# US 11,439,715 B2 · Compositions and methods to detect GLUA1 in brain and to identify the presence of GLUA1-mediated post-traumatic stress disorder and other neurological disorders > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,439,715 B2 - Document ID: US11439715B2 - Status: Granted - Kind: B2 - Application number: 16/642,220 - Filed: 2018-08-28 - Published: 2021-03-11 - Granted: 2022-09-13 - Earliest claimed: 2017-08-28 - Assignees: Neurovation Labs, Inc. - Applicants: Neurovation Labs, Inc. - Inventors: Jennifer Nicole Perusini - Web page: https://patentgrep.com/patent/US11439715B2 ## CPC - A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} - A61K 51/0497: {conjugates with a carrier being an organic compounds} - A61B 6/501: {for diagnosis of the head, e.g. neuroimaging or craniography} - A61K 9/08: Solutions {(composition of solutions A61K47/00)} - A61K 47/02: Inorganic compounds - A61K 51/04: Organic compounds - C07B 59/001: {Acyclic or carbocyclic compounds} - C07C 211/40: containing only non-condensed rings - A61B 6/037: {Emission tomography} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61B: DIAGNOSIS; SURGERY; IDENTIFICATION (usefulness limited to only animals A61D) - C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F) - C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS ## Abstract The present invention provides compositions and methods for detecting GluA1, as a subunit protein and/or as a GluA1-containing, GluA2-lacking AMPAR complex. The invention further provides composition and methods for detecting and/or diagnosing GluA1-mediated disorders, such as PTSD. The invention further relates to compositions that can be detected using radiological imaging techniques, and processes for performing such imaging techniques using the compositions, to identify elevated GluA1 expression or activity in a subject. ## Claims ### Claim 1 A method of detecting GluA1 levels, or GluA1-containing, GluA2-lacking AMPAR levels, in a region of interest of a subject, comprising: a. administering to the subject a first amount of a radiolabeled composition comprising at least one ligand of GluA1 or of a GluA1-containing, GluA2-lacking AMPAR, labeled with a radioactive isotope, wherein the radiolabeled composition comprises any of the following structures: or pharmaceutically acceptable salts thereof, wherein the F is an [18F] radioisotope; b. subjecting at least the region of interest of the subject to radiological imaging capable of detecting radioactive emissions from an amount of the radiolabeled composition; and c. determining or quantifying, based at least in part upon the radiological imaging, an amount of radioactive emissions corresponding to a second amount of the radiolabeled composition that is in the region of interest after administration of the first amount. ### Claim 2 (depends on 1) The method of claim 1, further comprising: d. determining or quantifying a GluA1 subunit density or a GluA1-containing, GluA2-lacking AMPAR density in the region of interest of the subject based at least in part upon the amount of radioactive emissions corresponding to the second amount of the radiolabeled composition. ### Claim 3 (depends on 2) The method of claim 2, further comprising: e. comparing the density so determined or quantified with a predetermined baseline level, wherein a density different from the predetermined baseline level indicates a GluA1-mediated disorder in the subject. ### Claim 4 (depends on 3) The method of claim 3, wherein the region of interest is an amygdala, and the GluA1-mediated disorder is PTSD. ### Claim 5 (depends on 1) The method of claim 1, wherein the amount of radioactive emissions corresponding to the second amount of the radiolabeled composition corresponds to an amount of binding and localization of the radiolabeled composition in the region of interest, and a difference in binding and localization of the radiolabeled composition in the region of interest compared to a normal subject without a GluA1-mediated disorder is indicative of a GluA1-mediated disorder. ### Claim 6 (depends on 1) The method of claim 1, wherein the subject is a living subject. ### Claim 7 A compound having the following structure: or a pharmaceutically acceptable salt thereof, wherein the F is an [18F] radioisotope. ### Claim 8 (depends on 7) The compound of claim 7, wherein the compound is in a pharmaceutically acceptable carrier. ### Claim 9 (depends on 7) The compound of claim 7, wherein the compound is in a solution. ### Claim 10 (depends on 9) The compound of claim 9, wherein the solution is a saline solution. ### Claim 11 (depends on 7) The compound of claim 7, wherein the compound is a ligand of GluA1 or of a GluA1-containing, GluA2-lacking AMPAR. ### Claim 12 (depends on 7) The compound of claim 7, wherein the compound is suitable as a radiolabeled tracer for radiological imaging. ### Claim 13 (depends on 7) The compound of claim 7, wherein the compound serves as an imaging agent suitable for detecting GluA1 levels or GluA1-containing, GluA2-lacking AMPAR levels in a region of interest of a subject. ### Claim 14 A compound having the following structure: or a pharmaceutically acceptable salt thereof, wherein the F is an [18F] radioisotope. ### Claim 15 (depends on 14) The compound of claim 14, wherein the compound is in a pharmaceutically acceptable carrier. ### Claim 16 (depends on 14) The compound of claim 14, wherein the compound is in a solution. ### Claim 17 (depends on 16) The compound of claim 16, wherein the solution is a saline solution. ### Claim 18 (depends on 14) The compound of claim 14, wherein the compound is a ligand of GluA1 or of a GluA1-containing, GluA2-lacking AMPAR. ### Claim 19 (depends on 14) The compound of claim 14, wherein the compound is suitable as a radiolabeled tracer for radiological imaging. ### Claim 20 (depends on 14) The compound of claim 14, wherein the compound serves as an imaging agent suitable for detecting GluA1 levels or GluA1-containing, GluA2-lacking AMPAR levels in a region of interest of a subject.