SCIENTIFIC POSTER
An optimised method to quantify target engagement of Orexin-1 receptors and correlation with biophase free concentration of a selective OX1 receptor antagonist in the rat brain
A key part of a Drug Discovery strategy is to ensure that compounds identified in the screening cascade are able to engage the target under investigation at relevant blood concentrations.
Receptor occupancy (RO) measurements, using methods such as in vivo/ex vivo autoradiography, have proved extremely useful in identifying novel CNS candidate compounds due to their high
translational value when used to support clinical PET studies.
Orexins are neuromodulatory peptides involved in the control of diverse physiological functions through interaction with two receptors; Orexin-1 and Orexin-2 receptors (OX1 & OX2, respectively).
Recently presented at the Society for Neuroscience 2019 conference in Chicago by our expert, Renzo Carletti, download your copy of this scientific poster now and discover more.