期刊
FUTURE MEDICINAL CHEMISTRY
卷 8, 期 3, 页码 287-295出版社
FUTURE SCI LTD
DOI: 10.4155/fmc.15.191
关键词
amyotrophic lateral sclerosis; CNS distribution; multiple sclerosis; neurological disorders; Parkinson's disease; pharmacokinetic profile; S1R agonist
Aim: Nowadays, there is a great interest in the therapeutic potential of sigma1 receptor ligands for treating different CNS pathologies. Our previous investigations led to identify (R)-RC-33 as a potent and selective S1R agonist. Results: Herein, we report the gram-scale synthesis, pharmacokinetic profile and CNS distribution of (R)-RC-33 in the mouse to determine the most suitable dosage schedule for in vivo administration. For comparative purposes, the same experiments were also performed with PRE-084, the most widely used S1R agonist commonly in pharmacological experiments. Discussion: (R)-RC-33 shows a similar pharmacokinetic profile and a better CNS distribution when compared with PRE-084. Conclusion: (R)-RC-33 may be a promising candidate for in vivo studies in animal models of neurodegenerative diseases.
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