Orexin A (Hypocretin-1) (human, rat, mouse) acetate 是一种具有镇痛特性的下丘脑神经肽 (可透过血脑屏障)。Orexin A (human, rat, mouse) acetate 也是一种OX1R激动剂，能以时间和剂量依赖性的方式诱导 SH-SY5Y 细胞BDNF和TH蛋白的表达。Orexin A (human, rat, mouse) acetate 可用于食欲调节、神经退行性疾病，以及调节伤害性信息传递的研究。
| 生物活性 | Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate is also anOX1Ragonist that induces the expression ofBDNFandTHproteins in SH-SY5Y cells in a time- and dose-dependent manner. Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging[1][2][3]. |
体外研究
(In Vitro) | Orexin A (human, rat, mouse) acetate (0.1, 1, 10, 100 nM; 24 h) increases the expression of BDNF in SH-SY5Y human dopaminergic neuroblastoma cells in a dose-dependent manner[1].
Orexin A (human, rat, mouse) acetate (1 nM; 1, 3, 6, 12, 24 h) increases the expression of BDNF, TH, and PI3K in a time-dependent manner in SH-SY5Y cells[1].
Western Blot Analysis[1] | Cell Line: | SH-SY5Y cells | | Concentration: | 0.1, 1, 10, 100 nM | | Incubation Time: | 24 h | | Result: | Increased the expression of PI3K and TH in a dose-dependent manner.
Significantly induced BDNF expression at the dose of 1 and 10 nM. |
Western Blot Analysis[1] | Cell Line: | SH-SY5Y cells | | Concentration: | 1 nM | | Incubation Time: | 1, 3, 6, 12, 24 h | | Result: | Showed the expression of PI3K rapidly increased by 72.6 % as soon as 3 h, which maintained at high levels in the following 24 h.
Increased the protein level of BDNF and the increased rate was 44.8%, and the protein level of TH significantly increased at 12 h by 48.5%. |
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体内研究
(In Vivo) | Orexin A (human, rat, mouse) acetate (300 ng/mouse; i.c.v.; single daily for 8 days) attenuates the loss of dopaminergic neurons and the decrease of tyrosine hydroxylase (TH) expression in the substantia nigra, normalized the striatal dopaminergic fibers, and prevents the depletion of dopamine and its metabolites in the striatum[1].
Orexin A (human, rat, mouse) acetate (10, 30 mg/kg; i.v.; single) shows to be analgesic in the carrageenan-induced thermal hyperalgesia model and PPQ-induced mouse abdominal constriction model[2].
| Animal Model: | Male C57BL/6 mice (10-week-old; 22-26 g; MPTP-Induced Mouse Model of PD)[1]. | | Dosage: | 300 ng/mouse | | Administration: | Intracerebroventricular injection; single daily for 8 days | | Result: | Reversed MPTP-induced motor impairments via OX1R and increased the protein expression of BDNF in nigral dopaminergic neurons.
Improved MPTP-induced impairments in spatial Learning and memory and protected dopaminergic neurons against MPTP-induced neurotoxicity.
Attenuated the reduction of dopaminergic neurons in the substantia nigra and restored the reduction of dopaminergic fibers in the striatum. |
| Animal Model: | Female ICR mice (17-28 g; carrageenan-induced thermal hyperalgesia model)[2]. | | Dosage: | 10, 30 mg/kg | | Administration: | Intravenous injection; single; 5 min pre-test | | Result: | Increased paw withdrawal latency to the thermal stimulus back to baseline levels. |
| Animal Model: | Male ICR mice (17-20 g; phenyl-p-quinone (PPQ)-induced mouse abdominal constriction model)[2]. | | Dosage: | 3, 10, 30 mg/kg | | Administration: | Intravenous injection; single; given immediately before PPQ | | Result: | Increased the latency to the first PPQ-induced constriction from 357.4 s (blank control group) to 500.3 s at 10 mg/kg and 594.5 s at 30 mg/kg. |
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| 分子量 | |
| 性状 | |
| Formula | |
| Sequence Shortening | {Glp}-PLPDCCRQKTCSCRLYELLHGAGNHAAGILTL-NH2 (Disulfide bridge: Cys6-Cys12, Cys7-Cys14) |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| 溶解性数据 | In Vitro: H2O : ≥ 50 mg/mL(13.81 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 0.2762 mL | 1.3808 mL | 2.7616 mL | | 5 mM | 0.0552 mL | 0.2762 mL | 0.5523 mL | | 10 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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