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

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

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01194986

Enrollment

Registered

2010-09-03

Start date

2010-11-30

Completion date

2011-06-30

Last updated

2015-01-28

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Brain Distribution of [11C]AZ12807110 and AZD5213

Keywords

Receptor binding, Histamine H3 receptor, binding, radioligand

Brief summary

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.

Interventions

OTHER[11C]AZ12807110

Radioligand

DRUGAZD5213

Study design

Allocation

RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

BASIC_SCIENCE

Masking

SINGLE (Subject)

Eligibility

Sex/Gender

FEMALE

Age

20 Years to 45 Years

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

Design outcomes

Primary

Measure	Time frame	Description
Distribution volume (VT)	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).	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

Measure	Time frame
Vital signs (body temperature, BP and pulse)	Measured at screening, study days -1 to day 3 and at follow-up
Adverse events	Collected from Day 1 to follow-up

Countries

Sweden

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026