• Describe the different characteristics of the four agonists and how each mediates distinct biological activities. Include proposed mechanisms and the receptor it is targeting.
• Identify how the P450 enzyme system plays a role in the body’s absorption, distribution, and clearance of medication.
• Scavenge the literature after describing each agonist on the spectrum for research that is based on the medications in the table below.
• Apply the medications to the appropriate agonist on the agonist spectrum in your Concept Map
Understanding the Agonist Spectrum
Agonists are substances that bind to a receptor and activate it, producing a biological response. The agonist spectrum describes the varying degrees of efficacy an agonist can have:
- Full Agonist: Produces the maximal possible response.
- Partial Agonist: Produces a submaximal response, even at full receptor occupancy.
- Inverse Agonist: Binds to the same receptor as an agonist but produces the opposite pharmacological effect.
- Antagonist: Binds to the receptor but does not activate it, preventing agonists from binding and eliciting a response. (While not an agonist, it’s vital in the spectrum).
Four Agonists and Their Characteristics
Let’s consider these four agonist types in detail:
- Full Agonist:
- Characteristics: High efficacy, produces a maximal response when bound to its receptor.
- Mechanism: Binds to the receptor, causing a conformational change that triggers a signaling cascade leading to the full biological effect.
- Receptor Target: Examples include beta-adrenergic receptors (e.g., isoproterenol), opioid mu-receptors (e.g., morphine).
Understanding the Agonist Spectrum
Agonists are substances that bind to a receptor and activate it, producing a biological response. The agonist spectrum describes the varying degrees of efficacy an agonist can have:
- Full Agonist: Produces the maximal possible response.
- Partial Agonist: Produces a submaximal response, even at full receptor occupancy.
- Inverse Agonist: Binds to the same receptor as an agonist but produces the opposite pharmacological effect.
- Antagonist: Binds to the receptor but does not activate it, preventing agonists from binding and eliciting a response. (While not an agonist, it’s vital in the spectrum).
Four Agonists and Their Characteristics
Let’s consider these four agonist types in detail:
- Full Agonist:
- Characteristics: High efficacy, produces a maximal response when bound to its receptor.
- Mechanism: Binds to the receptor, causing a conformational change that triggers a signaling cascade leading to the full biological effect.
- Receptor Target: Examples include beta-adrenergic receptors (e.g., isoproterenol), opioid mu-receptors (e.g., morphine).