2. 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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Isamoltane hemifumarate Chemical Structure

Isamoltane hemifumarate Chemical Structure

CAS No. : 874882-92-5

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Isamoltane hemifumarate Related Antibodies

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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].

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.

Isamoltane hemifumarate Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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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Purity & Documentation
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Keywords:

Isamoltane hemifumarate874882-92-5Inhibitorinhibitorinhibit

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