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GRK-Biased Activation Via β2-Adrenergic Receptors in Human Skeletal Muscle
Sponsor: Morten Hostrup, PhD
Summary
This longitudinal mechanistic physiological study examines biased β2-adrenergic receptor (β2-AR) signaling in human skeletal muscle, with emphasis on G protein-coupled receptor kinase (GRK)-mediated pathways. Participants will receive daily oral dosing of the GRK-selective long-acting β2-agonist ATR-258 for 8 weeks. Muscle biopsies and physiological measurements will quantify GRK-, cAMP/PKA-, and β-arrestin-related up- and downstream signaling, fiber-type specificity, and potential receptor desensitization with repeated stimulation along with functional read-outs, tissue distribution, cardiovascular response and tolerability.
Official title: G Protein-Coupled Receptor Kinase (GRK)-Biased Signaling Via β2-Adrenergic Receptors and Downstream Activation and Its Role for Protein Synthesis-Regulating Kinases, Function and Receptor Desensitization in Human Skeletal Muscle
Key Details
Gender
MALE
Age Range
21 Years - 45 Years
Study Type
INTERVENTIONAL
Enrollment
13
Start Date
2026-02-19
Completion Date
2026-12-31
Last Updated
2026-10-14
Healthy Volunteers
Yes
Conditions
Interventions
ATR-258
Daily oral ATR-258 for 8 weeks with repeated experimental assessment days (Days 1, 15, 29, 56).
Locations (1)
University of Copenhagen, August Krogh Section for Human & Molecular Physiology
Copenhagen, Denmark