Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof.

Abstract: This disclosure is directed to methods of conducting dynamic single-molecule fluorescence studies such as smFRET on a membrane protein which permits observation and quantification of conformational dynamics of a membrane protein. Also disclosed herein are mutant membrane proteins in which one or more mutations have been introduced for affixing a fluorophore, as well as reagents and kits containing such mutant membrane proteins for conducting dynamic single-molecule fluorescence studies. The methods and compositions disclosed herein can be used in screening for compounds that enhance or reduce the activity of a membrane protein, useful for treating diseases associated with the malfunction of the membrane protein or alterations in membrane protein conformation.

Abstract: The present invention provides, inter alia, compounds of formula (I): (structurally represented). Also provided are pharmaceutical compositions containing such compounds and methods for treating or ameliorating the effects of a medical condition in a subject using such compounds or pharmaceutical compositions.

Abstract: The present invention relates to compounds that inhibit VIPR2 in the CNS, pharmaceutical compositions comprising said compounds, and methods of using such compounds and compositions in the treatment of a CNS disorder such as a behavioral disorder, including but not limited to schizophrenia.

Abstract: This disclosure is directed to methods of conducting dynamic single-molecule fluorescence studies such as sm-FRET on a membrane protein which permits observation and quantification of conformational dynamics of a membrane protein. Also disclosed herein are mutant membrane proteins in which one or more mutations have been introduced for affixing a fluorophore, as well as reagents and kits containing such mutant membrane proteins for conducting dynamic single-molecule fluorescence studies. The methods and compositions disclosed herein can be used in screening for compounds that enhance or reduce the activity of a membrane protein, useful for treating diseases associated with the malfunction of the membrane protein or alterations in membrane protein conformation.

Abstract: The present invention is directed to, inter alia, a biological reagent that includes a complex having a first GPCR and a second GPCR linked to a G-protein, the linkage between the second GPCR and the G-protein being of a length, which pre-vents productive interaction between the G-protein and the second GPCR, wherein the first GPCR and the second GPCR linked to the G-protein alone are incapable of producing a signal when presented with a ligand. The invention also provides methods of producing such a biological reagent, as well as methods of determining oligomeric GPCR interactions, methods of identifying compounds that have an effect on GPCR oligomers, methods of identifying a compound capable of interacting with GPCR oligomers, methods of identifying a compound having the ability to modulate binding between a GPCR oligomer and its ligand, and methods for evaluating differential G-protein coupling.