113 related articles for article (PubMed ID: 16278192)
1. In vitro microsomal metabolic studies on a selective mGluR5 antagonist MTEP: characterization of in vitro metabolites and identification of a novel thiazole ring opening aldehyde metabolite.
Yang X; Chen W
Xenobiotica; 2005 Aug; 35(8):797-809. PubMed ID: 16278192
[TBL] [Abstract][Full Text] [Related]
2. In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4-yl) ethynyl]-pyridine (MTEP).
Green MD; Yang X; Cramer M; King CD
Neurosci Lett; 2006 Jan; 391(3):91-5. PubMed ID: 16153770
[TBL] [Abstract][Full Text] [Related]
3. A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif.
Kalgutkar AS; Driscoll J; Zhao SX; Walker GS; Shepard RM; Soglia JR; Atherton J; Yu L; Mutlib AE; Munchhof MJ; Reiter LA; Jones CS; Doty JL; Trevena KA; Shaffer CL; Ripp SL
Chem Res Toxicol; 2007 Dec; 20(12):1954-65. PubMed ID: 17935300
[TBL] [Abstract][Full Text] [Related]
4. [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.
Anderson JJ; Rao SP; Rowe B; Giracello DR; Holtz G; Chapman DF; Tehrani L; Bradbury MJ; Cosford ND; Varney MA
J Pharmacol Exp Ther; 2002 Dec; 303(3):1044-51. PubMed ID: 12438526
[TBL] [Abstract][Full Text] [Related]
5. Physical and crystallographic characterisation of the mGlu5 antagonist MTEP and its monohydrochloride.
McIldowie MJ; Gandy MN; Skelton BW; Brotchie JM; Koutsantonis GA; Spackman MA; Piggott MJ
J Pharm Sci; 2010 Jan; 99(1):234-45. PubMed ID: 19499574
[TBL] [Abstract][Full Text] [Related]
6. Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors.
Lea PM; Movsesyan VA; Faden AI
Br J Pharmacol; 2005 Jun; 145(4):527-34. PubMed ID: 15821750
[TBL] [Abstract][Full Text] [Related]
7. Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Iso Y; Grajkowska E; Wroblewski JT; Davis J; Goeders NE; Johnson KM; Sanker S; Roth BL; Tueckmantel W; Kozikowski AP
J Med Chem; 2006 Feb; 49(3):1080-100. PubMed ID: 16451073
[TBL] [Abstract][Full Text] [Related]
8. The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety.
Busse CS; Brodkin J; Tattersall D; Anderson JJ; Warren N; Tehrani L; Bristow LJ; Varney MA; Cosford ND
Neuropsychopharmacology; 2004 Nov; 29(11):1971-9. PubMed ID: 15305166
[TBL] [Abstract][Full Text] [Related]
9. In vitro metabolism and covalent binding of enol-carboxamide derivatives and anti-inflammatory agents sudoxicam and meloxicam: insights into the hepatotoxicity of sudoxicam.
Obach RS; Kalgutkar AS; Ryder TF; Walker GS
Chem Res Toxicol; 2008 Sep; 21(9):1890-9. PubMed ID: 18707140
[TBL] [Abstract][Full Text] [Related]
10. The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles.
Varty GB; Grilli M; Forlani A; Fredduzzi S; Grzelak ME; Guthrie DH; Hodgson RA; Lu SX; Nicolussi E; Pond AJ; Parker EM; Hunter JC; Higgins GA; Reggiani A; Bertorelli R
Psychopharmacology (Berl); 2005 Apr; 179(1):207-17. PubMed ID: 15682298
[TBL] [Abstract][Full Text] [Related]
11. In vitro metabolism of MK-0767 [(+/-)-5-[(2,4-dioxothiazolidin-5-yl)methyl]-2-methoxy-N-[[(4-trifluoromethyl)-phenyl] methyl]benzamide], a peroxisome proliferator-activated receptor alpha/gamma agonist. II. Identification of metabolites by liquid chromatography-tandem mass spectrometry.
Liu DQ; Karanam BV; Doss GA; Sidler RR; Vincent SH; Hop CE
Drug Metab Dispos; 2004 Sep; 32(9):1023-31. PubMed ID: 15319345
[TBL] [Abstract][Full Text] [Related]
12. mGluR5 antagonist-induced psychoactive properties: MTEP drug discrimination, a pharmacologically selective non-NMDA effect with apparent lack of reinforcing properties.
Swedberg MD; Ellgren M; Raboisson P
J Pharmacol Exp Ther; 2014 Apr; 349(1):155-64. PubMed ID: 24472725
[TBL] [Abstract][Full Text] [Related]
13. Reactive metabolite trapping studies on imidazo- and 2-methylimidazo[2,1-b]thiazole-based inverse agonists of the ghrelin receptor.
Kalgutkar AS; Ryder TF; Walker GS; Orr ST; Cabral S; Goosen TC; Lapham K; Eng H
Drug Metab Dispos; 2013 Jul; 41(7):1375-88. PubMed ID: 23610086
[TBL] [Abstract][Full Text] [Related]
14. The metabotropic glutamate 5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine reduces ethanol self-administration in multiple strains of alcohol-preferring rats and regulates olfactory glutamatergic systems.
Cowen MS; Djouma E; Lawrence AJ
J Pharmacol Exp Ther; 2005 Nov; 315(2):590-600. PubMed ID: 16014750
[TBL] [Abstract][Full Text] [Related]
15. In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine).
Anderson JJ; Bradbury MJ; Giracello DR; Chapman DF; Holtz G; Roppe J; King C; Cosford ND; Varney MA
Eur J Pharmacol; 2003 Jul; 473(1):35-40. PubMed ID: 12877935
[TBL] [Abstract][Full Text] [Related]
16. Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice.
Bradbury MJ; Campbell U; Giracello D; Chapman D; King C; Tehrani L; Cosford ND; Anderson J; Varney MA; Strack AM
J Pharmacol Exp Ther; 2005 Apr; 313(1):395-402. PubMed ID: 15590770
[TBL] [Abstract][Full Text] [Related]
17. Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
Kulkarni SS; Newman AH
Bioorg Med Chem Lett; 2007 Jun; 17(11):2987-91. PubMed ID: 17446071
[TBL] [Abstract][Full Text] [Related]
18. Inhibition of human hepatic CYP isoforms by mGluR5 antagonists.
Green MD; Jiang X; King CD
Life Sci; 2004 Jul; 75(8):947-53. PubMed ID: 15193955
[TBL] [Abstract][Full Text] [Related]
19. Neuroprotective effects of MTEP, a selective mGluR5 antagonists and neuropeptide Y on the kainate-induced toxicity in primary neuronal cultures.
Domin H; Kajta M; Smiałowska M
Pharmacol Rep; 2006; 58(6):846-58. PubMed ID: 17220542
[TBL] [Abstract][Full Text] [Related]
20. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects.
Swedberg MD; Raboisson P
J Pharmacol Exp Ther; 2014 Aug; 350(2):212-22. PubMed ID: 24876235
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
