Detalles de la búsqueda
1.
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Bioorg Med Chem Lett
; 28(10): 1679-1685, 2018 06 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29705142
2.
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Bioorg Med Chem Lett
; 27(21): 4858-4866, 2017 11 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28958625
3.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.
Bioorg Med Chem Lett
; 27(13): 2990-2995, 2017 07 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28522253
4.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.
Bioorg Med Chem Lett
; 27(23): 5179-5184, 2017 12 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29089231
5.
Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.
Bioorg Med Chem Lett
; 27(11): 2296-2301, 2017 06 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28442253
6.
Evaluating the Disposition of a Mixed Aldehyde Oxidase/Cytochrome P450 Substrate in Rats with Attenuated P450 Activity.
Drug Metab Dispos
; 44(8): 1296-303, 2016 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-26936972
7.
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.
Bioorg Med Chem Lett
; 26(8): 1894-900, 2016 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26988308
8.
A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo.
Drug Metab Dispos
; 43(11): 1718-26, 2015 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-26265743
9.
Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.
Bioorg Med Chem Lett
; 25(3): 690-4, 2015 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25542588
10.
Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bioorg Med Chem Lett
; 24(15): 3307-14, 2014 Aug 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-24969015
11.
Heterotropic activation of the midazolam hydroxylase activity of CYP3A by a positive allosteric modulator of mGlu5: in vitro to in vivo translation and potential impact on clinically relevant drug-drug interactions.
Drug Metab Dispos
; 41(12): 2066-75, 2013 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-24003250
12.
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.
Bioorg Med Chem Lett
; 23(13): 3713-8, 2013 Jul 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23727046
13.
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bioorg Med Chem Lett
; 23(21): 5779-85, 2013 Nov 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-24074843
14.
Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184].
Bioorg Med Chem Lett
; 28(17): 3014, 2018 09 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-30076050
15.
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
Drug Metab Dispos
; 40(9): 1834-45, 2012 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-22711749
16.
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
J Med Chem
; 60(12): 5072-5085, 2017 06 22.
Artículo
en Inglés
| MEDLINE | ID: mdl-28530802
17.
Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects.
Neuropsychopharmacology
; 41(4): 1166-78, 2016 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-26315507
18.
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.
J Med Chem
; 58(20): 7959-71, 2015 Oct 22.
Artículo
en Inglés
| MEDLINE | ID: mdl-26426481
19.
Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.
J Med Chem
; 58(22): 9027-40, 2015 Nov 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-26524606
20.
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.
J Med Chem
; 58(18): 7485-500, 2015 Sep 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-26335039