LY 344864
Catalog No.
A3569
5-HT1F受体激动剂
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IC50 Value: 6 nM(Ki) LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. It possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1]. in vitro: he 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs [2]. in vivo: After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels declined with time whereas brain cortex levels remained relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibited dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Sumatriptan, zolmitriptan, rizatriptan, and naratriptan all contracted the rabbit saphenous vein from baseline tone, whereas LY344864 in concentrations up to 10(-4) M did not contract the rabbit saphenous vein. Furthermore, vascular contractions to sumatriptan were markedly augmented in the presence of prostaglandin F(2alpha) (PGF(2alpha)). However, even in the presence of PGF(2alpha) (3 x 10(-7) M), LY344864 did not contract the rabbit saphenous vein in concentrations well in excess of its 5-HT(1F) receptor affinity (pK(i) = 8.2) [3]. Clinical trial: N/A
Storage | Store at -20°C |
M.Wt | 351.42 |
Cas No. | 186544-26-3 |
Formula | C21H22FN3O |
Synonyms | LY344864;LY-344864 |
Solubility | Soluble in DMSO |
Chemical Name | (R)-N-(3-(dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl)-4-fluorobenzamide |
SDF | Download SDF |
Canonical SMILES | CN([C@]1([H])CCC2=C(C3=C(N2)C=CC(NC(C4=CC=C(F)C=C4)=O)=C3)C1)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |