First-in-human evaluation of 18F-PF-06445974, a PET radioligand that preferentially labels phosphodiesterase-4B

Y Wakabayashi, P Stenkrona, R Arakawa… - Journal of Nuclear …, 2022 - Soc Nuclear Med
Phosphodiesterase-4 (PDE4), which metabolizes the second messenger cyclic adenosine
monophosphate (cAMP), has 4 isozymes: PDE4A, PDE4B, PDE4C, and PDE4D. PDE4B …

Preclinical evaluation of 18F-JNJ41510417 as a radioligand for PET imaging of phosphodiesterase-10A in the brain

S Celen, M Koole, M De Angelis, I Sannen… - Journal of nuclear …, 2010 - Soc Nuclear Med
Phosphodiesterases are enzymes that inactivate the intracellular second messengers 3′,
5′-cyclic adenosine-monophosphate and/or cyclic guanosine-monophosphate. Of all 11 …

Preclinical evaluation of 18F-PF-05270430, a novel PET radioligand for the phosphodiesterase 2A enzyme

L Chen, N Nabulsi, M Naganawa… - Journal of Nuclear …, 2016 - Soc Nuclear Med
The enzyme phosphodiesterase 2A (PF-05270430) is a potential target for development of
novel therapeutic agents for the treatment of cognitive impairments. The goal of the present …

In vivo assessment and dosimetry of 2 novel PDE10A PET radiotracers in humans: 18F-MNI-659 and 18F-MNI-654

O Barret, D Thomae, A Tavares, D Alagille… - Journal of Nuclear …, 2014 - Soc Nuclear Med
Phosphodiesterase (PDE) 10A is an enzyme involved in the regulation of cyclic adenosine
monophosphate and cyclic guanosine monophosphate and is highly expressed in medium …

Characterization of the binding properties of T-773 as a PET radioligand for phosphodiesterase 10A

A Harada, K Suzuki, S Miura, T Hasui… - Nuclear Medicine and …, 2015 - Elsevier
Abstract Introduction Phosphodiesterase 10A (PDE10A) is a dual-substrate PDE that
hydrolyzes both cAMP and cGMP and is selectively expressed in striatal medium spiny …

Robust Quantification of Phosphodiesterase-4D in Monkey Brain with PET and 11C-Labeled Radioligands That Avoid Radiometabolite Contamination

M Jiang, S Tang, MD Jenkins, AC Lee… - Journal of Nuclear …, 2024 - Soc Nuclear Med
Phosphodiesterase-4D (PDE4D) has emerged as a significant target for treating
neuropsychiatric disorders, but no PET radioligand currently exists for robustly quantifying …

Discovery and development of 11C-Lu AE92686 as a radioligand for PET imaging of phosphodiesterase10A in the brain

J Kehler, JP Kilburn, S Estrada… - Journal of Nuclear …, 2014 - Soc Nuclear Med
Phosphodiesterase 10A (PDE10A) plays a key role in the regulation of brain striatal
signaling, and several pharmaceutical companies currently investigate PDE10A inhibitors in …

Phosphodiesterase 10A PET radioligand development program: from pig to human

C Plisson, D Weinzimmer, S Jakobsen… - Journal of Nuclear …, 2014 - Soc Nuclear Med
Four novel phosphodiesterase 10A (PDE10A) PET tracers have been synthesized,
characterized in preclinical studies, and compared with the previously reported 11C-MP-10 …

Evaluation of a novel PDE10A PET radioligand, [11C]T‐773, in nonhuman primates: Brain and whole body PET and brain autoradiography

A Takano, V Stepanov, B Gulyás, R Nakao, N Amini… - Synapse, 2015 - Wiley Online Library
ABSTRACT Phosphodiesterase 10A (PDE10A) is considered to be a key target for the
treatment of several neuropsychiatric diseases. The characteristics of [11C] T‐773, a novel …

First-in-human assessment of the novel PDE2A PET radiotracer 18F-PF-05270430

M Naganawa, RN Waterhouse, N Nabulsi… - Journal of Nuclear …, 2016 - Soc Nuclear Med
This was a first-in-human study of the novel phosphodiesterase-2A (PDE2A) PET ligand 18F-
PF-05270430. The primary goals were to determine the appropriate tracer kinetic model to …