2064172-83-2
2064172-83-2 structure
- Name: RGM8-51
- Chemical Name: RGM8-51
- CAS Number: 2064172-83-2
- Molecular Formula: C39H44N2O3
- Molecular Weight: 588.792
- Create Date: 2022-07-01 12:16:08
- Modify Date: 2023-01-25 19:29:12
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RGM8-51 is a β-lactam derivative, potent, selective TRPM8 antagonist with IC50 of 1.06 and 1.74 uM for rat and human TRPM8, respectively.RGM8-51 does not have any ability to activate TRPM8 channels, but produces a concentration-dependent inhibition of menthol activation.RGM8-51 is selective for cold-activated TRPM8 channels, displays no agonist or antagonist profile in cool-activated TRPA1 channels and has negligible activity as TRPV3 and ASIC3 channel antagonists.RGM8-51 (1 µM) inhibited menthol-activated currents in rTRPM8-expressing HEK293 cells.RGM8-51 exhibits in vivo antinociceptive activity in response to cold, in a mouse model of oxaliplatin-induced peripheral neuropathy.RGM8-51 reduces cold, mechanical and heat hypersensitivity in a rat model of neuropathic pain arising after chronic constriction of the sciatic nerve.RGM8-51 exhibits mechanical hypersensitivity-relieving activity, in a mouse model of NTG-induced hyperesthesia.
| Name | RGM8-51 |
|---|
| Description | RGM8-51 is a β-lactam derivative, potent, selective TRPM8 antagonist with IC50 of 1.06 and 1.74 uM for rat and human TRPM8, respectively.RGM8-51 does not have any ability to activate TRPM8 channels, but produces a concentration-dependent inhibition of menthol activation.RGM8-51 is selective for cold-activated TRPM8 channels, displays no agonist or antagonist profile in cool-activated TRPA1 channels and has negligible activity as TRPV3 and ASIC3 channel antagonists.RGM8-51 (1 µM) inhibited menthol-activated currents in rTRPM8-expressing HEK293 cells.RGM8-51 exhibits in vivo antinociceptive activity in response to cold, in a mouse model of oxaliplatin-induced peripheral neuropathy.RGM8-51 reduces cold, mechanical and heat hypersensitivity in a rat model of neuropathic pain arising after chronic constriction of the sciatic nerve.RGM8-51 exhibits mechanical hypersensitivity-relieving activity, in a mouse model of NTG-induced hyperesthesia. |
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| References | 1. Martín-Escura C, et al. Int J Mol Sci. 2022 Feb 28;23(5):2692. |
| Molecular Formula | C39H44N2O3 |
|---|---|
| Molecular Weight | 588.792 |