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Posted: September 8th, 2022
Psychopharmacologic Approaches to Treatment of Psychopathology
Antagonists may bind to receptors that can prevent the endogenous neurotransmitters from working or a medication that utilizes the same receptors from working or both to a lesser degree depending on the action .
An example can include a medication that binds to the same dopamine receptor sites that normally would have been bound by dopamine, but instead of activating the dopamine receptor sites like the dopamine would, it fails to activate it. The end result is that there will be less dopamine available in the synapse (Stahl, 2013).
Stahl discusses a perfect example and I appreciate any examples you may bring up as a continuation for this topic. Any research, discussions or any posts would be great!
All references require creditable sources, nothing less than 5 years. References require doi or http
Psychopharmacologic Approaches to Treatment of Psychopathology
Antagonists are the receptor ligands that bind to a receptor, thereby blocking it, which leads to the dampening of a biological response. These antagonists include blockers such as the; calcium channel, beta, and alpha-blockers. The binding disrupts the function and interaction of agonists at the receptors following the lack of efficacy for their cognate receptors. Despite the lack of efficacy, antagonists are associated with a measure of affinity. By binding to the allosteric site of the receptor, the antagonists manage to mediate their effects, thereby creating a reversible or an irreversible activity depending on the duration in which the complex is bound (Wang et al., 2017). In most cases, the drug antagonists acquire their potency through a competition with the substrates or the endogenous ligands.
Antagonists are not characterized by efficacy, considering that they are unable to activate a receptor, but they inhibit the functionality of the inverse agonists. To measure the range of concentration based on its ability, a dose-response curve is used. This is achieved by reversing the activity of an agonist. On the other hand, antagonists are characterized by the affinity that determines the duration of inhibition. Such a level of affinity is determined using Schild regression or the Cheng-Prusoff equation (Stahl, 2013). There are different types of antagonists, which include the competitive, non-competitive, and uncompetitive ones. These characterizations are structured around the unique approach in which a particular antagonist binds to the active site of the receptor.
References
Stahl, S. M., & Stahl, S. M. (2013). Stahl’s essential psychopharmacology: neuroscientific basis and practical applications. Cambridge university press. *Preface, pp. ix-xii. Retrieved from: https://books.google.co.ke/books?hl=en&lr=&id=BBtMzTV8OMgC&oi=fnd&pg=PR9&dq=Stahl,+S.+M.+(2013).+Stahl%E2%80%99s+essential+psychopharmacology:+Neuroscientific+basis+and+practical+applications+(4th+ed.).+New+York,+NY:+Cambridge+University+Press+*Preface,+pp.+ix%E2%80%93x&ots=HgvkA3QpJ3&sig=q3SuymI1tQTe4vndUNBeaVtMufw&redir_esc=y#v=onepage&q&f=false
Wang, X. H., Xie, X., Luo, X. G., Shang, H., & He, Z. Y. (2017). Inhibiting purinergic P2X7 receptors with the antagonist brilliant blue G is neuroprotective in an intranigral lipopolysaccharide animal model of Parkinson’s disease. Molecular medicine reports, 15(2), 768-776.
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