Describe the mechanism of action of beta-2 receptor agonists…

Describe the mechanism of action of beta-2 receptor agonists such as albuterol (structure shown) or salmeterol. Identify important structure-activity elements. What happens inside the cell after the agonist binds to the receptor? What kind of amino acid residues are essential in the active center of the target for activity of the beta-2 receptor agonist? Structure of beta-2 receptor agonist albuterol

A drug in development is a full agonist at the μ-(mu)opioid…

A drug in development is a full agonist at the μ-(mu)opioid receptor. You are involved in its development as an oral analgesic with reduced or no risk of addiction or dependence. You can run tests to see if the new drug can be antagonized with either a competitive or non-competitive antagonist. Draw a log-dose response curve of the full agonist alone the full agonist with a competitive antagonist the full agonist with a non-competitive antagonist the competitive antagonist alone If you were tasked to formulate the drug for oral application, describe what approaches you would take to reduce the risk of abuse? In other words, describe at least 2 approaches that can reduce the abuse risk of the drug.

You are tasked to evaluate an antibotic drug for its oral bi…

You are tasked to evaluate an antibotic drug for its oral bioavailability. Which physicochemical parameters are important to determine if a drug is feasible for oral administration? List and briefly describe optimal ranges for these parameters. Then evaluate the following structure and the provided information from SwissADME to determine if this structure has beneficial ADME properties for oral administration. Structure of antibiotic drug Physicochemical properties Formula C37H67NO13 Molecular weight 733.93 g/mol Num. heavy atoms 51 Num. arom. heavy atoms 0 Fraction Csp3 0.95 Num. rotatable bonds 7 Num. H-bond acceptors 14 Num. H-bond donors 5 Molar Refractivity 189.36 TPSA 193.91 Ų Log Po/w (XLOGP3) 3.06 Log S (ESOL) -5.86 Solubility 1.02e-03 mg/ml ; 1.39e-06 mol/l Class Moderately soluble P-gp substrate Yes CYP3A4 inhibitor No Provide as much information as possible.