Isamoltane hemifumarate  (Synonyms: (±)-Isamoltane hemifumarate)

Isamoltane hemifumarate is a selective antagonist of 5-HT_1B receptor, with an IC₅₀ of 39 nM for inhibits the binding of [¹²⁵I]ICYP to 5-HT_1B 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].

Isamoltane exhibits 27-fold selectivity for the 5-HT_1B receptor over 5-HT_1A (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 (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.

332.40

C₁₆H₂₂N₂O₂.1/2C₄H₄O₄

874882-92-5

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

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]

  [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.  [Content Brief]