterol (10-1000 ng/mL, 12, 24, 48 h, BEAS-2B) 剂量依赖性抑制 BEAS-2B 细胞单层对 IL-1b 和 TNF-a 反应的 RANTES 释放, 在 IL-1b 作用下增强 GM-CSF mRNA 的表达。Procaterol (0.1 μM, 72 h, Human tracheal surface epithelial cells) 可降低鼻病毒滴度和 RNA、细胞因子浓度、鼻病毒感染易感性、14 型鼻病毒受体细胞间粘附分子-1 (ICAM-1) 的表达以及鼻病毒 RNA 进入细胞质的细胞内酸性内体的数量。Procaterol (10 nM, one time, Lung ephelial cells) 通过 cAMP 以剂量依赖的方式增加 ciliary bend amplitude (CBA) 和 ciliary beating frequency (CBF)。
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