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5-(2-Fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)pyridine-3-yl]oxy]-3-oxo-2,3-dihydro-1H-indole-2-carboxamide, also known as Compound X, is a potent and selective antagonist of the neonatal rat vasopressin 1a receptor (nrv1aR).
This research article, titled "Exploring thephylogeny andreceptor repertoiresof the vasopressin 1a receptor gene family in teleosts," was published in the journal Genome Biology and Evolution in 2017.
The study of Compound X has been valuable in understanding the actions of this class of compounds on the nrv1aR, which is a G protein–coupled receptor that is selectively expressed in the hypothalamus of the brain.
The research has also provided insight into the evolution of the receptor and its actions in the context of the teleost fish.
Compound X was synthesized by researchers at Monash University in Australia, who were looking to develop new treatments for water balance disorders such as diabetes insipidus.
The compound was found to be highly selective for the nrv1aR, with little or no binding to other G protein–coupled receptors.
This selectivity makes it an attractive candidate for the treatment of disorders such as diabetes insipidus and other conditions that are caused by abnormal regulation of water balance.
The study of Compound X has also provided information about the evolution of the nrv1aR and its receptor activity in teleosts, which are a group of fish that includes zebrafish and other common species.
The researchers found that the nrv1aR has been evolutionarily conserved in teleosts, with similar receptor properties and functions across different species.
This conservation suggests that the nrv1aR has played an important role in the survival and success of these fish, and that it continues to play a vital role in their physiology and behavior.
The research on Compound X has also highlighted the importance of considering the evolutionary history of a receptor when developing new treatments.
By understanding the ways in which a receptor has evolved over time, researchers can gain insight into its function and the actions of compounds that bind to it.
This information can be used to develop more effective and targeted therapies that are less likely to cause side effects or interact with other receptors.
In conclusion, the study of Compound X has provided valuable information about the nrv1aR and its role in the physiology and behavior of teleosts.
The research has also highlighted the importance of considering the evolutionary history of a receptor when developing new treatments, and has provided insight into the actions of compounds that bind to this receptor.
The continued study of Compound X and other similar compounds has the potential to lead to the development of new and effective treatments for water balance disorders and other conditions.