Ace Therapeutics offers specialized services for psychiatric research, including radioligand binding assays, receptor occupancy studies, and high-resolution autoradiography. Our platform supports quantitative in vitro, ex vivo, and in vivo imaging using tritium (³H), carbon-14 (¹⁴C), and iodine-125 (¹²⁵I) isotopes to provide precise receptor mapping and occupancy data. Ultimately, we help our global customers accelerate psychiatric research and the development of novel antipsychotic therapies.

Introduction to Autoradiography in Psychiatry

Radiographic autoradiography is a well-established method for measuring metabolic changes, receptor activation, and GPCR signaling in response to compound stimuli in brain tissue. Non-invasive imaging methods are widely used to study metabolic changes and alterations in ligand-receptor signaling in the brain as part of the progression of psychiatric disorders and in response to therapeutic interventions via small molecules or biological agents.

Fig. 1 Representative scheme of the biodistribution study with the digital autoradiographic system. (Urbano N, et al., 2021)

Autoradiography Services

Ace Therapeutics provides a comprehensive assessment of the pathophysiology of psychiatric disorders and data on the mechanism of action of therapeutic compounds through radiographic autoradiography combined with behavioral readouts. Our approach uses read-time imaging with radioisotopes and generates quantitative data several hours after scanning the sample. We use cell membranes, live cells, human tissue, and animal tissue.

• Functional GPCR Activation Assay

We measure the activation of the studied GPCRs by measuring the amount of radiolabeled GTP bound to the cell membrane. Quantitative measurements of GPCR activation and inhibition of protein recruitment can be accurately determined using our analysis system. We are committed to the rational use of animals to model GPCR function in psychiatric disorders to help you identify new therapeutic targets for psychiatric disorders and predict targeted side effects.

• Imaging Services of Cerebral Glucose Metabolism

Our ¹⁸F-FDG radiographic autoradiography method allows the detection of changes in glucose metabolism in the early stages of mental illness. We can provide high resolution images and allow absolute quantification of local concentrations of tracer radioactivity in the brain. We are committed to providing you with landmark biomarkers associated with psychiatric disorders that characterize pathophysiological mechanisms and clinical correlates throughout the brain by using region-of-interest or voxel-based brain mapping.

• In Vivo and Ex Vivo Receptor Occupancy Assay

We use both in vivo and ex vivo modalities to measure drug receptor occupancy. We can provide custom-developed receptor occupancy analysis based on customer-defined parameters to determine the binding of anti-psychotic drugs to their specific targets. We are committed to improving anti-psychotic drug discovery lead optimization process protocols by measuring receptor occupancy at defined target engagement levels.

Technical Highlights

Multi-isotope Capability

³H, ¹⁴C, and ¹²⁵I for receptor autoradiography, in situ hybridization, or metabolic mapping.

High-resolution Phosphor Imaging

Advanced digital autoradiography system supporting rapid, high-sensitivity, wide dynamic range quantitative autoradiography detection.

Receptor Occupancy Study Designs

Customizable protocols: single/multiple dose, time-course, PK/RO relationship, ED50 determination, and competition with unlabeled drug.

What Can We Help You Achieve in Psychiatry with Autoradiography ?

• Advancing Rational Drug Design for New Therapies for Neuropsychiatric Disorders from Migraine to Schizophrenia and Depression
• Investigating biased agonism in mu-opioid receptors (MOR)
• Assessing the biodistribution and target engagement of antipsychotics in animal brain
• Analyzing binding sites associated with adverse side effects of antipsychotic drugs
• Better understand the pharmacokinetic and pharmacodynamic relationships (PK/PD) of drug candidates
• Identifying the neurobiological basis of cognitive dysfunction associated with psychiatric disorders

Ace Therapeutics uses gold-standard radiometric methods for maximum sensitivity and robustness, as well as label-free kinetic affinity techniques. Whether you are developing small molecules, antibodies, cells, or gene therapies for anti-psychiatric disorders, you can use our services to accelerate your program and drive translation from in vitro biology to the clinic. Our experienced neuroscientists are ready to support you, so please feel free to make an inquiry.

Reference

1. Urbano N, et al. Novel Biological and Molecular Characterization in Radiopharmaceutical Preclinical Design. J Clin Med. 2021, 10(21):4850.