| Identification | Back Directory | [Name]
N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluoro-benzamide hydrochloride | [CAS]
1217756-94-9 | [Synonyms]
LY344864 hydrochloride >=98% (HPLC) | [Molecular Formula]
C21H23ClFN3O | [MDL Number]
MFCD09971079 | [MOL File]
1217756-94-9.mol | [Molecular Weight]
387.878 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
H2O: soluble10mg/mL, clear | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 10mg/mL, clear | [InChI]
1S/C21H22FN3O.ClH/c1-25(2)16-8-10-20-18(12-16)17-11-15(7-9-19(17)24-20)23-21(26)13-3-5-14(22)6-4-13;/h3-7,9,11,16,24H,8,10,12H2,1-2H3,(H,23,26);1H/t16-;/m1./s1 | [InChIKey]
OKUHLSYESBLBCP-PKLMIRHRSA-N | [SMILES]
Fc1ccc(cc1)C(=O)Nc2cc3c([nH]c4c3C[C@@H](CC4)N(C)C)cc2.Cl |
| Hazard Information | Back Directory | [Uses]
LY-344864 Hydrochloride is used as a selective 5-HTIF receptor agonist. | [Biological Activity]
LY344864 hydrochloride is a potent and selective 5-HT1F receptor agonist. It has an EC50 of 3 nMand displays > 80-fold selectivity over other 5-HT receptors ''LY344864 might be useful in the treatment approach for migraine. LY344864 is found to prevent the extravasation of dura protein and reduce c-fos like immunoreactions induced by capsaicin. | [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 ID50 of 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. |
| [IC 50]
human 5-HT1F Receptor: 0.006 μM (Ki); 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) | [storage]
Store at -20°C |
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