Concept map exploring the four agonists on the agonist spectrum
submit a concept map exploring the four agonists on the agonist spectrum (agonist, partial agonist, antagonist, and inverse agonist) in which you:
• Describe the different characteristics of the four agonists and how each mediates distinct biological activities. Include proposed mechanisms and the receptor it is targeting.
• 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.
Medications
Oxycodone
Brexpiprazole
Haloperidol
Naloxone
Aripiprazole
Amphetamine
Risperidone
Pimavanserin
Sample Solution
Agonist Spectrum Concept Map
Central Idea: Agonists and antagonists interact with receptors to produce different biological effects.
Main Branches:
- Agonist: Binds to a receptor and initiates a cellular response.
- Full Agonist: Produces the maximum possible response from the receptor. (e.g., Oxycodone)
- Mechanism: Mimics the natural ligand, causing a conformational change that activates the G protein signaling pathway.
- Receptor Target: Varies depending on the agonist (Oxycodone targets mu-opioid receptors)
- Partial Agonist: Produces a submaximal response compared to a full agonist. (e.g., Brexpiprazole)
- Mechanism: Binds to the receptor but only partially activates the G protein pathway.
- Receptor Target: Varies depending on the agonist (Brexpiprazole targets dopamine D2 and serotonin 5-HT1A receptors)
- Full Agonist: Produces the maximum possible response from the receptor. (e.g., Oxycodone)
- Antagonist: Binds to a receptor but does not activate it, blocking the effects of agonists. (e.g., Haloperidol)
- Competitive Antagonist: Competes with the agonist for binding to the receptor. (e.g., Haloperidol)
- Mechanism: Binds to the receptor without causing a conformational change, preventing agonist binding.
- Receptor Target: Varies depending on the antagonist (Haloperidol targets dopamine D2 receptors)
- Noncompetitive Antagonist: Binds to a different site on the receptor, altering its shape and preventing agonist activation. (e.g., Naloxone)
- Mechanism: Binds allosterically, changing the receptor's conformation and preventing agonist effect.
- Receptor Target: Varies depending on the antagonist (Naloxone targets mu-opioid receptors)
- Competitive Antagonist: Competes with the agonist for binding to the receptor. (e.g., Haloperidol)
- Inverse Agonist: Binds to a receptor and inherently reduces its basal activity below its resting state. (e.g., Pimavanserin) * Mechanism: Binds to the receptor and induces a conformational change that decreases basal activity. * Receptor Target: Varies depending on the inverse agonist (Pimavanserin targets serotonin 5-HT2A receptors)
- Full Agonist: Oxycodone (mu-opioid receptor agonist - pain medication)
- Partial Agonist: Brexpiprazole (dopamine D2 and serotonin 5-HT1A partial agonist - antipsychotic)
- Competitive Antagonist: Haloperidol (dopamine D2 receptor antagonist - antipsychotic)
- Noncompetitive Antagonist: Naloxone (mu-opioid receptor antagonist - opioid overdose reversal)
- Atypical Antipsychotic (Mechanism not fully understood):
- Aripiprazole (possibly a partial agonist at dopamine D2 and serotonin 5-HT1A receptors)
- Risperidone (possibly a partial agonist at dopamine D2 and serotonin 5-HT2A receptors)
- The specific effects of each medication depend on the receptor it targets and the overall balance of agonist and antagonist activity at that receptor.
- The concept map provides a simplified overview. Real-world interactions between drugs and receptors can be more complex.
- Research the specific mechanisms of action for Aripiprazole and Risperidone.
- Explore the effects of different agonist efficacies (full vs. partial) on cellular signaling pathways.