Drug intelligence / Profile preview

SKF 97541

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Not Applicable (used In Research; Most Common Is In Vitro, Ex Vivo, Or Injection In Animal Studies)
01

Overview

SKF 97541 is a highly potent small molecule agonist of the GABA-B receptor (gamma-aminobutyric acid type B receptor) with an EC50 of approximately 50 nM for receptor activation[1][3][5][10]. It is at least ten times more active than baclofen as a GABA-B agonist[4][10]. SKF 97541 is also an antagonist at the GABA-A-rho (also referred to as GABAA-ρ) receptor[1][4][9]. The compound is blood-brain barrier permeable and depresses striatal synaptic potentials and hyperpolarizes nigral and septal neurons[1][3][5][7]. In animal models, it shows antidepressant and sedative effects and has been used in research trials investigating neurological and psychiatric indications such as depression and drug addiction[1][3][5][7][9][10]. SKF 97541 is a synthetic organic molecule developed for research use[8].

Other names
3-aminopropyl-methylphosphinic acid3-Aminopropyl(methyl)phosphinic acid
02

Targets

GABRR (GABA-A receptor subunit rho)GABA-B (Gamma-aminobutyric acid receptor type B)

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