NURS 6630 Foundational Neuroscience

NURS 6630 Foundational Neuroscience

Foundational Neuroscience

1. Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents, including how partial and inverse agonist functionality may impact the efficacy of psychopharmacologic treatments.

Drugs possess two fundamental properties: affinity and intrinsic efficacy. Affinity refers to a drug’s capacity to attach itself to a receptor. Intrinsic efficacy refers to the ability of a drug to affect receptor activity, potentially inducing changes in cellular activity (Shiriaeva et al., 2022). The affinity and intrinsic efficacy of a drug-receptor pair are constant and distinct due to the receptor’s structure and the drug itself.  Agonists are pharmacological substances that bind to specific receptors, inducing changes in the receptor structure and triggering a physiological response (Miyachi, 2023). Antagonists or inverse agonists exhibit an opposing effect by failing to elicit a response upon binding to the receptor. A full agonist elicits its maximum response, while a partial agonist elicits only a partial or fraction of the response. A partial agonist can exhibit both agonistic and antagonistic properties due to its binding ability to specific molecules, resulting in minimal activity.

1. Compare and contrast the actions of g couple proteins and ion-gated channels.

GPCRs are a large family of receptors that utilize slower messenger systems (Hu et al., 2022). G proteins are utilized for intracellular signal transmission. Malfunctions of this receptor can lead to various disorders, as it plays a crucial role in numerous physiological functions within the human body. A distinct response is elicited when these proteins and their subunits interact with cellular proteins. G protein units are created through the binding of guanosine triphosphate. GTP is released and subsequently converted into GPD.

Ion-gated channels regulate the flow of ions across the cell membrane and play a crucial role in controlling neuronal firing (Shen et al., 2023). Upon ligand attachment, a channel is opened, facilitating the passage of specific ions. The formation of this channel occurs via the membrane-spanning region of the receptor. These channels play a crucial role in the functioning of the nervous system. Neurotransmitter messages are converted to electrical currents with the assistance of signaling mechanisms.

1. Explain how the role of epigenetics may contribute to pharmacologic action.

Epigenetics refers to changes in genetic sequence that occur in addition to the primary genetic code (Ganesan et al., 2019).  Epigenetics encompasses mechanisms that modulate gene expression without altering the underlying DNA sequence. This biological process is inherent and essential for various organism functions. However, there are instances where abnormalities in this process can arise, resulting in significant health and behavioral complications. Cancer is a primary focus of epigenetic research. Various diseases, including cancer, exhibit distinct mutations that are challenging to detect and treat effectively, potentially resulting in cancer recurrence. Understanding epigenetic variations is crucial for effective disease treatment, as solely targeting one pathway may prove ineffective due to the involvement of multiple pathways. Treatment methods are influenced by alterations in cellular function resulting from epigenetic modifications.

1. Explain how this information may impact how you prescribe medications to patients. Include a specific example of a situation or case with a patient in which the psychiatric mental health nurse practitioner must be aware of the medication’s action.

Understanding the biological mechanism and factors of a medication is crucial for PMHNPs when prescribing it to ensure effective treatment for the patient. Enhanced comprehension of brain function and dysfunction, specifically biological mechanisms, will facilitate the development of improved treatment modalities and medications. Selecting the most effective medication depends on the individual’s characteristics, family medical background, and genetic makeup (Phoenix, 2019). Cell behavior and interactions vary among individuals, leading to variations in cellular responses and, for instance, comparing the prescription of medications for depression in elderly patients versus young individuals. Another scenario involves the prescription of antipsychotic medication for pregnant women, as opposed to individuals who are not pregnant. These situations necessitate a high level of medication knowledge for PMHNPs when prescribing to diverse populations or individuals. Specific mutations in the TSH receptor lead to an increase in constitutive activity towards adenylyl cyclase. In addition to increasing the synthesis and release of thyroid hormone, activation of these receptors causes thyrocyte growth and proliferation. Modifications in these receptors may also lead to the development of malignancies concurrent with hypothyroidism.

References

Ganesan, A., Arimondo, P. B., Rots, M. G., Jeronimo, C., & Berdasco, M. (2019). The timeline of epigenetic drug discovery: from reality to dreams. Clinical Epigenetics, 11(1). https://doi.org/10.1186/s13148-019-0776-0

Hu, Y., Chen, M., Wang, M., & Li, X. (2022). Flow-mediated vasodilation through mechanosensitive G protein-coupled receptors in endothelial cells. Trends in Cardiovascular Medicine, 32(2), 61–70. https://doi.org/10.1016/j.tcm.2020.12.010

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. https://doi.org/10.3390/ijms24043940

Phoenix, B. J. (2019). The Current Psychiatric Mental Health Registered Nurse Workforce. Journal of the American Psychiatric Nurses Association, 25(1), 38–48. https://doi.org/10.1177/1078390318810417

Shen, Z., Pu, S., Cao, X., Tang, M., Wang, S., Bai, D., & Jiang, G. (2023). Bioinformatics and network pharmacology analysis of drug targets and mechanisms related to the comorbidity of epilepsy and migraine. Epilepsy Research, 189, 107066. https://doi.org/10.1016/j.eplepsyres.2022.107066

Shiriaeva, A., Park, D., Kim, G., Lee, Y., Hou, X., Jarhad, D. B., Kim, G., Yu, J., Hyun, Y. E., Kim, W., Gao, Z.-G., Jacobson, K. A., Han, G. W., Stevens, R. C., Jeong, L. S., Choi, S., & Cherezov, V. (2022). GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A_2A Adenosine Receptor. Journal of Medicinal Chemistry, 65(17), 11648–11657. https://doi.org/10.1021/acs.jmedchem.2c00462

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