SH-I-048A

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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[edit]


References[edit]

  1. ^ Obradović ALj, 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 Res. 2014 Mar 20;1554:36-48. doi:10.1016/j.brainres.2014.01.036 PMID 24472579
  2. ^ Clayton T, et al. A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. Int J Med Chem. 2015; 2015: 430248. doi:10.1155/2015/430248 PMID 26682068
  3. ^ Obradović LA, Joksimović S, Poe MM, Timić T, Cook JM, Savić MM. Delayed Behavioral Effects of SH–I–048A, a Novel Nonselective Positive Modulator of Gabaa Receptors, After Peripheral Nerve Injury in Rats. Acta Veterinaria. 2014 Jun 1;64(2):189-99. doi:10.2478/acve-2014-0018
  4. ^ Elgarf A, Siebert D, Steudle F, Draxler A, Li G, Huang S, Cook JM, Ernst M, Scholze P. Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors. ACS Chemical Biology 2018; 13(8):2033-2039. doi:10.1021/acschembio.8b00144