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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Neuronal Signal Pathway > 8-OH-DPATCAS：78950-78-4
Molecular Formula：C16H25NO
Molecular Weight：247.38
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥95%
Appearance：White to off-white Solid
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| CAS | 78950-78-4 |
| Name | 8-OH-DPAT |
| Molecular Formula | C16H25NO |
| Molecular Weight | 247.38 |
| Solubility | Soluble in DMSO |
| Purity | ≥95% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | CCCN(CCC)C1CCC2=C(C1)C(=CC=C2)O |
| InChIKey | ASXGJMSKWNBENU-UHFFFAOYSA-N |
| InChI | InChI=1S/C16H25NO/c1-3-10-17(11-4-2)14-9-8-13-6-5-7-16(18)15(13)12-14/h5-7,14,18H,3-4,8-12H2,1-2H3 |
| PubChem CID | 1220 |
| Target Point | 5-HT Receptor |
| Passage | Neuronal Signaling;GPCR & G Protein |
| Background | 8-OH-DPAT is a potent and selective 5-HT agonist. |
| Biological Activity | 8-OH-DPAT (8-Hydroxy-DPAT)是一种经典的5-HT1A激动剂，pIC50为8.19。对5-HT1结合位点亚型具有近1000倍选择性，其半衰期为1.5小时。[1-4] |
| In Vitro | 8-OH-DPAT对5-HT1B仅有微弱的效果，pIC50为5.42 ± 0.08(n = 5)。 在浓度低于100 nM时，8-OH-DPAT对5-HT1B没有效果[1]。在人类RPE细胞中，8-OH-DPAT能够减少自噬来源和感光细胞外节段来源的脂褐质、增加抗氧化保护能力和减少氧化损伤[4]。 |
| In Vivo | 在严重出血时，对低血压患者静脉注射8-OH-DPAT可快速逆转其心搏徐缓的反应。8-OH-DPAT是亲脂性分子，能够穿透血脑屏障[3]。 |
| Cell Experiment | Animal Models: Male Lister hooded rats; Dosages: 0，3.0，10，100 和 300 μg/kg; Administration: i.p.[2] |
| Animal Experiment | 将细胞暴露在200 μM H202下1小时，或是在暴露前或暴露后用10 μM 8-OH DPAT处理24小时。如果是预处理，在H2O2暴露后24小时进行检测；如果是暴露后加药处理，在H2O2暴露后立即加药。为了检测8-OH DPAT在RPE细胞中减少脂褐质形成的效果，将0.1-20 μM的化合物加入到培养基中，每48小时更换一次。实验使用的是基础培养基，对照组加入的是PBS作为阴性对照。为了检验终止5-HT1A受体激动剂处理后，8-OH DPAT的药效持续作用，在处理28天后，终止8-OH DPAT的加药，将细胞继续培养在基础培养基中或fed POS中28天。为了检测8-OH DPAT去除现有的脂褐质的能力，让自噬来源的脂褐质和噬菌来源的脂褐质累积起来，然后隔一天进行一次8-OH DPAT的加药处理，持续28天。为了确认8-OH DPAT是通过5-HT1A受体发挥作用，在一些实验中用到了另一种5-HT1A激动剂S(-)-UH-301。为了检测8-OH DPAT对氧化应激标记的时间效应，在将细胞暴露于200 μM H2O2中1小时前，对RPE细胞进行8-OH DPAT(at 1 or 10 μM)的预处理，预处理3小时或24小时；或是用其他5HT1A激动剂进行处理。没有处于氧化应激条件下的细胞作为阴性对照，而处于氧化应激中、但没有进行药物处理的作为阳性对照。[4] |
| Data Literature Source | [1] Middlemiss DN，et al. Eur J Pharmacol. 1983，90(1):151-3. [2] Montgomery AM，et al. J Neural Transm Gen Sect. 1991，83(1-2):139-48. [3] Scrogin KE. Am J Physiol Regul Integr Comp Physiol. 2003，284(3):R782-91. [4] Thampi P，et al. PLoS One. 2012，7(4):e34468. |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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