In Vitro Efficacy Testing Services for Sleep Apnea

We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for sleep apnea. Our service enables the detailed assessment of candidate compounds targeting key pathways implicated in sleep apnea, such as neurotransmitter signaling, G protein-coupled receptor (GPCR) activity, and inflammatory mediators. We focus on relevant targets including adrenergic, muscarinic, and other modulatory receptors involved in airway regulation and central respiratory control. Our platforms allow investigation of the molecular and cellular processes underlying airway obstruction, neuromuscular tone, and ventilatory control disruptions characteristic of sleep apnea.

Our in vitro testing services utilize a diverse range of biochemical and cell-based assays to evaluate compound efficacy, mechanism of action, and target engagement. These methods encompass receptor binding, signal transduction, enzyme activity, and ligand displacement, providing comprehensive data on drug interactions and functional outcomes. The overall purpose is to identify promising candidates and elucidate their pharmacological profiles relevant to sleep apnea.

Arrestin protease recruitment assay: Measures recruitment of arrestin proteins to activated GPCRs, important for understanding receptor desensitization and drug efficacy.

Bioluminescent assay: Employs enzyme-substrate reactions emitting light, enabling sensitive quantification of biological activities such as receptor activation or enzyme function.

Chemiluminescent assay: Detects light emitted from chemical reactions, useful for monitoring enzyme activities or ligand binding in a highly sensitive format.

Displacement of [3H]-N-methylscopolamine: Evaluates competitive binding at muscarinic receptors, critical for assessing antagonist or agonist affinities.

Displacement of [3H]-noradrenaline: Measures compound binding at adrenergic receptors, relevant for modulating sympathetic pathways implicated in sleep apnea.

ELISA assay: Uses antibody-based detection to quantify proteins or biomarkers, facilitating the measurement of inflammatory mediators or receptor expression.

Fluorescence resonance energy transfer (FRET) assay: Monitors molecular interactions or conformational changes via energy transfer between fluorophores, ideal for studying protein-protein interactions.

Fluorescent assay: Utilizes fluorescence-based detection to measure enzymatic activity, receptor binding, or cellular responses with high sensitivity.

Homogeneous Time Resolved Fluorescence (HTRF) assay: Integrates fluorescence resonance energy transfer with time-resolved detection for precise quantification of biomolecular interactions.

Luciferine/luciferase assay: Detects bioluminescence generated by luciferase enzymes, providing a sensitive readout for cellular signaling or gene expression.

cAMP accumulation assay: Measures intracellular cyclic AMP levels, serving as a key indicator of GPCR activation and downstream signaling relevant to respiratory control.

We quantify key pharmacological parameters such as potency, efficacy, and binding affinity to provide a comprehensive understanding of compound activity. These parameters are essential for comparing candidate drugs, optimizing lead compounds, and predicting in vivo responses. Accurate measurement ensures selection of the most promising treatments for further development.

EC-50: The concentration of a compound that produces 50% of its maximal effect; indicates drug potency and is crucial for dose selection.

IC-50: The concentration required to inhibit a specific biological or biochemical function by 50%; important for evaluating antagonist or inhibitor efficacy.

Ki: The equilibrium dissociation constant for inhibitor binding; reflects binding affinity and informs on selectivity and specificity.

pEC-50: The negative logarithm of the EC-50 value; provides a more convenient scale for comparing potencies across compounds.

pIC-50: The negative logarithm of the IC-50 value; facilitates direct comparison of inhibitor strengths in a standardized format.

pKi: The negative logarithm of the Ki value; allows straightforward affinity ranking of compounds targeting the same site.

Recommended In Vitro Efficacy Tests

Glucagon Like Peptide 1 Receptor

Our Glucagon Like Peptide 1 Receptor (GLP-1R) testing service supports sleep apnea drug development by assessing receptor involvement in respiratory regulation. This testing is vital for identifying and characterizing compounds that modulate GLP-1R activity. We utilize advanced methods, including fluorescent, chemiluminescent, and bioluminescent assays (e.g., HTRF, FRET, luciferase, cAMP, ELISA), measuring key parameters such as Ki, EC-50, and IC-50 to ensure robust pharmacological profiling.

Hypocretin Receptor 1

The Hypocretin Receptor 1 (HCRTR1) is crucial in regulating wakefulness and is implicated in sleep apnea pathophysiology. Testing HCRTR1 activity is vital for developing targeted sleep apnea therapies. Our service utilizes Homogeneous Time Resolved Fluorescence (HTRF) and fluorescent assays to assess drug-receptor interactions, providing key pharmacological parameters including pEC-50, EC-50, and IC-50 for accurate efficacy and potency profiling of candidate compounds.

Hypocretin Receptor 2

Our Hypocretin Receptor 2 testing service supports sleep apnea drug development by evaluating compounds that target this receptor, which regulates wakefulness and respiratory stability. Using advanced Homogeneous Time Resolved Fluorescence (HTRF) and fluorescent assays, we accurately determine key pharmacological parameters: pEC-50, EC-50, and IC-50. This testing is essential for identifying and optimizing therapeutic candidates that modulate Hypocretin Receptor 2 activity for sleep apnea treatment.

Muscarinic Acetylcholine Receptor (Machr) (Nonspecified Subtype)

The Muscarinic Acetylcholine Receptor (Machr) is implicated in airway muscle tone regulation, making it a relevant target in sleep apnea research. Our testing service evaluates compound interactions with Machr (nonspecified subtype) using [3H]-N-methylscopolamine displacement assays. This approach determines binding affinity via pIC₅₀ and pKᵢ parameters, providing essential data for developing effective sleep apnea therapeutics. Accurate receptor profiling ensures candidate drug specificity and efficacy.

Purinergic Receptor P2X 3

Our Purinergic Receptor P2X3 testing service supports sleep apnea drug development by evaluating compounds targeting P2X3, a receptor implicated in sensory signaling and airway reflexes linked to apnea events. Using a sensitive fluorescent assay, we determine compound potency via IC50 values, enabling precise assessment of inhibitory effects. This testing is crucial for identifying promising therapeutics that modulate P2X3 activity to alleviate sleep apnea symptoms.

Solute Carrier Family 6 Member 2

Solute Carrier Family 6 Member 2 (SLC6A2) regulates noradrenaline reuptake, influencing arousal pathways implicated in sleep apnea. Our testing service enables drug screening by assessing compound effects via fluorescent assays and [3H]-noradrenaline displacement. Determination of IC-50 values provides quantitative insights into inhibitor potency, supporting the development of novel sleep apnea therapeutics targeting SLC6A2-mediated neurotransmission.