[3H]methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: In vitro and in vivo characterization

Journal of Pharmacology and Experimental Therapeutics

Volumn 303, Issue 3, 2002, Pages 1044-1051

  Anderson, Jeffery J ^a   Rao, Sara P ^a   Rowe, Blake ^a   Giracello, Darlene R ^a   Holtz, Greg ^a   Chapman, Deborah F ^a   Tehrani, Lida ^a   Bradbury, Margaret J ^a   Cosford, Nicholas D P ^a   Varney, Mark A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 CHLORO 5 HYDROXYPHENYLGLYCINE; 2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; BRAIN RECEPTOR; METABOTROPIC RECEPTOR; METABOTROPIC RECEPTOR AGONIST; METABOTROPIC RECEPTOR ANTAGONIST; METHOXYMETHYL 3 [(2 METHYL 1,3 THIAZOL 4 YL)ETHYNYL]PYRIDINE; METHOXYMETHYL 3 [(2 METHYL 1,3 THIAZOL 4 YL)ETHYNYL]PYRIDINE H 3; PHOSPHATIDYLINOSITIDE; RADIOLIGAND; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG; 6 METHYL 2 (PHENYLETHYNYL)PYRIDINE; 6-METHYL-2-(PHENYLETHYNYL)PYRIDINE; AMINO ACID RECEPTOR BLOCKING AGENT; METABOTROPIC RECEPTOR 5; METHOXYMETHYL 3 ((2 METHYL 1,3 THIAZOL 4 YL)ETHYNYL)PYRIDINE; METHOXYMETHYL-3-((2-METHYL-1,3-THIAZOL-4-YL)ETHYNYL)PYRIDINE; PYRIDINE DERIVATIVE; THIAZOLE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN MEMBRANE; CEREBELLUM; CONTROLLED STUDY; DOSE RESPONSE; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; FOREBRAIN; GENE DELETION; HIPPOCAMPUS; HYDROLYSIS; IC 50; IN VITRO STUDY; IN VIVO STUDY; ISOTOPE LABELING; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; ANIMAL; BINDING SITE; BRAIN; CHEMISTRY; COMPARATIVE STUDY; DRUG ANTAGONISM; METABOLISM; PHYSIOLOGY; SPRAGUE DAWLEY RAT;

ANIMALS; BINDING SITES; BRAIN; CEREBELLUM; EXCITATORY AMINO ACID ANTAGONISTS; HIPPOCAMPUS; MALE; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, METABOTROPIC GLUTAMATE; THIAZOLES;

EID: 0036882079     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.102.040618     Document Type: Article

References (41)

1. 3H]Ro 15-1788 binding reflect selectivity for alpha 1 versus alpha 2 and alpha 3 subunit-containing GABAA receptors. Neuropsychopharmacology 20:255-262.
2. 5 on acute nociceptive transmission. Brain Res 871:223-233.
3. Brodkin J, Busse C, Sukoff SJ, and Varney MA (2002) Anxiolytic-like activity of the mGluR5 antagonist MPEP: A comparison with diazepam and buspirone. Pharmacol Biochem Behav 73:359-366.
4. Conn PJ and Pin JP (1997) Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol 37:205-237.
5. Cosford NDP, Roppe J, Tehrani L, Schweiger E, Seiders TJ, Rao S, and Varney MA (2002) Potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu 5) receptor. Bioorg Med Chem Lett, in press.
6. Fisher K and Coderre TJ (1996) Comparison of nociceptive effects produced by intrathecal administration of mGluR agonists. Neuroreport 7:2743-2747.
7. Fisher K and Coderre TJ (1998) Hyperalgesia and allodynia induced by intrathecal (R,S)-dihydroxyphenylglycine in rats. Neuroreport 9:1169-1172.
8. Freedman SB, Harley EA, and Patel S (1989) Direct measurement of muscarinic agents in the central nervous system of mice using ex vivo binding. Eur J Pharmacol 174:253-260.
9. 3H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5. Bioorg Med Chem Lett 12:407-409.
10. Gasparini F, Lingenhohl K, Stoehr N, Flor PJ, Heinrich M, Vranesic I, Biollaz M, Allgeier H, Heckendorn R, Urwyler S, et al. (1999) 2-Methyl-6-(phenylethynyl)pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist. Neuropharmacology 38:1493-1503.
11. 3H]Ro 15-1788. Life Sci 37:345-355.
12. Jia H, Rustioni A, and Valtschanoff JG (1999) Metabotropic glutamate receptors in superficial laminae of the rat dorsal horn. J Comp Neurol 410:627-642.
13. Johnson MP, Chamberlain M, and Kelly GM (1999) Phosphoinositide hydrolysis in vivo with group I metabotropic glutamate receptor agonists. Brain Res 821:539-545.
14. Karim F, Wang CC, and Gereau RWT (2001) Metabotropic glutamate receptor subtypes 1 and 5 are activators of extracellular signal-regulated kinase signaling required for inflammatory pain in mice. J Neurosci 21:3771-3779.
15. Laemmli UK (1970) Cleavage of structural proteins during the assembly of the head of bacteriophage T4. Nature (Lond) 227:680-685.
16. 3H]WAY 100635 in the mouse. Eur J Pharmacol 271:505-514.
17. Lu YM, Jia Z, Janus C, Henderson JT, Gerlai R, Wojtowicz JM, and Roder JC (1997) Mice lacking metabotropic glutamate receptor 5 show impaired learning and reduced CA1 long-term potentiation (LTP) but normal CA3 LTP. J Neurosci 17:5196-5205.
18. Martin LJ, Blackstone CD, Huganir RL, and Price DL (1992) Cellular localization of a metabotropic glutamate receptor in rat brain. Neuron 9:259-270.
19. 3H]MK-801 binding to NMDA receptors in vivo and in vitro. Eur J Pharmacol 397:263-270.
20. 3H]dicarboxycyclopropyl)glycine binding in rat brain. J Neurochem 71:2558-2564.
21. 3H]Quisqualate binding to recombinant rat metabotropic glutamate la and 5a receptors and to rat and human brain sections. J Neurochem 75:2590-2601.
22. Nakanishi S (1992) Molecular diversity of the glutamate receptors. Clin Neuropharmacol 15 (Suppl 1):4A-5A.
23. O'Leary DM, Movsesyan V, Vicini S, and Faden AI (2000) Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism. Br J Pharmacol 131:1429-1437.
24. Pagáno A, Ruegg D, Litschig S, Stoehr N, Stierlin C, Heinrich M, Floersheim P, Prezeau L, Carroll F, Pin JP, et al. (2000) The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan [b] chromen-1α-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors. J Biol Chem 75:33750-33758.
25. Patel S and Freedman SB (1994) The muscarinic receptor agonist L-658,903 modulates the in vivo accumulation of inositol monophosphates in mouse brain. Eur J Pharmacol 267:329-334.
26. Paxinos G and Watson C (1986) The Rat Brain in Stereotaxic Coordinates, Academic Press, Sydney.
27. Pin JP and Duvoisin R (1995) The metabotropic glutamate receptors: Structure and functions. Neuropharmacology 34:1-26.
28. 3H]MK-801 binding to the N-methyl-D-aspartate receptor-ion channel complex by L-glutamate, glycine and polyamines. J Neurochem 51:830-836.
29. Romano C, Sesma MA, McDonald CT, O'Malley K, Van den Pol AN, and Olney JW (1995) Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain. J Comp Neurol 355:455-469.
30. 3H]LY354740, in rat brain. Mol Pharmacol 53:228-233.
31. Schoepp DD, Jane DE, and Monn JA (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38:1431-1476.
32. Schulz B, Fendt M, Gasparini F, Lingenhohl K, Kuhn R, and Koch M (2001) The metabotropic glutamate receptor antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) blocks fear conditioning in rats. Neuropharmacology 41:1-7.
33. Shigemoto R, Nomura S, Ohishi H, Sugihara H, Nakanishi S, and Mizuno N (1993) Immunohistochemical localization of a metabotropic glutamate receptor, mGluR5, in the rat brain. Neurosci Lett 163:53-57.
34. 5 receptors and CNS disorders. Trends Pharmacol Sci 22:331-337.
35. Spooren WP, Vassout A, Neijt HC, Kuhn R, Gasparini F, Roux S, Porsolt RD, and Gentsch C (2000) Anxialytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine in rodents. J Pharmacol Exp Ther 295:1267-1275.
36. Sumiyoshi T, Kido H, Sakamoto H, Urasaki K, Suzuki K, Yamaguchi N, Mori H, Shiba K, and Yokogawa K (1994) In vivo dapamine-D2 and serotonin-5-HT2 receptor binding study of risperidone and haloperidol. Pharmacol Biochem Behav 47:553-557.
37. Tatarczynska E, Klodzinska A, Chojnacka-Wojcik E, Palucha A, Gasparini F, Kuhn R, and Pilc A (2001) Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist. Br J Pharmacol 132:1423-1430.
38. Varney MA, Cosford ND, Jachec C, Rao SP, Sacaan A, Lin FF, Bleicher L, Santori EM, Flor PJ, Allgeier H, et al. (1999) SIB-1757 and SIB-1893: Selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J Pharmacol Exp Ther 290:170-181.
39. Walker K, Bowes M, Panesar M, Davis A, Gentry C, Kesingland A, Gasparini F, Spooren W, Stoehr N, Pagano A, et al. (2001a) Metabotropic glutamate receptor subtype 5 (mGlu5) and nociceptive function. I. Selective blockade of mGlu5 receptors in models of acute, persistent and chronic pain. Neuropharmacology 40:1-9.
40. Walker K, Reeve A, Bowes M, Winter J, Wotherspoon G, Davis A, Schmid P, Gasparini F, Kuhn R, and Urban L (2001b) mGlu5 receptors and nociceptive function II. mGlu5 receptors functionally expressed on peripheral sensory neurones mediate inflammatory hyperalgesia. Neuropharmacology 40:10-19.
41. 3H]LY341495 binding to group II metabotropic glutamate receptors in rat brain. J Pharmacol Exp Ther 298:453-460.