[11C]Yohimbine PET Study of alpha2-AR

NCT03520543 | Completed Phase 1 DMC

• 2 other identifiers: 69HCL17_01962018-000380-82
• Study Type: interventional
• Target: 16
• Locations: 1 country
• Sites: 1

Brief Summary

The main purpose of this study is to model tissue specific kinetics of \[11C\]Yohimbine in healthy male participants by positron emission tomography (PET) and the appropriate arterial input function (part A) ; to determine the reproducibility of measures (classical test-retest study, part B1) and to measure the blocking of \[11C\]Yohimbine uptake in the brain following single oral dose administration of clonidine (part B2).

Conditions

Healthy Controls

Keywords

PET imaging; Noradrenaline; Radiotracer

Outcome Measures

Primary Outcomes (1)

• Binding potentials

  Binding potentials are calculated using compartmental modelling techniques

  180 minutes

Secondary Outcomes (1)

• Number of participants with adverse events as a measure of safety and tolerability

  Up to 7 days after part B

Study Arms (2)

Part A : Imput function

EXPERIMENTAL

Compartmental model of the volume of distribution of \[11C\]Yohimbine in Brain by PET

Drug: [11C]Yohimbine

Part B : validity of the measure

EXPERIMENTAL

Part B1 : Test Retest Variability in the distribution of \[11C\]Yohimbine Part B2 : Percentage of alpha2-adrenergic receptor occupancy

Drug: [11C]Yohimbine (Part B1) and [11C]Yohimbine + clonidine (Part B2)

Interventions

[11C]Yohimbine DRUG

Each subject will receive an intravenous (IV) bolus injection of \[11C\]Yohimbine at a dose of 370 MegaBecquerel (MBq) ± 10% with concomitant arterial blood sampling. The distribution of \[11C\]Yohimbine in brain will be measured by dynamic PET scans obtained from the time of injection for up to 90 minutes along with measurement of the tracer input function with arterial samples for intact tracer and metabolites to establish the total and regional compartmental kinetics of \[11C\]Yohimbine.

Part A : Imput function

[11C]Yohimbine (Part B1) and [11C]Yohimbine + clonidine (Part B2) DRUG

Part B1 : Test Retest Variability will be assessed on percent difference in the binding potential following \[11C\]Yohimbine PET scan (IV bolus injection of \[11C\]Yohimbine at a dose of 370 MBq ± 10%) obtained at least 1 week after \[11C\]Yohimbine PET scan of part A. Part B2 : Occupancy of alpha2-adrenergic receptors in brain by clonidine will be evaluated by comparing the binding potential of \[11C\]Yohimbine (IV bolus injection of \[11C\]Yohimbine at a dose of 370 MBq ± 10%) after single oral dose of clonidine (0,15mg) to the binding potential of \[11C\]Yohimbine obtained at baseline (part A).

Part B : validity of the measure

Eligibility Criteria

• Age: 20 Years - 35 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male volunteers
• Age between 20 years and 35 years
• Weight between 50kg and 90kg
• Without neurologic or psychiatric history
• Without head trauma history including loss of consciousness superior to 30 minutes.
• Affiliated to a social security or similar scheme
• Not subject to any legal protection measures
• Participant must have signed an informed consent document indicating that they understand the purpose of, and procedures required for, the study and are willing to participate in the study and comply with the study procedures and restrictions

You may not qualify if:

• Allen test (assessing the arterial blood flow to the hand) indicating abnormal blood supply to the hand
• Subject with orthostatic hypotension
• Subject with alcohol or substance abuses history
• Subject with somatic drug therapies
• MRI contraindications (implanted or embedded metal objects in the head or body)
• PET contraindications
• Clonidine contraindications
• Exposed to 1 millisievert or more of ionizing radiation in the year before the start of this study
• Subject unable to sign written consent for participation in the study

Sponsors & Collaborators

• Hospices Civils de Lyon: lead

Study Sites (1)

Service de Neurologie C - Hôpital Neurologique et Neurochirurgical Pierre Wertheimer, GHE

Bron, 69500, France

Location

Related Publications (1)

• Laurencin C, Lancelot S, Merida I, Costes N, Redoute J, Le Bars D, Boulinguez P, Ballanger B. Distribution of alpha2-Adrenergic Receptors in the Living Human Brain Using [11C]yohimbine PET. Biomolecules. 2023 May 15;13(5):843. doi: 10.3390/biom13050843.

  PMID: 37238713 RESULT

MeSH Terms

Interventions

Clonidine

Intervention Hierarchy (Ancestors)

Imidazolines; Imidazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Chloe LAURENCIN, MD

  Service de neurologie C

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: PARALLEL
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: April 26, 2018
• First Posted: May 9, 2018
• Study Start: May 21, 2018
• Primary Completion: July 21, 2018
• Study Completion: January 21, 2019
• Last Updated: September 12, 2025

Record last verified: 2020-02

Locations

FR (1)