874882-92-5
874882-92-5 structure
- Name: Isamoltane hemifumarate
- Chemical Name: Isamoltane hemifumarate
- CAS Number: 874882-92-5
- Molecular Formula: C16H22N2O2.1/2C4H4O4
- Molecular Weight: 332.40
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2021-01-06 11:21:26
- Modify Date: 2024-01-12 18:39:58
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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].
| Name | Isamoltane hemifumarate |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
β-adrenoceptor:8.4 nM (IC50) 5-HT1B Receptor:39 nM (IC50) |
| 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]. Animal Model: Male Sprague-Dawley rats (200-300 g)[1] Dosage: 0.3, 1, 3, 10, 30 mg/kg Administration: I.p. Result: 38% reduction of 5-HTP accumulation was found with 30 mg/ kg in the striatum. Did not alter the accumulation of 5-HTP in the hippocampus. Increased 5-HT synthesis at 0.3, 1 and 3 mg/kg in cortical tissue. |
| References |
| Molecular Formula | C16H22N2O2.1/2C4H4O4 |
|---|---|
| Molecular Weight | 332.40 |