PSEM 89S TFA

PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

PSEM 89S (10 or 30μM) activates layer 2/3 cortical neurons expressing (Pharmacologically Selective Actuator Module) PSAML141F,Y115F-5HT3 high conductance (HC)[1]. PSEM 89S (10 μM) reversibly silenced transfected neurons by reducing cellular input resistance[1].

PSEM 89S strongly reduces photostimulation-evoked feeding in mice expressing PSAML141F,Y115F- glycine receptor (GlyR) (30 mg/kg) but not in mice expressing only channelrhodopsin-2 (ChR2) (50 mg/kg)[1]. PSEM 89S (30 mg/kg) shows good brain penetrance in mice after minimally invasive intraperitoneal administration[1]. Animal Model: Male Agrp-cre mice (3-6 weeks)[1] Dosage: 30 mg/kg Administration: I.p. administration Result: Almost completely suppressed fos (a marker of neuron activation) in ChR2-expressing neurons. Animal Model: C57BL/6 mice[1] Dosage: 30 mg/kg (Pharmacokinetic Analysis) Administration: I.p. administration Result: Rised rapidly in serum and brain, and was mostly cleared from both compartments in 1 h.

[1]. Christopher JM, et, al. Chemical and genetic engineering of selective ion channel-ligand interactions. Science. 2011 Sep 2; 333(6047): 1292-6.