(4R)-1-[(3-(11C)Methylpyridin-4-Yl)Methyl]-4-(3,4,5-Trifluorophenyl)Pyrrolidin-2-One

This article discusses clinical trials utilizing the drug (4R)-1-[(3-(11C)Methylpyridin-4-Yl)Methyl]-4-(3,4,5-Trifluorophenyl)Pyrrolidin-2-One, also known as [11C]UCB-J. This compound is being investigated as a radioactive tracer in Positron Emission Tomography (PET) imaging studies to measure synaptic density in the brain. The trials explore its potential in understanding various conditions, including major depressive disorder, cancer-related depression, and Alzheimer’s disease. These studies aim to provide insights into brain function and potentially improve diagnosis and treatment of these conditions.

Table of Contents

Introduction

(4R)-1-[(3-(11C)METHYLPYRIDIN-4-YL)METHYL]-4-(3,4,5-TRIFLUOROPHENYL)PYRROLIDIN-2-ONE, also known as 11C-UCB-J or [11C]UCB-J, is a radioactive tracer used in brain imaging studies[1]. This compound is designed to help researchers and doctors visualize specific aspects of brain function using a special imaging technique called Positron Emission Tomography (PET).

What is UCB-J?

UCB-J is a radiotracer, which means it’s a substance that emits a small amount of radiation that can be detected by special cameras. The “11C” in its name refers to carbon-11, a radioactive form of carbon used to label the molecule. This allows it to be tracked in the body during imaging studies.

Specifically, UCB-J is designed to bind to synaptic vesicle glycoprotein 2A (SV2A), a protein found in synapses – the connection points between brain cells[2]. By measuring how much UCB-J binds in different brain areas, researchers can estimate the density of synapses, which is an important indicator of brain health and function.

Uses in Medical Research

UCB-J is primarily used as a research tool to study various brain conditions. Some of its key applications include:

  • Alzheimer’s Disease Research: UCB-J is being used to study synaptic density in patients with Alzheimer’s disease. This can help researchers understand how the disease affects brain connections and potentially lead to new diagnostic methods or treatments[3].
  • Depression Studies: Some research is exploring the use of UCB-J to investigate synaptic changes in patients with major depressive disorder, particularly those with cancer-related depression[1].
  • Brain Inflammation Research: UCB-J is sometimes used alongside other tracers to study the relationship between inflammation, protein accumulation, and synaptic density in various brain disorders[3].

Administration and Dosage

UCB-J is administered as a solution for injection, typically given intravenously (into a vein)[2]. The dose used can vary depending on the specific study, but it’s generally in the range of 150-500 MBq (megabecquerels, a unit of radioactivity)[1][2][3].

It’s important to note that UCB-J is not a treatment or a drug in the traditional sense. It’s a diagnostic tool used in very small amounts for imaging studies and does not have a therapeutic effect.

Safety and Side Effects

As UCB-J is used in very small quantities for imaging purposes, it generally does not cause significant side effects. However, as with any medical procedure involving radiation, there are some considerations:

  • The radiation exposure from a single PET scan with UCB-J is relatively low and considered safe for research purposes.
  • People who are pregnant or breastfeeding are typically excluded from studies using UCB-J due to potential risks to the developing fetus or infant[3].
  • As with any injection, there’s a small risk of pain, bruising, or infection at the injection site.

Ongoing Research

Several clinical trials are currently underway to further explore the potential of UCB-J in various neurological and psychiatric conditions:

  • A study is investigating the use of UCB-J alongside other tracers to understand the relationship between microglial activation (a sign of brain inflammation), tau protein accumulation, and synaptic density in Alzheimer’s disease[3].
  • Another trial is using UCB-J to study synaptic changes in patients with cancer-related depression who are being treated with psilocybin, a potential new therapy for depression[1].

These ongoing studies highlight the potential of UCB-J as a valuable tool in neuroscience research, potentially leading to better understanding and treatment of various brain disorders.

Aspect Details
Compound Name (4R)-1-[(3-(11C)Methylpyridin-4-Yl)Methyl]-4-(3,4,5-Trifluorophenyl)Pyrrolidin-2-One (also known as [11C]UCB-J)
Primary Use Radiotracer for PET imaging to measure synaptic density
Conditions Studied Major Depressive Disorder, Cancer-related Depression, Alzheimer’s Disease
Administration Method Intravenous injection or infusion
Typical Dose Range 150-500 MBq
Key Research Objectives Analyze synaptic density changes, correlate with disease progression and treatment response
Potential Benefits Improved understanding of brain function, potential for better diagnosis and treatment monitoring

Ongoing Clinical Trials on (4R)-1-[(3-(11C)Methylpyridin-4-Yl)Methyl]-4-(3,4,5-Trifluorophenyl)Pyrrolidin-2-One

  • Study on the Early Effects of Ketamine and Venlafaxine for Hospitalized Patients with Severe Major Depression

    Recruiting

    3 1 1 1
    France
  • Study on Psilocybin for Treating Depression in Cancer Patients

    Not yet recruiting

    2 1 1
    Investigated diseases:
    Sweden
  • Study of microglial activation and synaptic density using [18F]-DPA-714, [18F]-Ro948, [11C]-UCB-J, and [11C]PiB PET imaging in patients with Alzheimer’s disease

    Not recruiting

    2 1 1
    Investigated diseases:
    France

Glossary

  • Synaptic density: The number of synapses (connections between nerve cells) in a given area of the brain. It is an important measure of brain health and function.
  • PET (Positron Emission Tomography): An imaging technique that uses small amounts of radioactive tracers to visualize and measure activity in different parts of the body, particularly useful for studying brain function.
  • Radiotracer: A substance containing a radioactive atom that can be detected by imaging equipment, used to study biological processes in the body.
  • Megabecquerel (MBq): A unit of measurement for radioactivity, often used to describe the dose of radioactive tracers in medical imaging.
  • Intravenous administration: The delivery of a substance directly into a vein, typically through injection or infusion.
  • Major Depressive Disorder: A mental health condition characterized by persistent feelings of sadness, hopelessness, and loss of interest in activities.
  • Alzheimer's disease: A progressive brain disorder that affects memory, thinking, and behavior, typically in older adults.
  • Microglial activation: The process by which microglia, immune cells in the brain, become active in response to injury or disease.
  • Tau pathology: Abnormal accumulation of tau protein in the brain, associated with various neurodegenerative diseases, including Alzheimer's.

References

  1. http://clinicaltrials.eu/trial/study-on-psilocybin-for-treating-depression-in-cancer-patients/
  2. http://clinicaltrials.eu/trial/study-on-the-early-effects-of-ketamine-and-venlafaxine-for-hospitalized-patients-with-severe-major-depression/
  3. http://clinicaltrials.eu/trial-id/2024-516566-11-00