The purpose of this study is to validate [11C]ORM-13070 as an alpha2C-adrenoceptor imaging
agent for human positron emission tomography (PET) studies of brain alpha2C-adrenoceptor
occupancy.
Inclusion Criteria:
- Written informed consent (IC) obtained.
- Good general health ascertained by detailed medical history, laboratory
investigations and physical examination.
- Males between 20 and 40 years of age (inclusive).
- Body mass index (BMI) between 18-28 kg/m2 inclusive (BMI = weight/height2).
- Weight 60-100 kg (inclusive).
Exclusion Criteria:
- Suspected poor compliance with the protocol or inability to communicate well with the
study personnel.
- Veins unsuitable for repeated venipuncture.
- CYP2D6 slow metabolizer or ultrarapid metabolizer genotype.
- Evidence of clinically significant cardiovascular, renal, hepatic, haematological,
gastrointestinal, pulmonary, metabolic-endocrine, neurological, urogenital or
psychiatric disease as judged by the investigator.
- Any condition requiring regular concomitant medication including herbal products or
likely to need any concomitant medication during the study.
- Susceptibility to severe allergic reactions.
- Intake of any medication that could affect the outcome of the study, within 2 weeks
prior to the tracer administration (2 months for enzyme inducing drugs like
rifampicin or carbamazepine), or less than 5 times the half-life of the medication.
- Regular consumption of more than 21 units of alcohol per week (1 unit = 4 cl spirits,
about 13 g of alcohol).
- Current use of nicotine-containing products more than 5 cigarettes or equivalent/day.
- Inability to refrain from using nicotine-containing products during the stay at the
study centre.
- Inability to refrain from consuming caffeine-containing beverages during the stay at
the study centre, e. g. propensity for headache when refraining from
caffeine-containing beverages.
- Blood donation or loss of significant amount of blood within 2 months prior to the
screening visit.
- Abnormal 12-lead electrocardiogram (ECG) finding of clinical relevance after 10
minutes rest in supine position at the screening visit, for example:
- QTc (calculated using Bazett's formula) > 450 msec,
- PR < 120 msec or > 210 msec,
- QRS < 70 msec or > 120 msec.
- Heart rate (HR) < 40 beats/minute or > 90 beats/minute after 10 minutes rest in
supine position at the screening visit.
- At the screening visit, systolic blood pressure (BP) < 90 mmHg or > 140 mmHg after 10
minutes in supine position, diastolic BP < 50 mmHg or > 90 mmHg after 10 minutes in
supine position.
- Any abnormal laboratory value, vital sign or physical examination result, which may
in the opinion of the investigator interfere with the interpretation of the test
results or cause a health risk to the subject if he takes part in the study.
- History of drug abuse or positive result in drug abuse test.
- Positive serology to human immunodeficiency virus antibodies (HIVAb), hepatitis B
surface antigen (HBsAg) or hepatitis C virus antibodies (HCVAb).
- Anatomical abnormality in brain MRI which may in the opinion of the investigator
interfere with the interpretation of the PET results.
- Any other condition that in the opinion of the investigator would interfere with the
evaluation of the results or constitute a health risk to the subject.
- Participation in another clinical drug study within 3 months prior to this study.
- Participation in a prior PET study or other medical or occupational exposure to
significant doses of ionizing radiation.
- Any contraindication to MRI of the brain.
