Antipsychotic drugs make it to the list of widely prescribed and consumed medicines across the globe especially with individuals diagnosed with autism, bipolar disorders, and schizophrenia.
However, a recent study has observed individuals diagnosed with the above conditions, are most likely to experience side effects to the extreme since the drugs are likely to interact with other receptors in the brain. Scientists at the UC San Francisco and the UNC School of Medicine have been successful in solving the first high-resolution images of the DRD2 structure that is seen to have an underlying link with the antipsychotic drug Risperidone.
This, scientists believe, is a long-awaited tool that is bound to help psychiatrists, neuroscientists and manufacturers to better their treatments. The outcome of this research will help researchers in selectively activating DRD2 which will limit antipsychotic drug side effects such as anxiety, dizziness, indigestion, weight gain, and agitations, to a considerable extent.
Prof. Michael Hooker says, “To create better medications, the first and foremost step will be to observe how the D2 receptors will look in high-resolution.” The professor further comments, “We have a structure in place now and we are capable of exploring other compounds which are bound to benefit millions of people who are in need of better and timely treatments.”
30 percent of the medications available on the market tend to activate G-protein receptors on the surface of the cells which are a triggering factor for chemical signals present in the inner regions of the cells to yield their therapeutic effects. The authors highlight scientists’ inability to thoroughly target specific types of receptors owing to their lack of knowledge about the underlying structural differences between different receptors in the brain.
“With the help of these structures captured using the best resolution, we can aim to discover the compounds that interact with specific receptors thus aiming to minimize side effects,” explains Roth.
To overcome technical challenges, Roth and colleagues from the UNC, have conducted tireless studies over the past couple of years to have DRD2 crystallize the results while being bound tightly to Risperidone.
The researchers highlight seeing, with high-resolution images, that Risperidone binds in ways that were not previously known. Other computational models performed by the UCSF researchers Anat Levit and Brian Shoichel reveal binding modes were initially unpredictable.
“We are able to identify accurate structural differences between receptors that are similar in nature. This will further assist us in envisioning methods that will be helpful in creating newer compounds that will be capable of interacting and only bind to DRD2 without having to interact dozens of other receptors unlike earlier.”
Wacker concludes, “This is the information that is the need of the hour and will help us to create safer and better therapeutics.”