farampator

Farampator (CX-691;Org24448) is an AMPA receptor positive modulator.

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

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Farampator has potential in treating disorders characterised by cognitive deficits such as Alzheimer's disease and schizophrenia. CX691 attenuates a scopolamine-induced impairment of cued fear conditioning following acute administration (0.1 mg/kg p.o.) and a temporally induced deficit in novel object recognition following both acute (0.1 and 1.0 mg/kg p.o.) and sub-chronic (bi-daily for 7 days) administration (0.01, 0.03, 0.1 mg/kg p.o.). It also improves attentional set-shifting following sub-chronic administration (0.3 mg/kg p.o.)[1]. Farampator (500 mg) unequivocally improves short-term memory but appeares to impair episodic memory. Furthermore, it tends to decrease the number of switching errors in the CTMT. Drug-induced side effects (SEs) included headache, somnolence and nausea. Subjects with SEs has significantly higher plasma levels of farampator than subjects without SEs[2].

Rats: Rats are dosed acutely with CX691 (0.1, 0.3 and 1.0; 2 ml/kg; p.o.) or vehicle (1% methylcellulose; 1 ml/kg; p.o.), and microdialysate samples are collected every 30 min for 4 h post dose. At the end of each experimental day, animals are returned to their home cage and re-used in a randomised cross-over design, allowing at least 7 days drug ishout before subsequent use. After the completion of the final microdialysis experiment, animals are killed, and brains are removed and stored in formalin solution for probe placement verification[1].

[1]. Woolley ML, et al. Evaluation of the pro-cognitive effects of the AMPA receptor positive modulator, 5-(1-piperidinylcarbonyl)-2,1,3-benzoxadiazole (CX691), in the rat. Psychopharmacology (Berl). 2009 Jan;202(1-3):343-54.

[2]. Wezenberg E, et al. Acute effects of the ampakine farampator on memory and information processing in healthy elderly volunteers. Neuropsychopharmacology. 2007 Jun;32(6):1272-83.

(+)-MK 801 Maleate | CNQX | N-Methyl-D-aspartic acid | ifenprodil tartrate | D-AP5(mM/ml) | DNQX | Ro 25-6981 maleate | Flupirtine maleate | Mibampator | CX546 | Naspm | Talampanel | Centrophenoxine hydrochloride | 24-Hydroxycholesterol