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I2PETHV - Imidazoline2 Binding Site in Healthy Volunteers

NCT02323217 · Status: COMPLETED · Phase: EARLY_PHASE1 · Type: INTERVENTIONAL · Enrollment: 20

Last updated 2021-11-15

Study results available
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Summary

The imdazoline2 binding site (I2BS) is known to reside inside astrocytes. Changes in the numbers of I2BS in post mortem tissue has implicated them in a range of psychiatric conditions such as depression and addiction, along with neurodegenerative disorders such as Alzheimer's disease and Huntington's chorea. Preclinical studies have also demonstrated functional interactions with the opioid system, where I2BS ligands have been shown to affect tolerance to morphine and alleviate some of the morphine withdrawal syndrome in rats. Recently the I2BS and I2BS ligands have been shown to have some interesting analgesic effects in different models of pain and a novel I2BS ligand, CR4056, is currently undergoing Phase II clinical trials as a novel treatment for neuropathic pain and acute non- specific pain states.

The location of I2BS on astrocytic glial cells and the possibility that they may in some way regulate glial fibrillary acidic protein have led to increased interest into the role of I2BS and I2BS ligands in conditions characterised by marked gliosis. The number of I2BS has been shown to increase in Alzheimer's disease post mortem, and it has also been suggested that I2BS may be a marker for the severity and malignancy of human glioblastomas.

The lack of suitable imaging tools for the I2BS has meant that information regarding the number and distribution of I2BS in the brain has come from preclinical species and in vitro post-mortem studies. The recent development of \[11C\]BU99008 as a suitable PET ligand to quantify I2BS in vivo, enables the direct quantification of I2BS availability and regional distribution in the living human brain. In this study the investigators plan to utilise \[11C\]BU99008 to quantify the regional brain availability of I2BS in the human brain in vivo using PET.

Conditions

  • Healthy Volunteers
  • Alzheimer Disease
  • Molecular Imaging

Interventions

RADIATION

[11C]BU99008

Baseline Scan, Test-ReTest or Dosimetry

DRUG

Idazoxan

Idazoxan block of \[11C\]BU99008

DRUG

Isocarboxazid

Isocarboxazid block of \[11C\]BU99008

Sponsors & Collaborators

Principal Investigators

  • David J Nutt, MD · Director of Centre for Neuropsychopharmacology, Imperial College London

Study Design

Allocation
NA
Purpose
BASIC_SCIENCE
Masking
NONE
Model
SINGLE_GROUP

Eligibility

Min Age
40 Years
Max Age
65 Years
Sex
MALE
Healthy Volunteers
Yes

Timeline & Regulatory

Start
2015-01-31
Primary Completion
2016-02-29
Completion
2016-07-31

Countries

  • United Kingdom

Study Locations

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Entities

Companies

Read the full study record

This page highlights key information. For complete eligibility criteria, study locations, investigator contacts, and the full protocol, visit the original record on ClinicalTrials.gov.

View NCT02323217 on ClinicalTrials.gov