GEBR-7b Inhibitor

GEBR-7b is a phosphodiesterase-4 (PDE4) inhibitor. GEBR-7b also stops or slows the hydrolysis of cAMP. It increases the level of cAMP in the hippocampus without affecting the level of Abeta.

Brullo C, Massa M, Rocca M, Rotolo C, Guariento S, Rivera D, Ricciarelli R, Fedele E, Fossa P, Bruno O. Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors. J Med Chem. 2014 Aug 28;57(16):7061-72. doi: 10.1021/jm500855w. Epub 2014 Aug 15. PubMed PMID: 25126889.
Sierksma AS, van den Hove DL, Pfau F, Philippens M, Bruno O, Fedele E, Ricciarelli R, Steinbusch HW, Vanmierlo T, Prickaerts J. Improvement of spatial memory function in APPswe/PS1dE9 mice after chronic inhibition of phosphodiesterase type 4D. Neuropharmacology. 2014 Feb;77:120-30. doi: 10.1016/j.neuropharm.2013.09.015. Epub 2013 Sep 22. PubMed PMID: 24067928.
Liu X, Guo H, Sayed MD, Lu Y, Yang T, Zhou D, Chen Z, Wang H, Wang C, Xu J. cAMP/PKA/CREB/GLT1 signaling involved in the antidepressant-like effects of phosphodiesterase 4D inhibitor (GEBR-7b) in rats. Neuropsychiatr Dis Treat. 2016 Jan 21;12:219-27. doi: 10.2147/NDT.S90960. eCollection 2016. PubMed PMID: 26855578; PubMed Central PMCID: PMC4725689.
Bruno O, Fedele E, Prickaerts J, Parker LA, Canepa E, Brullo C, Cavallero A, Gardella E, Balbi A, Domenicotti C, Bollen E, Gijselaers HJ, Vanmierlo T, Erb K, Limebeer CL, Argellati F, Marinari UM, Pronzato MA, Ricciarelli R. GEBR-7b, a novel PDE4D selective inhibitor that improves memory in rodents at non-emetic doses. Br J Pharmacol. 2011 Dec;164(8):2054-63. doi: 10.1111/j.1476-5381.2011.01524.x. PubMed PMID: 21649644; PubMed Central PMCID: PMC3246667.

Small volumes of GEBR-7b, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5756248 is an inhibitor targeting GEBR-7b.