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Submit ReviewLY 344864 hydrochloride
Description: Potent and selective 5-HT1F agonist
Chemical Name: N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for LY 344864 hydrochloride
LY 344864 hydrochloride is a potent, selective 5-HT1F receptor agonist (EC50 = 3 nM). Displays > 80-fold selectivity over other 5-HT receptors (Ki values are 0.006, 0.53, 0.55, 0.56, 1.42, 1.70, 3.50, 3.94 and 4.85 μM for 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2B, 5-HT2C, 5-HT2A and 5-HT7 receptors respectively). Inhibits neurogenic dural inflammation in vivo following i.v. and oral administration.
Licensing Information
Sold under license from Eli Lilly and Company
Compound Libraries for LY 344864 hydrochloride
LY 344864 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LY 344864 hydrochloride
| M. Wt | 387.88 |
| Formula | C21H22N3OF.HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1217756-94-9 |
| PubChem ID | 56972176 |
| InChI Key | OKUHLSYESBLBCP-PKLMIRHRSA-N |
| Smiles | Cl[H].CN(C)[C@@H]1CCC2=C(C1)C1=CC(NC(=O)C3=CC=C(F)C=C3)=CC=C1N2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for LY 344864 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 19.39 | 50 | |
| DMSO | 38.79 | 100 |
Preparing Stock Solutions for LY 344864 hydrochloride
The following data is based on the product molecular weight 387.88. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.58 mL | 12.89 mL | 25.78 mL |
| 5 mM | 0.52 mL | 2.58 mL | 5.16 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.58 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets for LY 344864 hydrochloride
References for LY 344864 hydrochloride
References are publications that support the biological activity of the product.
Ramadan et al (2003) 5-HT1F receptor agonists in acute migraine treatment: a hypothesis. Cephalalgia 23 776 PMID: 14510923
Goadsby and Classey (2003) Evidence for serotonin (5-HT)1B, 5-HT1D and 5-HT1F receptor inhibitory effects on trigeminal neurons with craniovascular input. Neuroscience 122 491 PMID: 14614913
Lee et al (1997) 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 Science 61 2117
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Keywords: LY 344864 hydrochloride, LY 344864 hydrochloride supplier, Potent, selective, 5-HT1F, agonists, Serotonin, Receptors, LY344864, hydrochloride, 2451, Tocris Bioscience
3 Citations for LY 344864 hydrochloride
Citations are publications that use Tocris products. Selected citations for LY 344864 hydrochloride include:
Garrett et al (2014) Agonism of the 5-hydroxytryptamine 1F receptor promotes mitochondrial biogenesis and recovery from acute kidney injury. J Pharmacol Exp Ther 350 257 PMID: 24849926
Scholpa et al (2018) 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. Br J Pharmacol 175 348 PMID: 29057453
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.