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Results: 1 to 20 of 74

1.

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).

Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR.

J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. Epub 2014 Sep 3.

PMID:
25147929
[PubMed - in process]
2.

Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents.

Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK.

ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. Epub 2014 Aug 19.

PMID:
25137629
[PubMed - in process]
3.

Polymorphisms in human heat shock factor-1 and analysis of potential biological consequences.

Bridges TM, Scheraga RG, Tulapurkar ME, Suffredini D, Liggett SB, Ramarathnam A, Potla R, Singh IS, Hasday JD.

Cell Stress Chaperones. 2014 Jul 16. [Epub ahead of print]

PMID:
25023647
[PubMed - as supplied by publisher]
4.

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.

Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2.

PMID:
24961642
[PubMed - in process]
5.

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.

Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW.

ChemMedChem. 2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1.

PMID:
24692176
[PubMed - in process]
6.

M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location.

Foster DJ, Gentry PR, Lizardi-Ortiz JE, Bridges TM, Wood MR, Niswender CM, Sulzer D, Lindsley CW, Xiang Z, Conn PJ.

J Neurosci. 2014 Feb 26;34(9):3253-62. doi: 10.1523/JNEUROSCI.4896-13.2014.

PMID:
24573284
[PubMed - indexed for MEDLINE]
Free PMC Article
7.

Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100.

Byun NE, Grannan M, Bubser M, Barry RL, Thompson A, Rosanelli J, Gowrishankar R, Kelm ND, Damon S, Bridges TM, Melancon BJ, Tarr JC, Brogan JT, Avison MJ, Deutch AY, Wess J, Wood MR, Lindsley CW, Gore JC, Conn PJ, Jones CK.

Neuropsychopharmacology. 2014 Jun;39(7):1578-93. doi: 10.1038/npp.2014.2. Epub 2014 Jan 20.

PMID:
24442096
[PubMed - in process]
8.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW.

J Med Chem. 2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13.

PMID:
24164599
[PubMed - indexed for MEDLINE]
9.

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9.

PMID:
24050755
[PubMed - indexed for MEDLINE]
Free PMC Article
10.

Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5.

Rodriguez AL, Tarr JC, Zhou Y, Williams R, Gregory KJ, Bridges TM, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 17 [updated 2013 Mar 22].

PMID:
24027804
[PubMed]
Books & Documents
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.

Blobaum AL, Bridges TM, Byers FW, Turlington ML, Mattmann ME, Morrison RD, Mackie C, Lavreysen H, Bartolomé JM, Macdonald GJ, Steckler T, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR, Daniels JS.

Drug Metab Dispos. 2013 Dec;41(12):2066-75. doi: 10.1124/dmd.113.052662. Epub 2013 Sep 3.

PMID:
24003250
[PubMed - indexed for MEDLINE]
12.

N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.

Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK.

J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21.

PMID:
23965381
[PubMed - indexed for MEDLINE]
Free PMC Article
13.

Dimerization of the glucan phosphatase laforin requires the participation of cysteine 329.

Sánchez-Martín P, Raththagala M, Bridges TM, Husodo S, Gentry MS, Sanz P, Romá-Mateo C.

PLoS One. 2013 Jul 26;8(7):e69523. doi: 10.1371/journal.pone.0069523. Print 2013.

PMID:
23922729
[PubMed - indexed for MEDLINE]
Free PMC Article
14.

Development and characterization of a highly selective M5 PAM probe molecule with improved potency.

Gentry PR, Bridges TM, Daniels JS, Lamsal A, Vinson PN, Niswender CM, Hodder PS, Rosen H, Conn PJ, Engers J, Lindsley CW, Wood MR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 13 [updated 2013 Mar 22].

PMID:
23885365
[PubMed]
Books & Documents
15.

Structure of the Arabidopsis glucan phosphatase like sex four2 reveals a unique mechanism for starch dephosphorylation.

Meekins DA, Guo HF, Husodo S, Paasch BC, Bridges TM, Santelia D, Kötting O, Vander Kooi CW, Gentry MS.

Plant Cell. 2013 Jun;25(6):2302-14. doi: 10.1105/tpc.113.112706. Epub 2013 Jun 28.

PMID:
23832589
[PubMed - indexed for MEDLINE]
Free PMC Article
16.

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.

Bridges TM, Rook JM, Noetzel MJ, Morrison RD, Zhou Y, Gogliotti RD, Vinson PN, Xiang Z, Jones CK, Niswender CM, Lindsley CW, Stauffer SR, Conn PJ, Daniels JS.

Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.

PMID:
23821185
[PubMed - indexed for MEDLINE]
Free PMC Article
17.

Development of the First Highly Selective mAChR 5 (M5) Positive Allosteric Modulator (PAM).

Bridges TM, Lewis LM, Weaver CD, Wood MR, Daniels JS, Conn PJ, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2013 Mar 14].

PMID:
23762960
[PubMed]
Books & Documents
18.

Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity.

Bridges TM, Niswender CM, Jones CK, Lewis LM, Weaver CD, Wood MR, Daniels JS, Conn PJ, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2013 Mar 14].

PMID:
23762955
[PubMed]
Books & Documents
19.

Pure Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction.

Zhou Y, Chun A, Gogliotti RD, Dawson ES, Vinson PN, Niswender CM, Noetzel MJ, Rook JM, Bridges TM, Daniels JS, Jones C, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 31 [updated 2013 Mar 7].

PMID:
23762950
[PubMed]
Books & Documents
20.

Discovery of a novel structural class of M4 positive allosteric modulators: Characterization of ML293, N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicotinamide, with CNS exposure in rats.

Salovich JM, Sheffler DJ, Vinson PN, Lamsal A, Utley TJ, Blobaum AL, Bridges TM, Le U, Jones CK, Wood MR, Daniels JS, Conn PJ, Engers J, Niswender CM, Lindsley CW, Hopkins CR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 2 [updated 2013 Mar 14].

PMID:
23762944
[PubMed]
Books & Documents

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