Isamoltane hemifumarate
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.
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- CAS. Nr.: 874882-92-5
- Formel: C16H22N2O2.1/2C4H4O4
- Molecular Weight:332.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (200-300 g)[1]
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Dosage:0.3, 1, 3, 10, 30 mg/kg
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Administration:I.p.
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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.
Chemical Information
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CAS. Nr. 874882-92-5
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Molecular Weight 332.40
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Formel C16H22N2O2.1/2C4H4O4
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SMILES
OC(COC1=CC=CC=C1N2C=CC=C2)CNC(C)C.O=C(O)/C=C/C(O)=O.[1/2]
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Synonyms
(±)-Isamoltane hemifumarate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.
Reinheit & Dokumentation
Verweise
[1]. Waldmeier PC, et, al. Interactions of isamoltane (CGP 361A), an anxiolytic phenoxypropanolamine derivative, with 5-HT1 receptor subtypes in the rat brain. Naunyn Schmiedebergs Arch Pharmacol. 1988 Jun; 337(6): 609-20. [Content Brief]
[2]. Rényi L, et, al. Biochemical and behavioural effects of isamoltane, a beta-adrenoceptor antagonist with affinity for the 5-HT1B receptor of rat brain. Naunyn Schmiedebergs Arch Pharmacol. 1991 Jan;343(1):1-6. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Isamoltane hemifumarate Related Classifications
HY-19578B Related Classifications
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