PS75

PS75
Identifiers
	IUPAC name N-(pyridin-4-yl)-7-chloronaphthalen-1-amine;
CAS Number	none;
Chemical and physical data
Formula	C15H11ClN2
Molar mass	254.72 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc1cc2c(cccc2cc1)Nc1ccncc1;

PS75 is an experimental analgesic drug which acts as a functionally selective alpha-2A adrenergic agonist, with a K_i of 8.2nM and an EC₅₀ of 4.8nM at the α_2A receptor. In animal studies it was found to produce analgesia but without the sedation typical of older drugs acting at this target such as dexmedetomidine. While PS75 itself is unlikely to be developed for medical use, the successful separation of analgesia from sedative effects makes it likely that related compounds may be developed as non-sedating, nonopioid analgesic medications.^[1]

References

↑ Fink EA, Xu J, Hübner H, Braz JM, Seemann P, Avet C, et al. (September 2022). "Structure-based discovery of nonopioid analgesics acting through the α_2A-adrenergic receptor". Science. 377 (6614): eabn7065. doi:10.1126/science.abn7065. PMC 10360211. PMID 36173843.

This article is issued from Offline. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[pmid36173843-1] Fink EA, Xu J, Hübner H, Braz JM, Seemann P, Avet C, et al. (September 2022). "Structure-based discovery of nonopioid analgesics acting through the α_2A-adrenergic receptor". Science. 377 (6614): eabn7065. doi:10.1126/science.abn7065. PMC 10360211. PMID 36173843.

[1]