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Items: 35

1.

fMRI study of the role of glutamate NMDA receptor in the olfactory processing in monkeys.

Zhao F, Holahan MA, Wang X, Uslaner JM, Houghton AK, Evelhoch JL, Winkelmann CT, Hines CDG.

PLoS One. 2018 Jun 5;13(6):e0198395. doi: 10.1371/journal.pone.0198395. eCollection 2018.

2.

Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy.

Myers RW, Guan HP, Ehrhart J, Petrov A, Prahalada S, Tozzo E, Yang X, Kurtz MM, Trujillo M, Gonzalez Trotter D, Feng D, Xu S, Eiermann G, Holahan MA, Rubins D, Conarello S, Niu X, Souza SC, Miller C, Liu J, Lu K, Feng W, Li Y, Painter RE, Milligan JA, He H, Liu F, Ogawa A, Wisniewski D, Rohm RJ, Wang L, Bunzel M, Qian Y, Zhu W, Wang H, Bennet B, LaFranco Scheuch L, Fernandez GE, Li C, Klimas M, Zhou G, van Heek M, Biftu T, Weber A, Kelley DE, Thornberry N, Erion MD, Kemp DM, Sebhat IK.

Science. 2017 Aug 4;357(6350):507-511. doi: 10.1126/science.aah5582. Epub 2017 Jul 13.

PMID:
28705990
3.

Functional imaging of olfaction by CBV fMRI in monkeys: insight into the role of olfactory bulb in habituation.

Zhao F, Holahan MA, Houghton AK, Hargreaves R, Evelhoch JL, Winkelmann CT, Williams DS.

Neuroimage. 2015 Feb 1;106:364-72. doi: 10.1016/j.neuroimage.2014.12.001. Epub 2014 Dec 10.

PMID:
25498426
4.

Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.

Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ.

J Neurosci. 2010 May 12;30(19):6743-50. doi: 10.1523/JNEUROSCI.1381-10.2010.

5.

Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.

Zhu H, Young MB, Nantermet PG, Graham SL, Colussi D, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Shi XP, Tugusheva K, Holahan MA, Michener MS, Cook JJ, Simon A, Hazuda DJ, Vacca JP, Rajapakse HA.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11.

PMID:
20122828
6.

Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.

Nantermet PG, Rajapakse HA, Stanton MG, Stauffer SR, Barrow JC, Gregro AR, Moore KP, Steinbeiser MA, Swestock J, Selnick HG, Graham SL, McGaughey GB, Colussi D, Lai MT, Sankaranarayanan S, Simon AJ, Munshi S, Cook JJ, Holahan MA, Michener MS, Vacca JP.

ChemMedChem. 2009 Jan;4(1):37-40. doi: 10.1002/cmdc.200800308. No abstract available.

PMID:
19085994
7.

First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.

Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai MT, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi XP, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ.

J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14.

PMID:
18854490
8.

Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Wood MR, Schirripa KM, Kim JJ, Kuduk SD, Chang RK, Di Marco CN, DiPardo RM, Wan BL, Murphy KL, Ransom RW, Chang RS, Holahan MA, Cook JJ, Lemaire W, Mosser SD, Bednar RA, Tang C, Prueksaritanont T, Wallace AA, Mei Q, Yu J, Bohn DL, Clayton FC, Adarayn ED, Sitko GR, Leonard YM, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):716-20. Epub 2007 Nov 19.

PMID:
18061443
9.

Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

Kuduk SD, Di Marco CN, Chang RK, Wood MR, Schirripa KM, Kim JJ, Wai JM, DiPardo RM, Murphy KL, Ransom RW, Harrell CM, Reiss DR, Holahan MA, Cook J, Hess JF, Sain N, Urban MO, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

J Med Chem. 2007 Jan 25;50(2):272-82.

PMID:
17228869
10.

Demonstration of enhanced endogenous fibrinolysis in thrombin activatable fibrinolysis inhibitor-deficient mice.

Mao SS, Holahan MA, Bailey C, Wu G, Colussi D, Carroll SS, Cook JJ.

Blood Coagul Fibrinolysis. 2005 Sep;16(6):407-15.

PMID:
16093731
11.

9-hydroxyazafluorenes and their use in thrombin inhibitors.

Stauffer KJ, Williams PD, Selnick HG, Nantermet PG, Newton CL, Homnick CF, Zrada MM, Lewis SD, Lucas BJ, Krueger JA, Pietrak BL, Lyle EA, Singh R, Miller-Stein C, White RB, Wong B, Wallace AA, Sitko GR, Cook JJ, Holahan MA, Stranieri-Michener M, Leonard YM, Lynch JJ Jr, McMasters DR, Yan Y.

J Med Chem. 2005 Apr 7;48(7):2282-93.

PMID:
15801822
12.

An alternative method of chronic cerebrospinal fluid collection via the cisterna magna in conscious rhesus monkeys.

Gilberto DB, Zeoli AH, Szczerba PJ, Gehret JR, Holahan MA, Sitko GR, Johnson CA, Cook JJ, Motzel SL.

Contemp Top Lab Anim Sci. 2003 Jul;42(4):53-9.

PMID:
12906404
13.

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.

Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP.

J Med Chem. 2003 Feb 13;46(4):461-73.

PMID:
12570369
15.

Fibrinogen receptor antagonist-induced thrombocytopenia in chimpanzee and rhesus monkey associated with preexisting drug-dependent antibodies to platelet glycoprotein IIb/IIIa.

Bednar B, Cook JJ, Holahan MA, Cunningham ME, Jumes PA, Bednar RA, Hartman GD, Gould RJ.

Blood. 1999 Jul 15;94(2):587-99.

PMID:
10397726
16.

Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.

Egbertson MS, Cook JJ, Bednar B, Prugh JD, Bednar RA, Gaul SL, Gould RJ, Hartman GD, Homnick CF, Holahan MA, Libby LA, Lynch JJ Jr, Lynch RJ, Sitko GR, Stranieri MT, Vassallo LM.

J Med Chem. 1999 Jul 1;42(13):2409-21. Erratum in: J Med Chem 1999 Sep 23;42(19):4014.

PMID:
10395482
17.

Antithrombotic efficacy of thrombin inhibitor L-374,087: intravenous activity in a primate model of venous thrombus extension and oral activity in a canine model of primary venous and coronary artery thrombosis.

Cook JJ, Gardell SJ, Holahan MA, Sitko GR, Stump GL, Wallace AA, Gilberto DB, Hare TR, Krueger JA, Dyer DL, Sanderson PE, Vacca JP, Shafer JA, Lynch JJ Jr.

J Pharmacol Exp Ther. 1999 Apr;289(1):503-10.

PMID:
10087043
18.

Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.

Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP.

J Med Chem. 1998 Aug 13;41(17):3210-9.

PMID:
9703466
19.

Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.

Brady SF, Stauffer KJ, Lumma WC, Smith GM, Ramjit HG, Lewis SD, Lucas BJ, Gardell SJ, Lyle EA, Appleby SD, Cook JJ, Holahan MA, Stranieri MT, Lynch JJ Jr, Lin JH, Chen IW, Vastag K, Naylor-Olsen AM, Vacca JP.

J Med Chem. 1998 Jan 29;41(3):401-6.

PMID:
9464370
20.

Effects of pentobarbital on pharmacokinetics and pharmacodynamics of a potent fibrinogen receptor antagonist, L-734,217, in dogs.

Prueksaritanont T, Stranieri MT, Hand EL, Ellis JD, Holahan MA, Sitko GR, Cook JJ.

Biopharm Drug Dispos. 1997 Nov;18(8):649-63.

PMID:
9373723
21.

Nonpeptide glycoprotein IIb/IIIa inhibitors: 14: oral antithrombotic efficacy of L-738,167 in a conscious canine model of coronary artery electrolytic injury.

Cook JJ, Glass JD, Sitko GR, Holahan MA, Stupienski RF 3rd, Wallace AA, Stump GL, Hand EL, Askew BC, Hartman GD, Gould RJ, Lynch JJ Jr.

Circulation. 1997 Aug 5;96(3):949-58.

PMID:
9264506
22.

Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.

Askew BC, Bednar RA, Bednar B, Claremon DA, Cook JJ, McIntyre CJ, Hunt CA, Gould RJ, Lynch RJ, Lynch JJ Jr, Gaul SL, Stranieri MT, Sitko GR, Holahan MA, Glass JD, Hamill T, Gorham LM, Prueksaritanont T, Baldwin JJ, Hartman GD.

J Med Chem. 1997 Jun 6;40(12):1779-88.

PMID:
9191954
23.

Nonpeptide glycoprotein IIb/IIIa inhibitors. 15. Antithrombotic efficacy of L-738,167, a long-acting GPIIb/IIIa antagonist, correlates with inhibition of adenosine diphosphate-induced platelet aggregation but not with bleeding time prolongation.

Cook JJ, Sitko GR, Holahan MA, Stranieri MT, Glass JD, Askew BC, McIntyre CJ, Claremon DA, Baldwin JJ, Hartman GD, Gould RJ, Lynch JJ Jr.

J Pharmacol Exp Ther. 1997 May;281(2):677-89.

PMID:
9152373
24.

Non-peptide glycoprotein IIb/IIIa antagonists. 11. Design and in vivo evaluation of 3,4-dihydro-1 (1H)-isoquinolinone-based antagonists and ethyl ester prodrugs.

Hutchinson JH, Cook JJ, Brashear KM, Breslin MJ, Glass JD, Gould RJ, Halczenko W, Holahan MA, Lynch RJ, Sitko GR, Stranieri MT, Hartman GD.

J Med Chem. 1996 Nov 8;39(23):4583-91.

PMID:
8917647
25.

Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217.

Cook JJ, Holahan MA, Lyle EA, Ramjit DR, Sitko GR, Stranieri MT, Stupienski RF 3rd, Wallace AA, Hand EL, Gehret JR, Kothstein T, Drag MD, McCormick GY, Perkins JJ, Ihle NC, Duggan ME, Hartman GD, Gould RJ, Lynch JJ Jr.

J Pharmacol Exp Ther. 1996 Jul;278(1):62-73.

PMID:
8764336
26.

Investigation of (Oxodioxolenyl)methyl carbamates as nonchiral bioreversible prodrug moieties for chiral amines.

Alexander J, Bindra DS, Glass JD, Holahan MA, Renyer ML, Rork GS, Sitko GR, Stranieri MT, Stupienski RF, Veerapanane H, Cook JJ.

J Med Chem. 1996 Jan 19;39(2):480-6.

PMID:
8558516
27.

Nonpeptide glycoprotein IIb/IIIa inhibitors. 5. Antithrombotic effects of MK-0383.

Lynch JJ Jr, Cook JJ, Sitko GR, Holahan MA, Ramjit DR, Mellott MJ, Stranieri MT, Stabilito II, Zhang G, Lynch RJ, et al.

J Pharmacol Exp Ther. 1995 Jan;272(1):20-32.

PMID:
7815334
28.

Antithrombotic effects of MK-0852, a platelet fibrinogen receptor antagonist, in canine models of thrombosis.

Ramjit DR, Lynch JJ Jr, Sitko GR, Mellott MJ, Holahan MA, Stabilito II, Stranieri MT, Zhang G, Lynch RJ, Manno PD, et al.

J Pharmacol Exp Ther. 1993 Sep;266(3):1501-11.

PMID:
8371153
29.

Effect of E-4031, a class III antiarrhythmic agent, on experimental infarct size in a canine model of myocardial ischemia-reperfusion injury.

Holahan MA, Stranieri MT, Stabilito II, Lynch JJ Jr.

J Cardiovasc Pharmacol. 1992 Jun;19(6):892-8.

PMID:
1376809
31.

Vampire bat salivary plasminogen activator promotes rapid and sustained reperfusion without concomitant systemic plasminogen activation in a canine model of arterial thrombosis.

Mellott MJ, Stabilito II, Holahan MA, Cuca GC, Wang S, Li P, Barrett JS, Lynch JJ, Gardell SJ.

Arterioscler Thromb. 1992 Feb;12(2):212-21.

PMID:
1371932
33.

Effects of dietary fish oil on cardiac responsiveness to adrenoceptor stimulation.

Reibel DK, Holahan MA, Hock CE.

Am J Physiol. 1988 Mar;254(3 Pt 2):H494-9.

PMID:
3348428
34.

Dietary oils: effects on lethal superior mesenteric artery occlusion shock in the rat.

Hock CE, Beck LD, Holahan MA, Reibel DK.

Prog Clin Biol Res. 1988;264:425-31. No abstract available.

PMID:
3380843
35.

Effect of dietary fish oil on myocardial phospholipids and myocardial ischemic damage.

Hock CE, Holahan MA, Reibel DK.

Am J Physiol. 1987 Mar;252(3 Pt 2):H554-60.

PMID:
3826400

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