| Identification | Back Directory | [Name]
LY 344864 | [CAS]
186544-26-3 | [Synonyms]
CS-660
Y344864
LY 344864
LY344864 HCL
LY344864;LY-344864
LY 344864 hydrochloride
(R)-N-[3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide
Benzamide, N-[(3R)-3-(dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluoro-
(R)-N-(3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl)-4-fluorobenzamide hydrochloride
N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamidehydrochloride | [Molecular Formula]
C21H22FN3O | [MDL Number]
MFCD07772184 | [MOL File]
186544-26-3.mol | [Molecular Weight]
351.42 |
| Chemical Properties | Back Directory | [Boiling point ]
471.9±45.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
DMSO : ≥ 350 mg/mL (995.96 mM) | [form ]
Powder | [pka]
14.12±0.40(Predicted) | [color ]
White to off-white | [Water Solubility ]
water: 10mM
DMSO: 100mM | [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 |
| Hazard Information | Back Directory | [Uses]
LY-344864 Hydrochloride is used as a selective 5-HTIF receptor agonist. | [Biological Activity]
Potent, selective 5-HT 1F receptor agonist (EC 50 = 3 nM). Displays > 80-fold selectivity over other 5-HT receptors (K i values are 0.006, 0.53, 0.55, 0.56, 1.42, 1.70, 3.50, 3.94 and 4.85 μ M for 5-HT 1F , 5-HT 1A , 5-HT 1B , 5-HT 1D , 5-HT 1E , 5-HT 2B , 5-HT 2C , 5-HT 2A and 5-HT 7 receptors respectively). Inhibits neurogenic dural inflammation in vivo following i.v. and oral administration. | [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-HT2A Receptor: 3.499 μM (Ki); Human 5-HT3A Receptor: 3.935 mM (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) |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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