# US 9,040,581 B1 · Methods of treatment using D-serine

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- Number: US 9,040,581 B1
- Document ID: US9040581B1
- Status: Granted
- Kind: B1
- Application number: 14/185,421
- Filed: 2014-02-20
- Granted: 2015-05-26
- Earliest claimed: 2013-02-21
- Assignees: The Florida State University Research Foundation, Inc.
- Applicants: The Florida State University Research Foundation, Inc.
- Inventors: Sanjay Kumar
- Web page: https://patentgrep.com/patent/US9040581B1

## CPC

- A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205)
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0085: {Brain, e.g. brain implants; Spinal cord}
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/13: Amines {(A61K31/04 takes precedence)}
- A61P 25/08: Antiepileptics; Anticonvulsants
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Methods of treatment using D-serine to target brain cells expressing GluN3 subunit-containing triheteromeric NMDARs are disclosed. The methods include inhibiting calcium ion uptake by brain cells, treating epilepsy, and treating seizures by artificially administering D-serine.

## Claims

### Claim 1

A method of inhibiting calcium ion uptake by brain cells, the method comprising artificially administering D-serine to brain cells expressing GluN3 subunit-containing triheteromeric NMDARs, the amount of D-serine being effective to inhibit calcium ion uptake by the cells.

### Claim 2 (depends on 1)

The method of claim 1, wherein the brain cells are from a brain's temporal lobe.

### Claim 3 (depends on 1)

The method of claim 1, wherein the brain cells are from a brain's medial entorhinal cortex.

### Claim 4 (depends on 1)

The method of claim 1, wherein the GluN3 subunit-containing NMDARs are triheteromeric NMDARs containing GluN1 and GluN2 in addition to GluN3.

### Claim 5 (depends on 1)

The method of claim 1, wherein D-serine is artificially administered by selectively contacting brain cells from an area of the brain known to contain brain cells expressing GluN3 subunit-containing triheteromeric NMDARs.

### Claim 6 (depends on 1)

The method of claim 1, wherein the brain cells are from an epileptic patient.

### Claim 7 (depends on 6)

The method of claim 6,
wherein the D-serine is artificially administered by selectively contacting a region of the epileptic patient's brain with the D-serine, the region being pre-identified as having cells expressing GluN3 subunit-containing triheteromeric NMDARs.

### Claim 8 (depends on 6)

The method of claim 6, wherein the D-serine is artificially administered by selectively contacting a temporal lobe of the epileptic patient's brain with the D-serine.

### Claim 9 (depends on 6)

The method of claim 6, wherein the D-serine is artificially administered by selectively contacting a medial entorhinal cortex of the epileptic patient's temporal lobe with the D-serine.

### Claim 10 (depends on 6)

The method of claim 6, wherein the D-serine is artificially administered by injecting a temporal lobe of the patient's brain with the D-serine.

### Claim 11 (depends on 6)

The method of claim 6, wherein the D-serine is artificially administered by injecting a medial entorhinal cortex of the epileptic patient's temporal lobe with the D-serine.

### Claim 12 (depends on 6)

The method of claim 6, wherein the epileptic patient has temporal lobe epilepsy.

### Claim 13 (depends on 1)

The method of claim 1, wherein the brain cells are from a patient that has seizures.

### Claim 14 (depends on 13)

The method of claim 13, wherein D-serine is artificially administered by selectively contacting a region of the patient's brain pre-identified as having cells expressing GluN3 subunit-containing triheteromeric NMDARs with D-serine.

### Claim 15 (depends on 14)

The method of claim 14, wherein D-serine is artificially administered by selectively contacting a temporal lobe of the patient's brain with D-serine.

### Claim 16 (depends on 14)

The method of claim 14, wherein D-serine is artificially administered by selectively contacting a medial entorhinal cortex of the patient's temporal lobe with D-serine.

### Claim 17 (depends on 14)

The method of claim 14, wherein D-serine is artificially administered by injecting a temporal lobe of the patient's brain with D-serine.

### Claim 18 (depends on 14)

The method of claim 14, wherein D-serine is artificially administered by injecting a medial entorhinal cortex of the patient's temporal lobe with D-serine.

### Claim 19 (depends on 14)

The method of claim 14, wherein the seizures are caused by temporal lobe epilepsy.

### Claim 20 (depends on 1)

The method of claim 1, wherein the D-serine is artificially administered as a pharmaceutical dosage form comprising D-serine and at least one pharmaceutically acceptable excipient.