1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Adrenergic Receptor
  3. Isamoltane hemifumarate

Isamoltane hemifumarate 

目录号: HY-19578B
产品使用指南

Isamoltane hemifumarate 是一种选择性的 5-HT1B 受体拮抗剂,抑制 [125I]ICYP 与大鼠脑膜中 5-HT1B 识别位点结合的 IC50 值为 39 nM。Isamoltane hemifumarate 也是一种 β- 肾上腺素受体配体,IC50 值为 8.4 nM。Isamoltane hemifumarate 具有抗焦虑活性。

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Isamoltane hemifumarate Chemical Structure

Isamoltane hemifumarate Chemical Structure

CAS No. : 874882-92-5

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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].

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].

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.
Molecular Weight

332.40

Formula

C₁₆H₂₂N₂O₂.₁/₂C₄H₄O₄

CAS No.

874882-92-5

SMILES

OC(COC1=CC=CC=C1N2C=CC=C2)CNC(C)C.O=C(O)/C=C/C(O)=O.[1/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Isamoltane hemifumarate5-HT ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptor5-HT1Bbeta-adrenoceptoranxiolyticInhibitorinhibitorinhibit

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Isamoltane hemifumarate
目录号:
HY-19578B
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