Neuroactive steroids, compositions, and uses thereof
By administering 24(S)-hydroxycholesterol or its related compounds, the NMDA receptor activity is regulated, and the problem of NMDA receptor regulation in existing therapeutic methods is solved, and the therapeutic effect of psychotic disorders and central nervous system diseases is improved.
Patent Information
- Application Number
- CN202410635379.7
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2013-03-13
- Filing Date
- 2014-03-13
- Publication Date
- 2025-01-07
AI Technical Summary
Existing treatments are difficult to effectively regulate NMDA receptors, resulting in poor treatment of psychotic disorders and other central nervous system-related diseases.
By administering 24(S)-hydroxycholesterol or its related compounds, as an agonist or antagonist of the NMDA receptor, the activity of the NMDA receptor is modulated to increase or decrease its endogenous activity, and is used to treat schizophrenia, Depression and other diseases.
The fine regulation of NMDA receptors has been achieved, and the effect of treating psychotic disorders and other central nervous system diseases has been improved, providing potential clinical applications.
Smart Images
Figure BDA0004851509310000071 
Figure BDA0004851509310000072 
Figure BDA0004851509310000073
Abstract
Claims
1. A method of evaluating or treating a patient, e.g., a patient suffering from a disorder described herein, comprising: a) optionally, obtaining a patient sample; b) obtaining an assessment of the sample and / or assessing a change in the level of 24(S)-hydroxycholesterol in the sample compared to a reference standard.
2. The method of claim 1, further comprising administering to the patient (e.g., in response to evaluation of the sample) an effective amount of 24(S)-hydroxycholesterol or a structurally related sterol or steroid, an oxysterol, an agonist of NMDAR or a positive allosteric modulator (PAM) of NMDAR, or a compound described herein, e.g., a compound of formula (I).
3. The method of claim 1, further comprising administering to the patient (e.g., in response to evaluation of the sample) an effective amount of an antagonist of NMDAR or a negative allosteric modulator (NAM) of NMDAR.
4. The method of claim 1, further comprising administering to the patient (e.g., in response to the evaluation of the sample) an effective amount of a compound that increases (e.g., enhances) the endogenous activity or amount of 24(s)-hydroxycholesterol (e.g., a compound that inhibits an enzyme that metabolizes 24(s)-hydroxycholesterol (e.g., a compound that inhibits 24-hydroxycholesterol 7α-hydroxylase (CYP39))).
5. The method of claim 1, further comprising administering to the patient (e.g., in response to the evaluation of the sample) an effective amount of a compound that reduces the endogenous activity or amount of 24(s)-hydroxycholesterol (e.g., a compound that activates an enzyme that produces 24(s)-hydroxycholesterol (e.g., a compound that activates cholesterol 24(S)-hydroxylase (CYP46))).
6. The method of claim 1, wherein the method further comprises treating a patient, wherein the patient's memory deficit is treated or learning ability is improved.
7. The method of claim 1, wherein the method further comprises treating the patient for a drug overdose.
Citation Information
Patent Citations
Neuroactive steroids, compositions, and uses thereof
CN112057457A
Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
US5376645A