| Year |
Citation |
Score |
| 2016 |
Pero JE, Rossi MA, Kelly MJ, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, ... Jacobson MA, et al. Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI. Acs Medicinal Chemistry Letters. 7: 312-7. PMID 26985321 DOI: 10.1021/acsmedchemlett.5b00459 |
1 |
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| 2016 |
Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, ... ... Jacobson MA, et al. Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis. Bioorganic & Medicinal Chemistry Letters. PMID 26810316 DOI: 10.1016/j.bmcl.2016.01.021 |
1 |
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| 2014 |
Williams T, Jacobson MA, Kalinichev M, Rocher JP. Activation of the mGlu5 receptor for the treatment of schizophrenia and cognitive-deficit- associated disorders Topics in Medicinal Chemistry. 13: 143-182. DOI: 10.1007/7355_2014_57 |
1 |
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| 2012 |
Parmentier-Batteur S, O'Brien JA, Doran S, Nguyen SJ, Flick RB, Uslaner JM, Chen H, Finger EN, Williams TM, Jacobson MA, Hutson PH. Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration. Neuropharmacology. 62: 1453-60. PMID 21112344 DOI: 10.1016/j.neuropharm.2010.11.013 |
1 |
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| 2010 |
Garbaccio RM, Brnardic EJ, Fraley ME, Hartman GD, Hutson PH, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Small JH, Tang C, Kuo Y, Jacobson MA. Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor. Acs Medicinal Chemistry Letters. 1: 406-10. PMID 24900224 DOI: 10.1021/ml100115a |
1 |
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| 2010 |
Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, et al. 3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts. Bioorganic & Medicinal Chemistry Letters. 20: 3129-33. PMID 20409708 DOI: 10.1016/j.bmcl.2010.03.089 |
1 |
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| 2009 |
Ma L, Seager MA, Seager M, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, et al. Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proceedings of the National Academy of Sciences of the United States of America. 106: 15950-5. PMID 19717450 DOI: 10.1073/pnas.0900903106 |
1 |
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| 2009 |
Uslaner JM, Parmentier-Batteur S, Flick RB, Surles NO, Lam JS, McNaughton CH, Jacobson MA, Hutson PH. Dose-dependent effect of CDPPB, the mGluR5 positive allosteric modulator, on recognition memory is associated with GluR1 and CREB phosphorylation in the prefrontal cortex and hippocampus. Neuropharmacology. 57: 531-8. PMID 19627999 DOI: 10.1016/j.neuropharm.2009.07.022 |
1 |
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| 2009 |
Wolkenberg SE, Zhao Z, Wisnoski DD, Leister WH, O'Brien J, Lemaire W, Williams DL, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Gibson C, Ma BK, et al. Discovery of GlyT1 inhibitors with improved pharmacokinetic properties. Bioorganic & Medicinal Chemistry Letters. 19: 1492-5. PMID 19181525 DOI: 10.1016/j.bmcl.2009.01.015 |
1 |
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| 2009 |
Zhao Z, Leister WH, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Lindsley CW, Wolkenberg SE. Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors. Bioorganic & Medicinal Chemistry Letters. 19: 1488-91. PMID 19179073 DOI: 10.1016/j.bmcl.2008.12.115 |
1 |
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| 2009 |
Smith SM, Uslaner JM, Yao L, Mullins CM, Surles NO, Huszar SL, McNaughton CH, Pascarella DM, Kandebo M, Hinchliffe RM, Sparey T, Brandon NJ, Jones B, Venkatraman S, Young MB, ... ... Jacobson MA, et al. The behavioral and neurochemical effects of a novel D-amino acid oxidase inhibitor compound 8 [4H-thieno [3,2-b]pyrrole-5-carboxylic acid] and D-serine. The Journal of Pharmacology and Experimental Therapeutics. 328: 921-30. PMID 19088300 DOI: 10.1124/jpet.108.147884 |
1 |
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| 2008 |
Björklund O, Halldner-Henriksson L, Yang J, Eriksson TM, Jacobson MA, Daré E, Fredholm BB. Decreased behavioral activation following caffeine, amphetamine and darkness in A3 adenosine receptor knock-out mice. Physiology & Behavior. 95: 668-76. PMID 18930070 DOI: 10.1016/j.physbeh.2008.09.018 |
1 |
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| 2007 |
Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW. Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorganic & Medicinal Chemistry Letters. 17: 1386-91. PMID 17210250 DOI: 10.1016/j.bmcl.2006.11.081 |
1 |
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| 2006 |
Zhao Z, O'Brien JA, Lemaire W, Williams DL, Jacobson MA, Sur C, Pettibone DJ, Tiller PR, Smith S, Hartman GD, Wolkenberg SE, Lindsley CW. Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides. Bioorganic & Medicinal Chemistry Letters. 16: 5968-72. PMID 16987662 DOI: 10.1016/j.bmcl.2006.08.131 |
1 |
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| 2006 |
Lindsley CW, Zhao Z, Leister WH, O'Brien J, Lemaire W, Williams DL, Chen TB, Chang RS, Burno M, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, et al. Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides. Chemmedchem. 1: 807-11. PMID 16902933 DOI: 10.1002/cmdc.200600097 |
1 |
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| 2005 |
Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, et al. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. The Journal of Pharmacology and Experimental Therapeutics. 313: 199-206. PMID 15608073 DOI: 10.1124/jpet.104.079244 |
1 |
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| 2004 |
O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. The Journal of Pharmacology and Experimental Therapeutics. 309: 568-77. PMID 14747613 DOI: 10.1124/jpet.103.061747 |
1 |
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| 2003 |
Williams DL, O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Sur C, Duggan ME, Pettibone DJ, Conn PJ. Difference in mGluR5 interaction between positive allosteric modulators from two structural classes. Annals of the New York Academy of Sciences. 1003: 481-4. PMID 14684495 DOI: 10.1196/annals.1300.059 |
1 |
|
| 2003 |
Sur C, Mallorga PJ, Wittmann M, Jacobson MA, Pascarella D, Williams JB, Brandish PE, Pettibone DJ, Scolnick EM, Conn PJ. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proceedings of the National Academy of Sciences of the United States of America. 100: 13674-9. PMID 14595031 DOI: 10.1073/pnas.1835612100 |
1 |
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| 2003 |
Mallorga PJ, Williams JB, Jacobson M, Marques R, Chaudhary A, Conn PJ, Pettibone DJ, Sur C. Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine. Neuropharmacology. 45: 585-93. PMID 12941372 DOI: 10.1016/S0028-3908(03)00227-2 |
1 |
|
| 2003 |
O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Lindsley CW, Schaffhauser HJ, Sur C, Pettibone DJ, Conn PJ, Williams DL. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Molecular Pharmacology. 64: 731-40. PMID 12920211 DOI: 10.1124/mol.64.3.731 |
1 |
|
| 2003 |
Fedorova IM, Jacobson MA, Basile A, Jacobson KA. Behavioral characterization of mice lacking the A3 adenosine receptor: sensitivity to hypoxic neurodegeneration. Cellular and Molecular Neurobiology. 23: 431-47. PMID 12825837 DOI: 10.1023/A:1023601007518 |
1 |
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| 2003 |
Zhong H, Shlykov SG, Molina JG, Sanborn BM, Jacobson MA, Tilley SL, Blackburn MR. Activation of murine lung mast cells by the adenosine A3 receptor. Journal of Immunology (Baltimore, Md. : 1950). 171: 338-45. PMID 12817016 |
1 |
|
| 2003 |
Montesinos MC, Desai A, Delano D, Chen JF, Fink JS, Jacobson MA, Cronstein BN. Adenosine A2A or A3 receptors are required for inhibition of inflammation by methotrexate and its analog MX-68. Arthritis and Rheumatism. 48: 240-7. PMID 12528125 DOI: 10.1002/art.10712 |
1 |
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| 2003 |
Lopes LV, Rebola N, Costenla AR, Halldner L, Jacobson MA, Oliveira CR, Richardson PJ, Fredholm BB, Ribeiro JA, Cunha RA. Adenosine A3 receptors in the rat hippocampus: Lack of interaction with A1 receptors Drug Development Research. 58: 428-438. DOI: 10.1002/ddr.10188 |
1 |
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| 2002 |
Pettibone DJ, Hess JF, Hey PJ, Jacobson MA, Leviten M, Lis EV, Mallorga PJ, Pascarella DM, Snyder MA, Williams JB, Zeng Z. The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin. The Journal of Pharmacology and Experimental Therapeutics. 300: 305-13. PMID 11752130 DOI: 10.1124/jpet.300.1.305 |
1 |
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| 1999 |
Williams PD, Bock MG, Evans BE, Freidinger RM, Gallicchio SN, Guidotti MT, Jacobson MA, Kuo MS, Levy MR, Lis EV, Michelson SR, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, et al. Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency. Bioorganic & Medicinal Chemistry Letters. 9: 1311-6. PMID 10340620 DOI: 10.1016/S0960-894X(99)00181-X |
1 |
|
| 1998 |
Salvatore CA, Woyden CJ, Guidotti MT, Pettibone DJ, Jacobson MA. Cloning and expression of the rhesus monkey oxytocin receptor. Journal of Receptor and Signal Transduction Research. 18: 15-24. PMID 9493565 DOI: 10.3109/10799899809039162 |
1 |
|
| 1990 |
Near RI, Ng SC, Mudgett-Hunter M, Hudson NW, Margolies MN, Seidman JG, Haber E, Jacobson MA. Heavy and light chain contributions to antigen binding in an anti-digoxin chain recombinant antibody produced by transfection of cloned anti-digoxin antibody genes. Molecular Immunology. 27: 901-9. PMID 2120577 DOI: 10.1016/0161-5890(90)90157-U |
1 |
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| 1989 |
Jacobson MA, Forma FM, Buenaga RF, Hofmann KJ, Schultz LD, Gould RJ, Friedman PA. Expression and secretion of biologically active echistatin in Saccharomyces cerevisiae. Gene. 85: 511-6. PMID 2697646 DOI: 10.1016/0378-1119(89)90445-9 |
1 |
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| 1984 |
Jacobson MA, Colman RF. Evaluation of the intramolecular stacking of the fluorosulfonylbenzoyl derivatives of 1-N6-ethenoadenosine, adenosine, and guanosine Journal of Biological Chemistry. 259: 1454-1460. PMID 6693416 |
1 |
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| 1984 |
Jacobson MA, Colman RF. Isolation and identification of a tyrosyl peptide labeled by 5′-[p-(fluorosulfonyl)benzoyl]-1,N6-ethenoadenosine at a GTP site of glutamate dehydrogenase Biochemistry. 23: 6377-6382. PMID 6529553 DOI: 10.1021/bi00321a014 |
1 |
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| 1984 |
Jacobson MA, Colman RF. Distance relationships between the catalytic site labeled with 4-(iodoacetamido)salicylic acid and regulatory sites of glutamate dehydrogenase Biochemistry. 23: 3789-3798. PMID 6487574 DOI: 10.1021/bi00312a001 |
1 |
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| 1983 |
Jacobson MA, Colman RF. Resonance energy transfer between the adenosine 5prime;-diphosphate site of glutamate dehydrogenase and a guanosine 5′-triphosphate site containing a tyrosine labeled with 5′-[p-(Fluorosulfonyl)benzoyl]-1,N6-ethenoadenosine Biochemistry. 22: 4247-4257. PMID 6414507 DOI: 10.1021/bi00287a014 |
1 |
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| 1982 |
Jacobson MA, Colman RF. Affinity labeling of a guanosine 5′-triphosphate site of glutamate dehydrogenase by a fluorescent nucleotide analogue, 5′-[p-(fluorosulfonyl)benzoyl]-1,N6-ethenoadenosine Biochemistry. 21: 2177-2186. PMID 7093238 DOI: 10.1021/bi00538a029 |
1 |
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