LY 344864 hydrochloride
Based on 2 publication(s) in Google Scholar
LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 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.
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- CAS No.: 1217756-94-9
- Formula: C21H23ClFN3O
- Molecular Weight:387.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) LY 344864 hydrochloride
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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human 5-HT1F Receptor 0.006 μM (Ki) |
5-HT1F Receptor |
human 5-HT1A Receptor 0.530 μM (Ki) |
human 5-HT1B Receptor 0.549 μM (Ki) |
human 5-HT1D Receptor 0.575 μM (Ki) |
human 5-HT1E Receptor 1.415 μM (Ki) |
human 5-HT2B Receptor 1.695 μM (Ki) |
Human 5-HT2C Receptor 3.499 μM (Ki) |
Human 5-HT3A Receptor 3.935 μM (Ki) |
Human 5-HT7 Receptor 4.851 μM (Ki) |
rat α2-adrenergic receptor 3.69 μM (Ki) |
rat α1-adrenergic receptor 5.06 μM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats, migraine pain model[1]
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Dosage:1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous)
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Administration:Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation
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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 ID50 of 1.2 ng/kg was obtained.
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Animal Model:Male C57BL/6 mice, Parkinson’s disease model[2]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection, daily for 14d beginning 7d post-lesion
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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.
Chemical Information
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CAS No. 1217756-94-9
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Molecular Weight 387.88
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Formula C21H23ClFN3O
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SMILES
O=C(NC1=CC2=C(NC3=C2C[C@H](N(C)C)CC3)C=C1)C4=CC=C(F)C=C4.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
Purity & Documentation
References
[1]. Phebus LA, et al. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. [Content Brief]
[2]. Scholpa NE, et al. 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. Br J Pharmacol. 2018 Jan;175(2):348-358. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)