Isamoltane (hemifumarate)
CAS No. : 874882-92-5
(Synonyms: (±)-Isamoltane (hemifumarate))
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| Cat. No. : | HY-19578B |
| M.Wt: | 332.40 |
| Formula: | C16H22N2O2.1/2C4H4O4 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity[1].
In Vitro: Isamoltane exhibits 27-fold selectivity for the 5-HT1B receptor over 5-HT1A (IC50=1070 nM) in rat brain membranes[1].
Isamoltane (0.01-10 μM) increases the [3H]-overflow elicited by electrical stimulation in a concentration-dependent manner in rat cortical slices[1].
In Vivo: Isamoltane (0.3-30 mg/kg; i.p) does not alter the accumulation of 5-HTP in the rat hippocampus, and increases 5-HT synthesis in cortical tissue. Isamoltane reduces 5-HTP accumulation in the striatum[1].
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