Two new non-competitive mGlu1 receptor antagonists are potent tools to unravel functions of this mGlu receptor subtype

British Journal of Pharmacology

Volumn 151, Issue 6, 2007, Pages 723-724

  Knopfel T ^a  

^a RIKEN BRAIN SCIENCE INSTITUTE   (Japan)

Author keywords

Drug target; Metabotropic glutamate receptors; mGlu1; Purkinje neuron; Synaptic potential

Indexed keywords

3,4 DIHYDRO 2H PYRANO[2,3 B]QUINOLIN 7 YL 4 METHOXYCYCLOHEXYLMETHANONE; 6 AMINO N CYCLOHEXYL N,3 DIMETHYLTHIAZOLO[3,2 A]BENZIMIDAZOLE 2 CARBOXAMIDE; METABOTROPIC GLUTAMATE RECEPTOR 1 ANTAGONIST; METABOTROPIC RECEPTOR; RECEPTOR BLOCKING AGENT; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

BRAIN FUNCTION; DRUG POTENCY; DRUG SELECTIVITY; HUMAN; NONHUMAN; PRIORITY JOURNAL; PROTEIN FUNCTION; REVIEW; VALIDATION STUDY;

BENZIMIDAZOLES; BRAIN; DRUG DELIVERY SYSTEMS; ELECTROPHYSIOLOGY; HUMANS; QUINOLINES; RECEPTORS, METABOTROPIC GLUTAMATE; SYNAPTIC TRANSMISSION; THIAZOLES;

EID: 34447546676     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707289     Document Type: Review

References (17)

1. Annoura H, Fukunaga A, Uesugi M, Tatsuuoka T, Horikawa Y (1996). A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino) cyclopropa[b]chromen-1a-carboxylates. Biorg Med Chem Lett 6: 763-766.
2. Batchelor AM, Knöpfel T, Gasparini F, Garthwaite J (1997). Pharmacological characterization of synaptic transmission through mGluRs in rat cerebellar slices. Neuropharmacology 36: 401-403.
3. Batchelor AM, Madge DJ, Garthwaite J (1994). Synaptic activation of metabotropic glutamate receptors in the parallel fibre-Purkinje cell pathway in rat cerebellar slices. Neuroscience 63: 911-915.
4. Casabona G, Knöpfel T, Kuhn R, Gasparini F, Baumann P, Sortino MA et al. (1997). Expression and coupling to polyphosphoinositide hydrolysis of group I metabotropic glutamate receptors in early postnatal and adult rat brain. Eur J Neurosci 9: 12-17.
5. Charpak S, Gahwiler BH, Do KQ, Knöpfel T (1990). Potassium conductances in hippocampal neurons blocked by excitatory amino-acid transmitters. Nature 347: 765-767.
6. Coutinho V, Knöpfel T (2002). Metabotropic glutamate receptors: electrical and chemical signaling properties. Neuroscientist 8: 551-561.
7. Fukunaga I, Yeo CH, Batchelor AM (2007a). The mGlu1 antagonist CPCCOEt enhances the climbing fibre response in Purkinje neurones independently of glutamate receptors. Neuropharmacology 52: 450-458.
8. Fukunaga I, Yeo CH, Batchelor AM (2007b). Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices. Br J Pharmacol 151: 870-876 (this issue).
9. Knöpfel T, Kuhn R, Allgeier H (1995). Metabotropic glutamate receptors: novel targets for drug development. J Med Chem 38: 1417-1426.
10. Kohara A, Toya T, Tamura S, Watabiki T, Nagakura Y, Shitaka Y et al. (2005). Radioligand binding properties and pharmacological characterization of 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a] benzimidazole-2-carboxamide (YM-298198), a high-affinity, selective, and noncompetitive antagonist of metabotropic glutamate receptor type 1. J Pharmacol Exp Ther 315: 163-169.
11. Lavreysen H, Wouters R, Bischoff F, Nobrega Pereira S, Langlois X, Blokland S et al. (2004). JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology 47: 961-972.
12. Lingenhohl K, Olpe HR, Bendali N, Knöpfel T (1993). Phenylglycine derivatives antagonize the excitatory response to Purkinje cells to 1S,3R-ACPD: an in vivo and in vitro study. Neurosci Res 18: 229-234.
13. Masu M, Tanabe Y, Tsuchida K, Shigemoto R, Nakanishi S (1991). Sequence and expression of a metabotropic glutamate receptor. Nature 349: 760-765.
14. Nicoletti F, Bruno V, Copani A, Casabona G, Knöpfel T (1996). Metabotropic glutamate receptors: a new target for the therapy of neurodegenerative disorders? Trends Neurosci 19: 267-271.
15. Staub C, Vranesic I, Knöpfel T (1992). Responses to metabotropic glutamate receptor activation in cerebellar Purkinje cells: induction of an inward current. Eur J Neurosci 4: 832-839.
16. Steckler T, Lavreysen H, Oliveira AM, Aerts N, Van Craenendonck H, Prickaerts J et al. (2005a). Effects of mGlu1 receptor blockade on anxiety-related behaviour in the rat lick suppression test. Psychopharmacology (Berl) 179: 198-206.
17. Steckler T, Oliveira AF, Van Dyck C, Van Craenendonck H, Mateus AM, Langlois X et al. (2005b). Metabotropic glutamate receptor 1 blockade impairs acquisition and retention in a spatial Water maze task. Behav Brain Res 164: 52-60.