When it comes to viewing the agonist/antagonist dynamics within a particular matter, they can be distinctly seen within arginine vasopressin. Saleh et al. (2016) state that molecular dynamics modeling with enhanced metadynamics sampling revealed three different binding sites for the peptide within the V2 receptor. Two of them – the intermediate and vestibule sites – antagonize – that is, block –
the receptor. The third one is known as an orthosteric activation site – or an agonist. Simulations of meta-dynamics for the V2-receptor and its analog, according to Saleh et al. (2016), correlate excellently with experimental free-binding energies. The resulting mechanism of the three sites provides the separation of antagonists from the agonists and explains the selectivity of the subtypes.
G-protein coupled receptors (GPCRs) are among nature’s most remarkable formations. Not only do they guide many different processes, but they are also surprisingly versatile. According to Saleh et al. (2016), one receptor can act on regulation mechanisms through one or a few G proteins and arrestin paths. GPCR ligands’ functions are diverse as well; they can be antagonists or agonists – with the latter, even partial or inverse ones, and act following alternative paths. They amount to about 40 percent of all the drugs marketed. However, a lot is not yet known about the mechanisms that ensure these various functions.
As a person becomes a drug addict, their brain’s nerve cells, indeed, learn to adapt during repeated exposure to drugs at the epigenetic level. These drug-induced adaptations cause sustained changes in the brain’s functioning that promote permanent, drug-related disorders of behavior-defining addiction. Hamilton and Nestler (2019) suppose that if these particular alterations are to be targeted, understanding of the addiction’s basis on the biological level will be enhanced. As a result, even more, sufficient therapies may be implemented.
It is evident that for a professional to be successful in treating addiction, they must understand the basics of this process. Stewart et al. (2021) state that drug abusers suffer from chronic brain disorders, which imply the brain’s plasticity in adapting to more severe addicted states with time. Only a person properly trained can establish appropriate rapport with such individuals. Additionally, as per Ignaszewski (2021), the effects of substance abuse go beyond the serious health consequences – they spread to abusers’ families and other members of communities. Thus, in a way, helping those struggling is doing a favor to society as a whole.
References
Hamilton, P. J., & Nestler, E. J. (2019). Epigenetics and addiction.Current Opinion in Neurobiology, 59, 128-136. Web.
Ignaszewski, M. J. (2021). The epidemiology of drug abuse.The Journal of Clinical Pharmacology, 61, S10-S17. Web.
Saleh, N., Saladino, G., Gervasio, F. L., Haensele, E., Banting, L., Whitley, D. C.,… & Clark, T. (2016). A three‐site mechanism for agonist/antagonist selective binding to vasopressin receptors.Angewandte Chemie, 128(28), 8140-8144. Web.
Stewart, A. F., Fulton, S. L., & Maze, I. (2021). Epigenetics of drug addiction.Cold Spring Harbor perspectives in medicine, 11(7). Web.