Name | LY 393558 |
---|---|
Supplier | Tocris Bioscience |
Catalog | 5064 |
Prices | $199.00, $825.00 |
Sizes | 10 mg, 50 mg |
Function Type | Antagonist |
Cas Number | 271780-64-4 |
Chemical Name | 1-[2-[4-(6-Fluoro-1H-indol-3-yl)-3,6-dihydro-1(2H)-pyridinyl]ethyl]-3,4-dihydro-3-(1-methylethyl)-6-(methylsulfonyl)-1H-2,1,3-benzothiadiazine-2,2-dioxide |
Formula | C26H31FN4O4S2 |
Molecular Weight | 546.68 |
Purity | >97 % |
Description | Dual 5-HT 1B/1D receptor antagonist (pK B values are 9.05 and 8.98 respectively) and 5-HT re-uptake inhibitor (pIC 50 = 8.48). Potently antagonizes terminal autoreceptor activity in vitro and increases extracellular 5-HT levels above those evoked by fluoxetine (Cat. No. 0927) in vivo . Also acts as an antagonist at 5-HT 2A and 5-HT 2B receptors (pK i values are 7.29 and 7.35 respectively). |
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Mitchell SN, Greenslade RG, Cooper J. Eur J Pharmacol. 2001 Nov 30;432(1):19-27.
Pullar IA, Boot JR, Carney SL, Cohen ML, Colvin EM, Conway RG, Hardy CH, Lucaites VL, Nelson DL, Schenck KW, Tomlinson R, Wedley S. Eur J Pharmacol. 2001 Nov 30;432(1):9-17.
Morecroft I, Loughlin L, Nilsen M, Colston J, Dempsie Y, Sheward J, Harmar A, MacLean MR. J Pharmacol Exp Ther. 2005 May;313(2):539-48. Epub 2005 Jan 19.