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Items: 1 to 20 of 443

1.

Neuropharmacological Insight from Allosteric Modulation of mGlu Receptors.

Stansley BJ, Conn PJ.

Trends Pharmacol Sci. 2019 Feb 26. pii: S0165-6147(19)30037-9. doi: 10.1016/j.tips.2019.02.006. [Epub ahead of print] Review.

PMID:
30824180
2.

Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology.

Sengmany K, Hellyer SD, Albold S, Wang T, Conn PJ, May LT, Christopoulos A, Leach K, Gregory KJ.

Neuropharmacology. 2019 May 1;149:83-96. doi: 10.1016/j.neuropharm.2019.02.005. Epub 2019 Feb 11.

PMID:
30763654
3.

Discovery of an orally bioavailable and Central Nervous System (CNS) penetrant mGlu7 Negative Allosteric Modulator (NAM) in vivo tool compound: N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).

Reed CW, Yohn S, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.

J Med Chem. 2019 Jan 4. doi: 10.1021/acs.jmedchem.8b01810. [Epub ahead of print]

PMID:
30608678
4.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Jeffrey Conn P, Lindsley CW.

Bioorg Med Chem Lett. 2019 Feb 1;29(3):362-366. doi: 10.1016/j.bmcl.2018.12.039. Epub 2018 Dec 18.

PMID:
30580918
5.

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.

Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):342-346. doi: 10.1016/j.bmcl.2018.10.050. Epub 2018 Nov 1.

PMID:
30503632
6.

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Felts AS, Bollinger KA, Brassard CJ, Rodriguez AL, Morrison RD, Scott Daniels J, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Emmitte KA, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 1;29(1):47-50. doi: 10.1016/j.bmcl.2018.11.017. Epub 2018 Nov 10.

PMID:
30446311
7.

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

J Med Chem. 2018 Oct 31. doi: 10.1021/acs.jmedchem.8b01266. [Epub ahead of print]

PMID:
30350962
8.

Pick Your Model Wisely: Understanding the Negative Symptoms of Schizophrenia in Rodent Models.

Yohn SE, Conn PJ.

ACS Chem Neurosci. 2018 Oct 22. doi: 10.1021/acschemneuro.8b00553. [Epub ahead of print]

PMID:
30346132
9.

Mechanisms underlying prelimbic prefrontal cortex mGlu3/mGlu5-dependent plasticity and reversal learning deficits following acute stress.

Joffe ME, Santiago CI, Stansley BJ, Maksymetz J, Gogliotti RG, Engers JL, Nicoletti F, Lindsley CW, Conn PJ.

Neuropharmacology. 2019 Jan;144:19-28. doi: 10.1016/j.neuropharm.2018.10.013. Epub 2018 Oct 13.

PMID:
30326237
10.

VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events.

Engers JL, Childress ES, Long MF, Capstick RA, Luscombe VB, Cho HP, Dickerson JW, Rook JM, Blobaum AL, Niswender CM, Engers DW, Conn PJ, Lindsley CW.

ACS Med Chem Lett. 2018 Sep 4;9(9):917-922. doi: 10.1021/acsmedchemlett.8b00261. eCollection 2018 Sep 13.

PMID:
30258541
11.

The discovery, SAR and biological characterization of a novel series of 6-((1H-pyrazolo[4,3-b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

Bollinger S, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

J Med Chem. 2018 Sep 24. doi: 10.1021/acs.jmedchem.8b00994. [Epub ahead of print]

PMID:
30247901
12.

Antidepressant potential of metabotropic glutamate receptor mGlu2 and mGlu3 negative allosteric modulators.

Joffe ME, Conn PJ.

Neuropsychopharmacology. 2019 Jan;44(1):214-236. doi: 10.1038/s41386-018-0192-8. No abstract available.

PMID:
30202048
13.

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.

Yohn SE, Foster DJ, Covey DP, Moehle MS, Galbraith J, Garcia-Barrantes PM, Cho HP, Bubser M, Blobaum AL, Joffe ME, Cheer JF, Jones CK, Lindsley CW, Conn PJ.

Mol Psychiatry. 2018 Aug 16. doi: 10.1038/s41380-018-0206-2. [Epub ahead of print]

PMID:
30116027
14.

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators.

Engers JL, Bender AM, Kalbfleisch JJ, Cho HP, Lingenfelter KS, Luscombe VB, Han C, Melancon BJ, Blobaum AL, Dickerson JW, Rook JM, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Aug 9. doi: 10.1021/acschemneuro.8b00311. [Epub ahead of print]

PMID:
30086237
15.

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].

Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014. doi: 10.1016/j.bmcl.2018.07.022. Epub 2018 Jul 31. No abstract available.

PMID:
30076050
16.

Mutual activation of glutamatergic mGlu4 and muscarinic M4 receptors reverses schizophrenia-related changes in rodents.

Cieślik P, Woźniak M, Rook JM, Tantawy MN, Conn PJ, Acher F, Tokarski K, Kusek M, Pilc A, Wierońska JM.

Psychopharmacology (Berl). 2018 Oct;235(10):2897-2913. doi: 10.1007/s00213-018-4980-y. Epub 2018 Jul 27.

17.

The mGluR5 positive allosteric modulator VU0409551 improves synaptic plasticity and memory of a mouse model of Huntington's disease.

Doria JG, de Souza JM, Silva FR, Olmo IG, Carvalho TG, Alves-Silva J, Ferreira-Vieira TH, Santos JT, Xavier CQS, Silva NC, Maciel EMA, Conn PJ, Ribeiro FM.

J Neurochem. 2018 Oct;147(2):222-239. doi: 10.1111/jnc.14555. Epub 2018 Sep 11.

PMID:
30028018
18.

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.

Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

Bioorg Med Chem Lett. 2018 Aug 15;28(15):2641-2646. doi: 10.1016/j.bmcl.2018.06.034. Epub 2018 Jun 19.

PMID:
29958762
19.

Inhibition of endocannabinoid degradation rectifies motivational and dopaminergic deficits in the Q175 mouse model of Huntington's disease.

Covey DP, Dantrassy HM, Yohn SE, Castro A, Conn PJ, Mateo Y, Cheer JF.

Neuropsychopharmacology. 2018 Sep;43(10):2056-2063. doi: 10.1038/s41386-018-0107-8. Epub 2018 Jun 1.

PMID:
29925886
20.

Metabotropic Glutamate Receptors in Alcohol Use Disorder: Physiology, Plasticity, and Promising Pharmacotherapies.

Joffe ME, Centanni SW, Jaramillo AA, Winder DG, Conn PJ.

ACS Chem Neurosci. 2018 Sep 19;9(9):2188-2204. doi: 10.1021/acschemneuro.8b00200. Epub 2018 Jun 8.

PMID:
29792024

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