Summary of preclinical studies that describe S1R KO or antagonists in different NP models
Pain type | Pain model | Specie | Sex | Ligand | Route | Effect on pain | References |
---|---|---|---|---|---|---|---|
Central neuropathic pain | Spinal cord contusion | Mouse | F | E-52862 | i.p. 7 days | ↓ mechanical allodynia and thermal hyperalgesia | [98] |
Mouse | F | E-52862 | i.p. | ↓ mechanical allodynia and thermal hyperalgesia | [100] | ||
Mouse | F | KO | No mechanical allodynia and thermal hyperalgesia | [100] | |||
Peripheral neuropathic pain | Streptozotocin-induced | Rat | M | E-52862 | i.p., acute, b.i.d. 7 days | ↓ mechanical hyperalgesia | [97] |
Rat | M | PW507 | i.p., acute, b.i.d. 14 days | ↓ mechanical allodynia and thermal hyperalgesia | [111] | ||
Mouse | M | BD-1047 | i.t. 7 days | ↓ mechanical allodynia and thermal hyperalgesia | [112] | ||
Nicotinamide-streptozotocin induced | Mouse | M | Haloperidol | s.c. | ↓ mechanical allodynia and hyperalgesia | [113] | |
Mouse | M | LMH-2 | s.c. | ↓ mechanical allodynia and hyperalgesia | [113] | ||
Zucker diabetic fatty | Rat | M | E-52862 | i.p., acute, b.i.d. 14 days | ↓ mechanical allodynia and thermal hyperalgesia | [114] | |
High-fat diet | Mouse | M | KO | No mechanical allodynia and thermal hyperalgesia | [115] | ||
Mouse | M | BD-1047 | i.t. | ↓ mechanical allodynia and thermal hyperalgesia | [115] | ||
Oxaliplatin-induced | Rat | M | E-52862 | i.p., acute, b.i.d. 7 days | ↓ cold allodynia | [97] | |
Cisplatin-induced | Mouse | M | CM304 | i.p. | ↓ mechanical allodynia | [116] | |
Paclitaxel-induced | Mouse | F | E-52862 | s.c. | ↓ mechanical allodynia and cold hyperalgesia | [101] | |
Mouse | F | BD-1047 | s.c. | ↓ mechanical allodynia and cold hyperalgesia | [101] | ||
Mouse | F | KO | No mechanical allodynia and cold hyperalgesia | [101] | |||
Rat | M | PW507 | i.p. | ↓ cold hyperalgesia | [103] | ||
Partial sciatic nerve ligation | Mouse | M | E-52862 | i.p., acute, b.i.d. 21 days | ↓ mechanical allodynia and thermal hyperalgesia | [104] | |
Mouse | M | E-52862 | i.v.10 days | ↓ mechanical allodynia and thermal hyperalgesia | [105] | ||
Mouse | M | KO | No mechanical allodynia and thermal hyperalgesia | [102] | |||
Chronic constriction injury | Rat | M | BD-1047 | i.t. | ↓ mechanical allodynia | [106] | |
Rat | M | BD-1047 | p.o. | ↓ mechanical allodynia and cold hyperalgesia | [107] | ||
Mouse | M | BD-1047 | i.t. | ↓ mechanical allodynia | [108] | ||
Rat | M | E-52862 | i.p., acute, b.i.d. 7 days | ↓ mechanical allodynia | [97] | ||
Mouse | M | CM304 | i.p. | ↓ mechanical allodynia | [116] |
i.p.: intraperitoneal; i.pl.: intraplantar; i.t.: intrathecal; i.v.: intravenous; p.o.: oral; s.c.: subcutaneous; b.i.d.: twice daily; KO: knockout
The views expressed in the submitted article are the author’s own and not official positions of the author’s institutions (Rutgers Cancer Institute of New Jersey, Intra-Cellular Therapies, Inc., and Rutgers Robert Wood Johnson Medical School).
YP: Conceptualization, Data curation, Formal analysis, Funding acquisition, Investigation, Methodology, Writing—original draft, Writing—review & editing. QZ: Conceptualization, Data curation, Formal analysis, Investigation, Methodology, Writing—original draft, Writing—review & editing, Visualization. SC: Conceptualization, Writing—review & editing.
YP is an inventor on PCT/US2019/066048, which describes PW507 and its analogs as novel S1R ligands. These compounds are also discussed in this manuscript. The author declares that this patent may be relevant to the content of this study, but no financial interests are currently associated with it.
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YP is sponsored by Rutgers Cancer Institute of New Jersey Biomedical Informatics Shared Resource [NCI-CCSG P30CA072720-5917]. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.
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