Bay36-7620: A potent non-competitive mGlu1 receptor antagonist with inverse agonist activity

Molecular Pharmacology

Volumn 59, Issue 5, 2001, Pages 965-973

  Carroll, Fiona Y ^a   Stolle, Andreas ^b   Beart, Philip M ^c   Voerste, Arnd ^b   Brabet, Isabelle ^a   Mauler, Frank ^b   Joly, Cécile ^a   Antonicek, Horst ^b   Bockaert, Joël ^a   Müller, Thomas ^b   Pin, Jean Philippe ^a   Prézeau, Laurent ^a,d  

^a CNRS   (France)

^b BAYER AG   (Germany)

^c MONASH UNIVERSITY   (Australia)

^d INSERM   (France)

Author keywords

[No Author keywords available]

Indexed keywords

6A NAPHTHALEN 2 YLMETHYL 5 METHYLIDEN HEXAHYDROCYCLOPENTAL[C]FURAN 1 ON; BAY 36 7620; CHIMERIC PROTEIN; G PROTEIN COUPLED RECEPTOR; GLUTAMATE RECEPTOR; GLUTAMATE RECEPTOR 1; GLUTAMATE RECEPTOR ANTAGONIST; MEMBRANE PROTEIN; METABOTROPIC RECEPTOR; QUISQUALIC ACID; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

AGONIST; ANIMAL CELL; ARTICLE; COMPETITIVE INHIBITION; DOSE RESPONSE; DRUG MECHANISM; HUMAN; HUMAN CELL; KIDNEY CELL; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN DOMAIN; PROTEIN EXPRESSION; RAT; SYNAPTIC TRANSMISSION;

EID: 0035028011     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.59.5.965     Document Type: Article

References (40)

1. Constitutive Gi2-dependent activation of adenylyl cyclase type II by the 5-HT1A receptor
2. Constitutively signaling G-protein-coupled receptors and human disease
3. Constitutively active 5-hydroxytryptamine 2C receptors reveal novel inverse agonist activity of receptor ligands
4. 3D-model of the extracellular domain of the type 4a metabotropic glutamate receptor: New insights into the activation process
5. Molecular tinkering of G protein-coupled receptors: An evolutionary success
6. Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor
7. Comparative effect of L-CCG-I, DCG-IV and γ-carboxy-L-glutamate on all cloned metabotropic glutamate receptor subtypes
8. Calcium-receptor-regulated parathyroid and renal function
9. Inverse agonist activity of β-adrenergic antagonists
10. Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: Role of the C-terminal intracellular domain
11. ia
12. Pharmacology and functions of metabotropic glutamate receptors
13. 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function
14. Mapping the agonist-binding site of GABAB type 1 subunit sheds light on the activation process of GABAB receptors
15. αq/i proteins: Characterization of new antagonists
16. 2+ receptors
17. Ligand binding to the amino-terminal domain of the mGluR4 subtype of metabotropic glutamate receptor
18. Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1alpha metabotropic glutamate receptor
19. Functional importance of the Ala116-Pro136 region in the calcium-sensing receptor
20. Molecular, functional and pharmacological characterization of the metabotropic glutamate receptor type 5 splice variants: Comparison with mGluR1
21. Primary structure and functional characterization of a high-affinity glutamate transporter
22. Constitutive activation of the α1B-adrenergic receptor by all amino acid substitutions at a single site: Evidence for a region which constrains receptor activation
23. Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor
24. The two-state model of receptor activation
25. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins
26. CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding
27. B receptors is sufficient to specify agonist and antagonist binding
28. BAY 36-7620, a selective metabotropic glutamate receptor 1 antagonist with anticonvulsant and neuroprotective properties
29. The ligand-binding domain in metabotropic glutamate receptors is related to bacterial periplasmic binding proteins
30. Gα15 and Gα16 couple a wide variety of receptors to phospholipase C
31. Expression and purification of the extracellular ligand binding region of metabotropic glutamate receptor subtype 1
32. The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group-I metabotropic glutamate receptors
33. Conservation of the ligand recognition site of metabotropic glutamate receptors during evolution
34. The G-protein coupling profile of metabotropic glutamate receptors, as determined with exogenous G-proteins, is independent of their ligand recognition domain
35. New perspectives for the development of selective metabotropic glutamate receptor ligands
36. Pharmacological characterization of metabotropic glutamate receptors in several types of brain cells in primary cultures
37. Changes of the C-terminal domain of mGluR1 by alternative splicing generate receptors with different agonist independent activity
38. A mutation-induced activated state of the β2-adrenergic receptor
39. Pharmacological agents acting at subtypes of metabotropic glutamate receptors
40. Measurement of protein using bicinchoninic acid