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[1].

Product Specifications

CAS Number

[874882-92-5]

Product Name Alternative

(±) -Isamoltane (hemifumarate)

UNSPSC

12352005

Target

5-HT Receptor; Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/isamoltane-hemifumarate.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C16H22N2O2.1/2C4H4O4

Molecular Weight

332.40

References & Citations

[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.