[C]PS13 Demonstrates Pharmacologically Selective and Substantial Binding to Cyclooxygenase-1 in the Human Brain.

Our laboratory recently developed [C]PS13 as a PET radioligand to selectively measure cyclooxygenase-1 (COX-1). The cyclooxygenase enzyme family converts arachidonic acid into prostaglandins and thromboxanes, which mediate inflammation. The total brain uptake of [C]PS13, which is composed of both specific binding and background uptake, can be accurately quantified with gold standard methods of compartmental modeling.

Pharmacokinetic Analysis of [F]FES PET in the Human Brain and Pituitary Gland.

Purpose: Estrogen receptors (ER) are implicated in psychiatric disorders. We assessed if ER availability in the human brain could be quantified using 16α-[F]-fluoro-17β-estradiol ([F]FES) positron emission tomography (PET).

Procedures: Seven post‑menopausal women underwent a dynamic [F]FES PET scan with arterial blood sampling.

Binding of the Dual-Action Anti-Parkinsonian Drug AG-0029 to Dopamine D and Histamine H Receptors: A PET Study in Healthy Rats.

: Parkinson's disease (PD) is a neurodegenerative disorder characterized by motor dysfunction and a diverse range of nonmotor symptoms. Functional relationships between the dopaminergic and histaminergic systems suggest that dual-action pharmaceuticals like AG-0029 (D/D agonist/H antagonist) could ameliorate both the motor and cognitive symptoms of PD. The current study aimed to demonstrate the interaction of AG-0029 with its intended targets in the mammalian brain using positron emission tomography (PET).

Pharmacokinetic Modeling of [C]GSK-189254, PET Tracer Targeting H Receptors, in Rat Brain.

The histamine H receptor has been considered as a target for the treatment of various central nervous system diseases. Positron emission tomography (PET) studies with the radiolabeled potent and selective histamine H receptor antagonist [C]GSK-189254 in rodents could be used to examine the mechanisms of action of novel therapeutic drugs or to assess changes of regional H receptor density in animal models of neurodegenerative disease. [C]GSK-189254 was intravenously administered to healthy Wistar rats ( = 10), and a 60 min dynamic PET scan was carried out.

Is cyclooxygenase-1 involved in neuroinflammation?

Purpose: Reactive microglia are an important hallmark of neuroinflammation. Reactive microglia release various inflammatory mediators, such as cytokines, chemokines, and prostaglandins, which are produced by enzymes like cyclooxygenases (COX). The inducible COX-2 subtype has been associated with inflammation, whereas the constitutively expressed COX-1 subtype is generally considered as a housekeeping enzyme.

Proton Radiography With Timepix Based Time Projection Chambers.

The development of a proton radiography system to improve the imaging of patients in proton beam therapy is described. The system comprises gridpix based time projection chambers, which are based on the Timepix chip designed by the Medipix collaboration, for tracking the protons. This type of detector was chosen to have minimal impact on the actual determination of the proton tracks by the tracking detectors.