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Evaluation of Histamine H3 Receptor Radioligand [11C]AZ12807110 and Histamine H3 Receptor Occupancy of AZD5213 After Oral Administration

This study has been completed.
Information provided by (Responsible Party):
AstraZeneca Identifier:
First received: September 2, 2010
Last updated: January 27, 2015
Last verified: January 2015
The purpose of this study is to investigate features of radioligand [11C]AZ12807110 and how much AZD5213 displaces radioligand from histamine receptors when given together.

Condition Intervention Phase
Brain Distribution of [11C]AZ12807110 and AZD5213
Other: [11C]AZ12807110
Drug: AZD5213
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Intervention Model: Single Group Assignment
Masking: Single Blind (Participant)
Primary Purpose: Basic Science
Official Title: An Open-label Positron Emission Tomography Study to Evaluate Use of Histamine H3 Receptor Radioligand [11C]AZ12807110 and to Determine Histamine H3 Receptor Occupancy of AZD5213 After Oral Administration to Healthy Volunteers

Resource links provided by NLM:

Further study details as provided by AstraZeneca:

Primary Outcome Measures:
  • Distribution volume (VT) [ Time Frame: Venous blood samples for determination of concentrations of AZD5213 in plasma will be taken on many occasions from pre-dose until 48 h post-dose. Single PET measurement will take maximum 2 hours. ]
  • Estimation of the plasma concentration resulting in 50% receptor occupancy (Ki, pl). [ Time Frame: Venous blood samples for determination of concentrations of AZD5213 in plasma will be taken on many occasions from pre-dose until 48 h post-dose. ]
    Each healthy volunteer in the main panel will complete 3 PET measurements using radioligand; one at baseline and 2 after treatment with AZD5213.

Secondary Outcome Measures:
  • Adverse events [ Time Frame: Collected from Day 1 to follow-up ]
  • Vital signs (body temperature, BP and pulse) [ Time Frame: Measured at screening, study days -1 to day 3 and at follow-up ]

Enrollment: 13
Study Start Date: November 2010
Study Completion Date: June 2011
Primary Completion Date: June 2011 (Final data collection date for primary outcome measure)
Arms Assigned Interventions
Experimental: Pilot panel
[11C]AZ12807110 distribution and kinetics
Other: [11C]AZ12807110
Experimental: Main panel
Histamine receptor occupancy reached by AZD5213
Other: [11C]AZ12807110
Drug: AZD5213


Ages Eligible for Study:   20 Years to 45 Years   (Adult)
Sexes Eligible for Study:   Female
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Healthy male and/or female volunteers between 20 to 45 years with suitable veins for cannulation or repeated venipuncture (pilot panel)
  • Female must be of non-child bearing potential (pilot panel)
  • BMI between 18 to 30 30 kg/m2
  • Normal MRI scan
  • Provision of signed, written and dated informed consent

Exclusion Criteria:

  • History of any clinically significant disease or disorder
  • History or presence of gastrointestinal, hepatic or renal disease
  • Prolonged QTcF >450 ms or shortened QTcF <340 ms or family history of long QT syndrome
  • History of severe allergy or hypersensitivity or ongoing allergy or hypersensitivity
  • Healthy volunteer suffers from claustrophobia
  Contacts and Locations
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Please refer to this study by its identifier: NCT01194986

Research Site
Uppsala, Sweden
Sponsors and Collaborators
Study Director: Björn Paulsson, MD AstraZeneca
Principal Investigator: Wolfgang Kühn, MD Quintiles AB, Uppsala
  More Information

Additional Information:
Publications automatically indexed to this study by Identifier (NCT Number):
Responsible Party: AstraZeneca Identifier: NCT01194986     History of Changes
Other Study ID Numbers: D3030C00003
2009-010702-11 ( EudraCT Number )
Study First Received: September 2, 2010
Last Updated: January 27, 2015

Keywords provided by AstraZeneca:
Receptor binding
Histamine H3 receptor

Additional relevant MeSH terms:
Histamine phosphate
Histamine Agonists
Histamine Agents
Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Physiological Effects of Drugs processed this record on May 22, 2017