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| Name | Class |
|---|---|
| Moscow State University of Medicine and Dentistry | OTHER |
| National Medical Research Center for Cardiology, Ministry of Health of Russian Federation | OTHER_GOV |
| Branch of Shemyakin-Ovchinnikov Institute of Bioorganic chemistry of RAS |
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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| smoking | Experimental | Healthy smoking volunteers |
|
| non-smoking | Experimental | Healthy non-smoking volunteers |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Formoterol | Drug | The participants will receive inhalation of formoterol 12 micrograms |
|
| Measure | Description | Time Frame |
|---|---|---|
| Change 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 | 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. | Baseline (pre-dose), 40 minutes |
| Measure | Description | Time Frame |
|---|---|---|
| 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. | Baseline (pre-dose), 60 minutes |
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Inclusion Criteria:
1 Provision of signed and dated informed consent form 2. Healthy male or female, aged 18-60 years
Exclusion Criteria:
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| Name | Role | Phone | Extension | |
|---|---|---|---|---|
| Kirill A Zykov, Prof | Contact | +79257729462 | kirillaz@inbox.ru | |
| Anna V Eremenko | Contact | +79265598031 | a_nn87@list.ru |
| Name | Affiliation | Role |
|---|---|---|
| Kirill A Zykov, Prof | Federal State Budgetary Institution, Pulmonology Scientific Research Institute | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Kirill Zykov | Recruiting | Moscow | 115682 | Russia |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 26762097 | Result | Agapova OY, Skoblov YS, Zykov KA, Rvacheva AV, Beilina VB, Masenko VP, Chazova IE. [Radioligand Method of Assessment of beta-Adrenoceptor's Activity on Human T-Lymphocytes]. Bioorg Khim. 2015 Sep-Oct;41(5):592-8. doi: 10.1134/s1068162015050027. Russian. | |
| 28064316 | Result | Agapova OY, Skoblov YS, Tkachev GA, Mironova NA, Golitsyn SP, Masenko VP, Chazova IE, Zykov KA. [Changes in the receptor activity of beta2-adrenoreceptors of human T-lymphocytes under the effect of beta2-agonists]. Mol Biol (Mosk). 2016 Nov-Dec;50(6):999-1006. doi: 10.7868/S0026898416050025. Russian. |
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There are two groups: the first group is smokers, the second group is non - smokers. The participants of both groups will receive metacholine on the first visit, formoterol 12 micrograms on the second visit, then tiotropium bromide 18 mkg on the third visit.
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| Tiotropium Bromide | Drug | The participants will receive inhalation of tiotropium bromide 18 mkg once |
|
| metacholine test | Diagnostic Test | The participants will receive inhalation of metacholine once |
|
| 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. |
| 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 | 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. | Difference of change of beta-receptor binding activity measured with modified radioligand method before and after inhalation of metacholine | Baseline (pre-dose), 40 minutes |
| Result | Smolyakova E.V., Skoblov Y.S., Skoblova N.A., Agapova O.Y., Ambat'ello L.G., Klimova A.A., Kuznetsova T.V., Masenko V.P., Nistor S.Yu., Rvacheva A.V., Chazova I.E., Zykov K.A. Specificity and Selectivity of the Modified Radioligand Method for Assessment of β1-Adrenoreceptor's Binding Activity on Human T-Lymphocytes. Russian Journal of Bioorganic Chemistry 45(3): 295-301, 2019 |
| ID | Term |
|---|---|
| D016535 | Bronchial Hyperreactivity |
| ID | Term |
|---|---|
| D001982 | Bronchial Diseases |
| D012140 | Respiratory Tract Diseases |
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| ID | Term |
|---|---|
| D000068759 | Formoterol Fumarate |
| D000069447 | Tiotropium Bromide |
| ID | Term |
|---|---|
| D004983 | Ethanolamines |
| D000605 | Amino Alcohols |
| D000438 | Alcohols |
| D009930 | Organic Chemicals |
| D000588 | Amines |
| D012602 | Scopolamine Derivatives |
| D014326 | Tropanes |
| D053961 | Azabicyclo Compounds |
| D001372 | Aza Compounds |
| D000470 | Alkaloids |
| D006571 | Heterocyclic Compounds |
| D019086 | Bridged Bicyclo Compounds, Heterocyclic |
| D006572 | Heterocyclic Compounds, Bridged-Ring |
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