Preclinical Evaluation of [¹¹C]ORM-13070 for α2C Receptor PET Imaging

Validating a selective PET ligand to measure α2C receptor occupancy in non-human primate brain.

Publication Title: Preclinical in vitro and in vivo evaluation of [11C]ORM-13070 as PET ligand for alpha-2C adrenergic receptor occupancy using PET imaging in non-human primates

Authors: Isabel Piel, Cristian C Constantinescu, David de la Puente Bethencourt, David R Bonsall, Eugenii A Rabiner, Kenneth R Zasadny, Amy Llopis Amenta , Lisa A Wells, Thorsten Poethko, Wolfgang Prange, and Martina Delbeck

This study characterizes [¹¹C]ORM-13070 as a PET radioligand targeting the α2C adrenergic receptor, a receptor implicated in sleep regulation, mood, and cognitive function. Through in vitro human tissue assays and in vivo non-human primate imaging, the authors demonstrate high selectivity, reversible binding, and dose-dependent occupancy in response to a therapeutic antagonist (BAY 292). These results provide a strong foundation for clinical PET studies evaluating α2C-targeted drugs.

Why Read this Publication:

• Demonstrates high specific binding and strong receptor selectivity.
• Shows dose-dependent target engagement in NHP PET imaging.
• Establishes the EC50 for BAY 292 using occupancy modeling.
• Provides translational evidence supporting CNS penetration and pharmacology.
• Enables future clinical PET studies for α2C-modulating therapeutics.

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