874882-92-5

874882-92-5 structure
874882-92-5 structure
  • Name: Isamoltane hemifumarate
  • Chemical Name: Isamoltane hemifumarate
  • CAS Number: 874882-92-5
  • Molecular Formula: C16H22N2O2.1/2C4H4O4
  • Molecular Weight: 332.40
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2021-01-06 11:21:26
  • Modify Date: 2025-08-27 21:10:32
  • 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].

Name Isamoltane hemifumarate
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
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.

Molecular Formula C16H22N2O2.1/2C4H4O4
Molecular Weight 332.40
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