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Isamoltane hemifumarate

Names

[ CAS No. ]:
874882-92-5

[ Name ]:
Isamoltane hemifumarate

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[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]

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H22N2O2.1/2C4H4O4

[ Molecular Weight ]:
332.40

Related Compounds