| 词条 | SH-I-048A |
| 释义 |
| IUPAC_name = (3S)-7-bromo-5-(2-fluorophenyl)-3-methyl-1H-benzo[e] [1,4]diazepin-2(3H)-one | image = SH-I-048A_structure.png | width = 200 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_UK = | legal_status = | routes_of_administration = | addiction_liability = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 872874-11-8 | ATC_prefix = | ATC_suffix = | PubChem = 49850464 | ChemSpiderID = 57381614 | C=16 | H=12 | Br=1 | F=1 | N=2 | O=1 | melting_point = | smiles = Fc3ccccc3C2=N[C@@H](C)C(=O)Nc1ccc(Br)cc12 | StdInChI=1S/C16H12BrFN2O/c1-9-16(21)20-14-7-6-10(17)8-12(14)15(19-9)11-4-2-3-5-13(11)18/h2-9H,1H3,(H,20,21)/t9-/m0/s1 | StdInChIKey = QEFZCKUXGLDPPT-VIFPVBQESA-N }}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
References1. ^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 }} {{Benzodiazepines}}{{GABAAR PAMs}}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}} 2 : Benzodiazepines|GABAA receptor positive allosteric modulators |
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