Development of Pharmacological Strategies with Therapeutic Potential in Ischemic Stroke
Abstract
:1. Introduction
2. Development of New Pharmacological Neuroprotective Strategies for the Treatment of Ischemic Stroke
2.1. Quinolylnitrones as a Result of a Screening Program
2.1.1. Biological Characterization of RP19: A First-Hit Quinolylnitrone
2.1.2. Structure–Activity Relationship Study: The Identification of QN23
2.1.3. Future Perspectives: New Quinolyl Derivatives on the Way
2.2. Nitrone Attachment to Steroids: Cholesterol-Derived Nitrone ISQ201
3. Discussion
4. Summary and Outlook
5. Patents
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Structural Family | Quinolylnitrones | Cholesteronitrones |
Development strategy | SAR-screening-based strategy | Knowledge-based strategy |
Screening | Yes | No |
SAR | Yes | No |
Maximal effective concentration in cellular OGD model | 100 µM | 5 µM |
Effective dose (range) in transient cerebral ischemia | 1.5–2.5 mg/kg | 0.05–0.1 mg/kg |
Therapeutic window | Up to 3 h after reperfusion onset | Up to 6 h after reperfusion onset |
Elimination half-life (dose) | 0.16 h (2.0 mg/kg) | 1.66 h (0.07 mg/kg) |
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Escobar-Peso, A.; Martínez-Alonso, E.; Masjuan, J.; Alcázar, A. Development of Pharmacological Strategies with Therapeutic Potential in Ischemic Stroke. Antioxidants 2023, 12, 2102. https://doi.org/10.3390/antiox12122102
Escobar-Peso A, Martínez-Alonso E, Masjuan J, Alcázar A. Development of Pharmacological Strategies with Therapeutic Potential in Ischemic Stroke. Antioxidants. 2023; 12(12):2102. https://doi.org/10.3390/antiox12122102
Chicago/Turabian StyleEscobar-Peso, Alejandro, Emma Martínez-Alonso, Jaime Masjuan, and Alberto Alcázar. 2023. "Development of Pharmacological Strategies with Therapeutic Potential in Ischemic Stroke" Antioxidants 12, no. 12: 2102. https://doi.org/10.3390/antiox12122102