Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold

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Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold is …
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scholarly articleQ13442814

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P356DOI10.1016/J.BMCL.2008.05.091
P932PMC publication ID2533619
P698PubMed publication ID18550372
P5875ResearchGate publication ID5305386

P50authorAlice L. RodriguezQ67215392
Craig W. LindsleyQ67215429
P. Jeffrey ConnQ67215432
P2093author name stringSameer Sharma
P2860cites workApplication of combinatorial chemistry science on modern drug discoveryQ37065188
A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulatorsQ40374968
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activityQ44958079
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activityQ28263355
2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonistQ28374719
Pharmacology and functions of metabotropic glutamate receptorsQ29619150
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivoQ30842826
Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).Q33223813
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.Q33268568
Pharmacological agents acting at subtypes of metabotropic glutamate receptorsQ33756933
A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.Q34222874
A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrainQ34293120
A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral modelsQ34377770
Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytesQ34530165
Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP.Q34564332
P433issue14
P407language of work or nameEnglishQ1860
P921main subjectleadQ708
pharmacologyQ128406
P304page(s)4098-4101
P577publication date2008-05-29
P1433published inBioorganic & Medicinal Chemistry LettersQ2709483
P1476titleSynthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold
P478volume18

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