LY 344864 是一种选择性的、具有口服活性的5-HT1Freceptor激动剂，Ki为 6 nM。LY 344864 是一种完全激动剂，产生的效果与血清素本身的量级相似。 LY 344864 在一定程度上可以通过血脑屏障。
| 生物活性 | LY 344864 is a selective, orally active5-HT1Freceptoragonist with aKiof 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent[1]. |
| IC50& Target[1] | human 5-HT1FReceptor 0.006 μM (Ki) | human 5-HT1AReceptor 0.530 μM (Ki) | human 5-HT1BReceptor 0.549 μM (Ki) | human 5-HT1DReceptor 0.575 μM (Ki) | human 5-HT1EReceptor 1.415 μM (Ki) | human 5-HT2BReceptor 1.695 μM (Ki) | Human 5-HT2AReceptor 3.499 μM (Ki) | Human 5-HT3AReceptor 3.935 mM (Ki) | Human 5-HT7Receptor 4.851 μM (Ki) | rat α2-adrenergic receptor 3.69 μM (Ki) | rat α1-adrenergic receptor 5.06 μM (Ki) |
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体外研究
(In Vitro) | LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, 5-HT7, rat α1-adrenergic, rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively[1].
LY 344864 is a inducer of mitochondrial biogenesis[2].
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体内研究
(In Vivo) | LY 344864 (0-10 ng/kg; p.o. or i.v.; once) inhibits neurogenic dural inflammation in rat migraine pain model[1].
LY 344864 (1 mg/kg; i.v.; once) can cross the blood brain barrier to some extent in rats[1].
LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improved behavioral endpoints in a Parkinson’s disease mouse model[2].
| Animal Model: | Male Wistar rats, migraine pain model[1] | | Dosage: | 1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous) | | Administration: | Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation | | Result: | When given intravenously 10 minutes before stimulation, inhibited inflammation with an ID50(median infective dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal stimulation, an ID50of 1.2 ng/kg was obtained. |
| Animal Model: | Male C57BL/6 mice, Parkinson’s disease model[2] | | Dosage: | 2 mg/kg | | Administration: | Intraperitoneal injection, daily for 14d beginning 7d post-lesion | | Result: | Attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals, also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(284.56 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8456 mL | 14.2280 mL | 28.4560 mL | | 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | | 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.11 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.11 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.11 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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