Interventional open-labeled study in parallel groups is aimed to evaluate changes of beta receptors in healthy volunteers under the influence of inhaled metacholine, long-acting anticholinergics and beta-agonists using modified radioligand method.
Long-acting beta2-agonists and anticholinergics are main drugs in therapy of chronic obstructive pulmonary disease . Beta-agonists exert their bronchodilatory effects via β2 adrenoceptors located on airway smooth muscle cells. Anticholinergics block mainly M3-cholinoreceptors located in the airways, thus inhibiting bronchoconstriction. Metacholine blocks M2-cholinoreceptors thus inducing bronchoconstriction. It is known, that muscarine and beta-receptors interact with each other, but the detailed mechanism is unknown. For evaluating the binding activity of beta-receptors after inhalation of these drugs the modified radioligand method was used.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
HEALTH_SERVICES_RESEARCH
Masking
NONE
Enrollment
20
The participants will receive inhalation of formoterol 12 micrograms
The participants will receive inhalation of tiotropium bromide 18 mkg once
The participants will receive inhalation of metacholine once
Kirill Zykov
Moscow, Russia
RECRUITINGChange from baseline beta-receptor binding activity at 60 min after the inhalation of formoterol or tiotropium.
Beta-receptor binding activity will be measured with modified radioligand method before and after 60 min after the inhalation of formoterol or tiotropium
Time frame: Baseline (pre-dose), 60 minutes
Change from baseline beta-receptor binding activity at 40 min after the challenge test with metacholine.
Beta-receptor binding activity will be measured with modified radioligand method before and after 40 min after the challenge test with metacholine.
Time frame: Baseline (pre-dose), 40 minutes
Comparison of beta-receptor binding activity measured with modified radioligand after formoterol and tiotropium.
Difference of change of beta-receptor binding activity measured with modified radioligand method before and after 60 min after the inhalation of formoterol and tiotropium.
Time frame: Baseline (pre-dose), 60 minutes
Comparison of beta-receptor binding activity measured with modified radioligand method after formoterol or tiotropium in smokers and non-smokers.
Difference of change of beta-receptor binding activity measured with modified radioligand method before and after 60 min after the inhalation of formoterol or tiotropium in smokers and non-smokers.
Time frame: Baseline (pre-dose), 60 minutes
Comparison of beta-receptor binding activity measured with modified radioligand after metacholine
Difference of change of beta-receptor binding activity measured with modified radioligand method before and after inhalation of metacholine
Time frame: Baseline (pre-dose), 40 minutes
Comparison of beta-receptor binding activity measured with modified radioligand method after inhalation of metacholine in smokers and non-smokers.
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Difference of change of beta-receptor binding activity measured with modified radioligand method before and after inhalation of metacholine
Time frame: Baseline (pre-dose), 40 minutes