Discovery and characterization of non-competitive antagonists of group I metabotropic glutamate receptors

Farmaco

Volumn 56, Issue 1-2, 2001, Pages 95-99

  Gasparini, Fabrizio ^a   Floersheim, Philipp ^a   Flor, Peter Josef ^a   Heinrich, Micheline ^a   Inderbitzin, Werner ^a   Ott, David ^a   Pagano, Adriana ^a   Stierlin, Christine ^a   Stoehr, Natacha ^a   Vranesic, Ivo ^a   Kuhn, Rainer ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Metabotropic glutamate receptors; Molecular modeling; Non competitive antagonists

Indexed keywords

GLUTAMATE RECEPTOR; GLUTAMATE RECEPTOR ANTAGONIST; IONOTROPIC RECEPTOR; METABOTROPIC RECEPTOR; RECEPTOR SUBTYPE;

BINDING SITE; CONFERENCE PAPER; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; HUMAN; MODEL; NEUROPROTECTION; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

BINDING SITES; MODELS, MOLECULAR; RECEPTORS, METABOTROPIC GLUTAMATE;

EID: 0035273458     PISSN: 0014827X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-827X(01)01008-4     Document Type: Conference Paper

References (13)

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5. A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropa[b]-chromen-1a-carboxylates
6. Chiral resolution, pharmacological characterization and receptor docking of the non-competitive mGlu1 receptor antagonist (±)-2-hydroxyimino-1a,2-dihydro-1H-7-oxa-cyclopropa[b]naphtalene-7a-carboxylic acid ethyl ester (CPCCOEt)
7. 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist
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9. The non-competitive antagonists MPEP and CPCCOEt interact with overlapping binding pockets in the transmembrane region of group-I metabotropic glutamate receptors
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