This page uses content from Wikipedia and is licensed under CC BY-SA.

SH-I-048A

SH-I-048A
SH-I-048A structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC16H12BrFN2O
Molar mass347.187 g·mol−1
3D model (JSmol)

SH-I-048A (SH-i-048A) is a benzodiazepine derivative related in structure to compounds such as flubromazepam and meclonazepam. SH-I-048A is described as a non subtype selective superagonist at the benzodiazepine site of GABAA receptors,[1] with a binding affinity of 0.77nM at the α1 subtype, 0.17nM at α2, 0.38nM at α3 and 0.11nM at α5.[2] It has been used to study the functional differences between the different subtypes of the GABAA receptor.[3][4]

See also

References

  1. ^ Obradović AL, Joksimović S, Poe MM, Ramerstorfer J, Varagic Z, Namjoshi O, Batinić B, Radulović T, Marković B, Roth BL, Sieghart W, Cook JM, Savić MM. "Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: the approximated activation of receptor subtypes may explain behavioral effects". Brain Research. 1554.
  2. ^ Clayton T, Poe MM, Rallapalli S, Biawat P, Savić MM, Rowlett JK, et al. (2015). "A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model". International Journal of Medicinal Chemistry. 2015: 430248. doi:10.1155/2015/430248. PMC 4657098. PMID 26682068.
  3. ^ Obradović LA, Joksimović S, Poe MM, Timić T, Cook JM, Savić MM (June 2014). "Delayed Behavioral Effects of SH–I–048A, a Novel Nonselective Positive Modulator of Gabaa Receptors, After Peripheral Nerve Injury in Rats". Acta Veterinaria. 64 (2): 189–99. doi:10.2478/acve-2014-0018.
  4. ^ Elgarf AA, Siebert DC, Steudle F, Draxler A, Li G, Huang S, et al. (August 2018). "A Receptors". ACS Chemical Biology. 13 (8): 2033–2039. doi:10.1021/acschembio.8b00144. PMC 6102643. PMID 29767950.