LY 344864 hydrochloride 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 hydrochloride 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 hydrochloride 在一定程度上可以通过血脑屏障。
| 生物活性 | LY 344864 hydrochloride is a selective, orally active5-HT1Freceptoragonist with aKiof 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride 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-HT2CReceptor 3.499 μM (Ki) | Human 5-HT3AReceptor 3.935 μM (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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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