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TitleSynthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.
Journal, issue, pagesAcs Chem Neurosci, Vol. 7, Page 378-390, Year 2016
Publish dateJun 4, 2015 (structure data deposition date)
AuthorsLarsen, A.P. / Francotte, P. / Frydenvang, K. / Tapken, D. / Goffin, E. / Fraikin, P. / Caignard, D.H. / Lestage, P. / Danober, L. / Pirotte, B. / Kastrup, J.S.
External linksAcs Chem Neurosci / PubMed:26771108
MethodsX-ray diffraction
Resolution2.07 Å
Structure data

PDB-5buu:
Crystal structure of the GluA2 ligand-binding domain (L483Y-N754S) in complex with glutamate and BPAM-321 at 2.07 A resolution
Method: X-RAY DIFFRACTION / Resolution: 2.07 Å

Chemicals

ChemComp-4V6:
(3R)-7-chloro-2,3,4-trimethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide

ChemComp-GLU:
GLUTAMIC ACID

ChemComp-SO4:
SULFATE ION

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-HOH:
WATER

Source
  • rattus norvegicus (Norway rat)
KeywordsMEMBRANE PROTEIN / AMPA receptor ligand-binding domain / GluA2 L483Y-N754S / BPAM-321 positive allosteric modulation

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