- Differentiate between an Agonist, partial agonist and antagonist.
- describe the relationship between an agonist, partial agonist and antagonist.
- what is allosteric modulation?
Discussion Board Rubric
Criteria Ratings Points
Quality 2.5 to > 2pts
Exceeds
Expectations
Demonstrates
thorough
preparation,
synthesis and
informed opinion;
addresses topic
thoroughly;
comments/ asks
questions that
contribute to group
learning. Brings
relevant, reputable,
and appropriate
outside materials
into the discussion
(2-3 sources).
Includes citations in
the body of the post
as well as references
at the end of the
post using APA
format. Meets the
deadlines for
posting responses as
outlined by course
requirements.
2 to > 1.25 Meets
Expectations
Demonstrates
some preparation
and generally
addresses topic;
comments/asks
questions. Brings
outside materials
to class but may
lack
appropriateness
or relevance (1-2
sources). APA
formatting errors
in citations and
references. May
be inconsistent in
responses or
delayed in
response to
others.
1.25 to > 0pts
Does Not Meet
Expectations
Demonstrates
inadequate
preparation,
marginal or offtopic posts, lacks
synthesis, and
reaffirms existing
information,
minimal / no
contribution to
group learning.
Posts only within
the last 24 hours
of the week;
rarely supports
the efforts, ideas,
and work of
others. Late or no
response to
others. Posting
lacks citations and
references or
provides
inappropriate or
irrelevant
references.
2.5
Assessment,
Reasoning, and
Synthesis
2.5 to >2 pts
Exceeds
Expectations
Sound synthesis of
material and data
analysis from
assigned readings
and activities; Draws
appropriate
conclusions;
facilitates/stimulates
interaction and
discussion with
peers and instructor.
Presents new ideas
to the group.
2 to >1.25 pts
Meets
Expectations
Faulty or
incomplete
synthesis and
conclusions of
data analysis,
offers superficial
opinion;
Responses are
limited and may
not reflect
assigned weekly
reading or
activities.
Interactions and
ideas are limited
1.25 to >0 pts
Does Not Meet
Expectations
Unsatisfactory
synthesis of data
analysis and
conclusions;
content not
relevant; absence
of informed
opinion; absence
of new ideas;
responses are
weak and
disjointed.
2.5
Total 5
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PsychoPathopharmacology
Differences among agonist, partial agonists, and antagonist
Agonist, also known as full agonist, is a chemical compound that binds to the receptor site and activates it for a biological response (Miyachi, 2023). Agonist drugs such as Morphine depict endorphins’ action upon reaching opioid receptors. Hence, an agonist drug binds to a receptor and activates it to initiate a biological effect (Patinote et al., 2020). Secondly, a partial agonist can be described as a molecule that can bind to a particular receptor and activate it weakly, initiating a submaximal biological response (Masureel et al., 2018). This compound has the qualities of affinity. However, it has less intrinsic efficacy than chemical compounds acting as full agonists. The intrinsic activity of a partial agonist exceeds 0, but it is less than 1. For instance, upon reaching the μ receptor, Buprenorphine acts as a partial agonist. Lastly, an antagonist can be described as a molecule that binds to a particular receptor but does not activate it. Thus, an antagonist does not initiate a biological response. However, it covers the receptor site, preventing agonists from binding. Therefore, the antagonist mechanism of action involves blocking the biological effects of the agonist. For instance, Atropine acts as an antagonist by blocking Acetylcholine’s mechanism of action. In this case, Atropine demonstrates zero intrinsic activity.
The relationship between agonist, partial agonist, and antagonist
Agonist is a compound that can bind to a receptor and alter its state by activating it, initiating a biological response. A full agonist has the capacity to initiate the system’s maximal response capability. Secondly, a partial agonist does not achieve the system’s maximal response capability even upon occupying the receptor fully. Partial agonists demonstrate the effects of agonistic and antagonistic. A partial agonist demonstrates the effect of an antagonist if a full agonist is present. Therefore, it competes for the receptor site with the full agonist, reducing its capacity to initiate its maximum effect. Lastly, the antagonist has the ability to bind to receptors, lowering the receptor’s active conformation.
Allosteric Modulation
The allosteric modulation inhibits ligands from binding to the orthosteric binding site, decreasing their activity (Gado et al., 2022). Chemical compounds initiating this effect are negative allosteric modulators (NAMs) (Sharma et al., 2020). An allosteric modulator alters the action of the primary agonist without changing its effect on the receptor site.
References
Gado, F., Ferrisi, R., Polini, B., Mohamed, K. A., Ricardi, C., Lucarini, E., … & Manera, C. (2022). Design, synthesis, and biological activity of new CB2 receptor ligands: From orthosteric and allosteric modulators to dualsteric/bitopic ligands. Journal of Medicinal Chemistry, 65(14), 9918-9938.
Masureel, M., Zou, Y., Picard, L. P., van der Westhuizen, E., Mahoney, J. P., Rodrigues, J. P., … & Kobilka, B. K. (2018). Structural insights into binding specificity, efficacy and bias of a β2AR partial agonist. Nature chemical biology, 14(11), 1059-1066.
Miyachi, H. (2023). Structural Biology Inspired Development of a Series of Human Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Ligands: From Agonist to Antagonist. International Journal of Molecular Sciences, 24(4), 3940.
Patinote, C., Karroum, N. B., Moarbess, G., Cirnat, N., Kassab, I., Bonnet, P. A., & Deleuze-Masquéfa, C. (2020). Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes. European journal of medicinal chemistry, 193, 112238.
Sharma, R., Nakamura, M., Neupane, C., Jeon, B. H., Shin, H., Melnick, S. M., … & Park, J. B. (2020). Positive allosteric modulation of GABAA receptors by a novel antiepileptic drug cenobamate. European journal of pharmacology, 879, 173117.