Synonyms: 4-Benzyloxy-3,5-dimethoxy-N-[(1-dimethylaminocyclopentyl)methyl]benzamide hydrochloride; N-[[1-(Dimethylamino)cyclopentyl]methyl]-3,5-dimethoxy-4-(phenylmethoxy)benzamide hydrochloride; ORG 25,543 hydrochloride; ORG 25543 hydrochloride; ORG-25543 hydrochloride
Molecular Formula: C24H32N2O4·HCl
Molecular Weight: 448.98
Linear Structural Formula: C24H32N2O4·HCl
MDL Number: MFCD23701926
Purity: >=95% (HPLC)
Storage: room temp
Biochem Physiol Actions: ORG 25543 is a brain-penetrant (free brain/plasma ratio = 0.53; 35 min post 2 or 20 mg/kg i.v. in mice), high-affinity, potent and selective glycine transporter 2 (GlyT-2; GlyT2) inhibitor (human & mouse pIC50 = 7.9/ GlyT2 vs<4 lyt1) with great selectivity over a panel of 56 receptor and channel proteins. org 25543 is more potent and selective than the brain-impermeable alx-1393 (glyt2 lyt1 pic50="7.1/5.4)" and exhibits high in vivo efficacy in a murine diabetic neuropathic pain model (ed50="0.07-0.16" mg g i.v.; emin="0.01" mg g). org 25543 is practically irreversible due to its tight-binding nature, suboptimal dosage should be applied in vivo to allow low target occupancy only and minimize acute toxicity.<>