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

Isamoltane hemifumarate 

Cat. No.: HY-19578B
Handling Instructions

Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM. It is also a beta-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.

For research use only. We do not sell to patients.

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. It is also a beta-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity[1].

IC50 & Target[1]

5-HT1B Receptor

39 nM (IC50)

beta-adrenoceptor

8.4 nM (IC50)

In Vitro

Isamoltane exhibits 27-fold selectivity for the 5-HT1B receptor over 5-HT1A (IC50=1070 nM)[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]

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Storage

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

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Keywords:

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

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Isamoltane hemifumarate
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