1. 1
Curriculum Vitae -- Yu-Wen Li
Genetically-Defined Diseases, Research & Development, Bristol-Myers Squibb Company
3CD-442, 5 Research Parkway, Wallingford, CT, 06492-1996
Tel: 203-677 7458 Fax: 203-677 7569 Email: yuwenli@yahoo.com
Summary
Scientific team leader with 20 year experience in pharmaceutical drug discovery research.
Successfully provide critical support for multiple early and full phase programs include small
molecule, antisense oligonucleotide and gene therapies for psychiatric diseases (depression,
Schizophrenia, Rett syndrome), neurodegenerative diseases, neuropathic pain and heart failure
programs. Highly skilled in leading research teams to use a variety of in vitro, ex vivo and in vivo
approaches for target validation, understanding of mechanisms of action and characterization of
PK-PD relationships of drugs. Authorized over 40 papers with 12 as the first or senior author
since joining the pharmaceutical industry.
Pharmaceutical ResearchExperience
Senior Principal Scientist 2014 – present
Genetically-Defined Diseases, Bristol-Myers Squibb
- Managed a core group with 4 research scientists
o Biochemistry lab
 generated critical data to understand biodistribution (PK-PD) of target
proteins (transgenes) in cardiac and skeletal muscles following systemic
delivery of AAV-mediated gene using fluorescence
immunohistochemistry (IHC) and confocal imaging acquisition and
analysis.
 developed and utilized fluorescence in-situ hybridization (FISH) assays to
investigate X-chromosome reactivation in primary neuronal cultures,
embryonic fibroblastic cells in response to treatment with antisense
oligonucleotides (ASOs) and small molecules, and in target KO mouse
brain tissues as part of target validation.
 characterized ASO uptake and target knockdown effects of ASOs in
disease relevant brain regions of rodents and cynomolgus monkeys using
mRNA in situ hybridization (ISH) assays to support multiple ASO
programs.
 established and used an organotypic cerebellar slice culture assay to
characterize leading Immunoscience program compounds for treatment of
multiple sclerosis.
o In vivo electrophysiology lab
 established and used in vivo spinal electrophysiology assays to evaluate
effects of novel analgesic agents on windup and hyperactivity of spinal
dorsal horn in chronic constriction injury model of neuropathic pain.

2. 2
 established and used in vivo DRG neuronal recording assays to evaluate
effects of peripheral acting analgesic agents on DRG neuronal activity
- Contributed to 2 study reports for IND preparations.
- Authorized 10 publications including 4 as the first/senior author.
Senior Principal Scientist
Neuroscience Biology, Bristol-Myers Squibb 2007 – 2013
- Managed a core group with 6 research scientists (including one PhD)
o Biochemistry lab
 used in vitro and ex vivo binding/occupancy assays (autoradiography and
homogenate binding) to support multiple early and full-phase psychiatry
and neuropathic pain programs.
 used a number of ex vivo biochemistry assays using IHC & ISH
approaches to support early and full-phase discovery programs in
psychiatry, neuropathic pain and Tau neuropathy.
 established a unique focused microwave irradiation-assisted IHC
assay to study phosphor-protein immunoreactivity in response to
drug treatment.
o Electrophysiology lab
 established a unique ex vivo LTP assay as a surrogate readout of synaptic
plasticity to study long lasting effects of novel antidepressant drugs.
- Led to establish a biochemistry lab in the Biocon Bristol-Myers Squibb Research &
Development Center in India, and provided supervision and guidance on regular basis.
- Contributed to 5 study reports for IND preparations.
- Authorized 15 publications including 4 as the first/senior author
Principal Scientist 2004 - 2006
Neuroscience Biology, Bristol-Myers Squibb
- Managed a core group with 4 research scientists
- Provided ex vivo binding occupancy assay support for 5 full-phase programs
- Played a leading role in PET ligand development/PET imaging studies for neuroscience
programs
- Pioneered ex vivo homogenate occupancy assay automation and efficiency improvement
project in collaboration with Applied Biotechnology Discovery Biology Automation group
- Chaired one early-phase drug discovery program
- Contributed to 4 study reports for IND preparations.
- Authorized 4 publications
Senior Research Investigator II 2002 - 2004
Neuroscience Biology, Bristol-Myers Squibb
- Managed one core group with 4 research scientists
- Supported two full-phase and two early phase drug discovery programs in neurological
and psychiatric diseases
- Used ex vivo and in vivo ligand binding and imaging analysis assays for evaluation of
brain penetrance and site occupancy of test compounds
- Established an 18F in vitro biology lab to support PET ligand development

3. 3
- Contributed to 2 study reports for IND preparations
- Authorized 7 publications
Research/Senior ResearchScientist 1999 - 2001
CNS Diseases Research, DuPont Pharmaceuticals
- Managed one core function lab with 4 research scientists
- Supported two full-phase and one early phase drug discovery programs in neurological
and psychiatric, metabolic (obesity) diseases
- Developed competitive in vitro, ex vivo and in vivo ligand binding in brain section assays
and imaging analysis procedures for evaluating brain penetrance and site occupancy of
program compounds
- Developed in vivo electrophysiology assays to support analgesic drug discovery programs
ResearchScientist 1997 - 1998
Computational Biology Group, Central Research& Development, DuPont Company
- Developed in vitro and in vivo electrophysiology models to investigate neuronal
integration and modulation
- Collaborated internally and externally to investigate central regulation of
cardiorespiratory functions.
Academic ResearchExperience
Post-Doctoral ResearchFellow, American Heart Association 1993 - 1996
Department of Pharmacology, University of Virginia
- Investigated central mechanisms responsible regulation of cardiovascular functions using
whole-cell patch clamp in brain slide preparations
Post-Doctoral ResearchFellow, NH&MRC of Australia 1991 - 1992
Department of Physiology University of Sydney, Australia
Ph.D Candidate 1988 - 1990
Department of Medicine and Physiology, Flinders University of South Australia
- Developed and/or applied a variety of electrophysiological and anatomical techniques
including single and multiple unit recording, central microinjection, trans-synaptic
tracing with virus and c-fos functional mapping to investigate central pathways
responsible for control and regulation of cardiovascular functions
ResearchFellow, Australian-China Council 1986 - 1987
Department of Physiology Flinders University of South Australia
- Studied topographic and morphologic changes of brain monoaminergic and peptidergic
neurons in Parkinson's patients using immunohistochemistry and computer-image
analysis techniques
Assistant Professor 1985 - 1986
MasterDegree of Medical Science Candidate 1983 - 1985
Department of Human Anatomy, Hunan Medical University, China

4. 4
- Investigated prenatal development of human brain catecholaminergic neurons using
histofluorescence techniques
Intern in Internal Medicine 1982 - 1983
Anhui Medical College Hospital, China
EDUCATION
Ph.D in Neuroscience and Physiology 1991
Flinders University of South Australia, Australia
Advisor: W.W. Blessing, PhD, MD, Senior Principal Research Fellow of NH&MRC
Thesis: Central mechanisms of cardiovascular regulation
Masterof Medical Science in Neurobiology 1985
Hunan Medical University, Changsha, China
Advisor: H.S. Su, MD
Thesis: Monoaminergic neurons: Distribution in rodent and human brains
Bachelor of Medicine 1982
Anhui Medical College, China

5. 5
PUBLICATION LIST
1. Su, H.S., Peng, Z.C. and Li, Y.-W. (1987) Distribution of catecholamine-containing cell bodies in the human
diencephalon. Brain Research 409, 367-370.
2. Li, Y.-W., Halliday, G.M., Joh, T.H., Geffen, L.B. and Blessing, W.W. (1988) Tyrosine hydroxylase-
containing neurons in the supraoptic and paraventricular nuclei of the adult human. Brain Research 461, 75-
86.
3. Halliday, G.M., Li, Y.-W., Oliver, J.R., Joh, T.H., Cotton, R.G.H., Howe, P.R.C., Geffen, L.B. and Blessing,
W.W. (1988) The distribution of neuropeptide Y-like immunoreactive neurons in the human medulla
oblongata. Neuroscience 26, 179-191.
4. Halliday, G.M., Li, Y.-W., Hoh, T.H., Cotton, R.G.H., Howe, P.R.C., Geffen, L.B. and Blessing, W.W.
(1988) Monoamine-synthesizing neurons in the human medulla oblongata. Journal of Comparative
Neurology 273, 301-317.
5. Halliday, G.M., Li, Y.-W., Joh, T.H., Cotton, R.G.H., Howe, P.R.C., Geffen, L.B. and Blessing, W.W.
(1988) The distribution of substance P-like immunoreactive neurons the human medulla oblongata,
colocalization with monoamine-synthesizing neurons. Synapse 2, 353-370.
6. Halliday, G.M., Li, Y.-W., Joh, T.H., Cotton, R.G.H., Geffen, L.B. and Blessing, W.W. (1988) Topography
of monoamine and substance Pcontaining neurons in the human pons and midbrain. In: Neurology and
Neurobiology Vol.42B Progress in Catecholamine Research Part B: Central Aspects p.179. Alan R. Liss.
Inc., New York.
7. Halliday, G.M., Li, Y.-W., Blumbergs, P. C., Joh, T.H., Cotton, R.G.H., Howe, P.R.C., Blessing, W.W. and
Geffen, L.B. (1990) Neuropathology of immunohistochemically identified brainstem neurons in Parkinson's
disease.Annual of Neurology 27, 373-385.
8. Wesselingh,S.L., Li, Y.-W. and Blessing, W.W. (1989) PNMT-containing neurons in the rostral medulla
oblongata (C1, C3) groups are transneuronally labelled after injection of herpes simplex virus type I into the
adrenal gland. Neuroscience Letters 106, 99-104.
9. Blessing, W.W. and Li, Y.-W. (1989) Inhibitory vasomotorneurons in the caudal region of the medulla
oblongata. Progress in Brain Research 81, 83-97.
10. Li, Y.-W. and Blessing, W.W. (1990) Localization of vasodepressorneurons in the caudal ventrolateral
medulla of the rabbit. Brain Research 417, 227-239.
11. Blessing, W.W., Li, Y.-W. and Wesselingh,S.L. (1991) Transneuronaltransport of Herpes simplex virus
from the central vagus to brain neurons with axonal inputs to central vagal sensory nuclei in the rat.
Neuroscience 42, 261-274.

6. 6
12. Gieroba, Z.J., Li, Y.-W., Wesselingh,S.L. and Blessing, W.W. (1991) Transneuronally labeling of
monoamine-synthesizing neurons in rabbit brain after injection of Herpes Simplex virus type 1 into the aortic
nerve. Brain Research 558, 264-272.
13. Li, Y.-W., Gieroba, Z.J., McAllen, R.M. and Blessing, W.W. (1991) Neurons in rabbit caudal ventrolateral
medulla inhibit bulbospinal barosensitive neurons in rostral medulla. American Journal of Physiology 26,
R44-R51.
14. Li, Y.-W., Wesselingh,S.L. and Blessing,W.W. (1992) Neuronal tracing with Herpes Simplex virus and
phaseolus vulgaris lectin demonstrates inputs from the vasodepressorregion of the caudal medulla to C1 and
A5 sympathoadrenalpremotor neurons in rabbits. Journal of Comparative Neurology 317, 317-329.
15. Li, Y.-W., Ding, Z.-C., Wesselingh,S.L. and Blessing,W.W. (1992) Renal and adrenal sympathetic
preganglionic neurons in rabbit spinal cord: tracing with Herpes Simplex Virus. Brain Research 573, 147-
152.
16. Li, Y.-W., Polson, J. and Dampney, R.A.L. (1992) Angiotensin II injection into rabbit ventrolateral medulla
produces vasomotorresponse without affecting phrenic nerve activity. Brain Research 577, 161-164.
17. Li, Y.-W., Gieroba, Z.J. and Blessing, W.W. (1992) Chemoreceptor and baroreceptor responses ofneurons
projecting from A1 area to supraoptic nucleus in rabbit. American Journal of Physiology 32, R310-317.
18. Gieroba, Z.J., Li, Y.-W. and Blessing, W.W. (1992) Characteristics of caudal ventrolateral medullary neurons
antidromically activated from rostral ventrolateral medulla in the rabbit. Brain Research 582, 196-207.
19. Li, Y.-W. and Dampney, R.A.L. (1992) Expression of Fos proteins in medulla oblongata of conscious
rabbits in response to baroreceptor activation. Neuroscience Letters 144, 70-74.
20. Ding, Z.-C., Li, Y.-W., Wesselingh,S.L. and Blessing, W.W. (1993) Transneuronallabeling of neurons in
rabbit brain after injection of Herpes simplex virus type 1 into the renal nerve. Journal of Autonomic
Nervous System 42, 23-32.
21. Sasaki, S., Li, Y.-W. and Dampney, R.A.L. (1993) Comparison of the pressoreffects of different
angiotensin peptides in the rostral ventrolateral medulla. Brain Research 600, 335-338.
22. Li, Y.-W., Ding, Z.-C., Wesselingh,S.L. and Blessing, W.W (1993) Renal sympathetic preganglionic
neurons demonstrated by herpes simplex virus transneuronallabeling in the rabbits: close apposition of NPY
immunoreactive terminals. Neuroscience 53, 1143-1152.
23. Li, Y.-W., and Dampney, R.A.L. (1994) Expression of Fos-like protein in the brain following sustained
hypertension and hypotension in conscious rabbits. Neuroscience 61, 613-634.
24 Blessing, W.W., Ding, Z.-C., Li, Y.-W., Gieroba, Z.J., Wilson, A.L., Hallsworth, P.M. and Wesselingh,S.L.
(1994) Transneuronallabeling of CNS neurons with Herpes simplex virus type. Progress in Neurobiology
44, 37-53, 1994.
25. Dampney, R.A.L., Li, Y.-W., Potts,P., Polson, J.W. and Hirooka, Y. (1995) Use of c-fos functional
mapping to identify the central baroreceptor reflex pathway: advantages and limitations. Clinical
Experimental Hypertension 17, 197-208.
26. Li, Y.-W. and Dampney, R.A.L. (1995) Clonidine and rilmenidine suppress hypotension-induced Fos
expression in the lower brainstem of the conscious rabbit. Neuroscience 66, 391-402.
27. Polson, J.W., Potts,P., Li, Y.-W. and Dampney, R.A.L. (1995) Fos expression in neurons projecting to the
pressorregion in the rostral ventrolateral medulla after sustained hypertension in conscious rabbits.
Neuroscience 67, 107-123.

7. 7
28. Dampney, R.A.L., Polson, J.W., Potts,P, Li, Y.-W., Hirooka, Y. and Horiuchi, J. (2002) Functional
organization of brain pathways subserving the baroreceptorreflex: studies in conscious animals using
immediate early gene expression. Cellular and Molecular Neurobiology in press.
29. Li, Y.-W. and Guyenet, P.G. (1995) Neuronal excitation by angiotensin II in the rostral ventrolateral
medulla of the rat in vitro. American Journal of Physiology 268, R272-277.
29. Li, Y.-W. and Guyenet, P.G. (1995) Neuronal inhibition by GABAB receptor agonists in the rostral
ventrolateral medulla of the rat. American Journal of Physiology 268, R428-237.
30. Li, Y.-W. Bayliss, D.A. and Guyenet, P.G. (1995) C1 neurons of neonatal rats: intrinsic beating properties
and 2-adrenergic receptors. American Journal of Physiology 269, R1356-R1369.
31. Li, Y.-W. and Guyenet, P.G. (1996) Inhibition of a resting K+ conductance by angiotensin II in rat
bulbospinal C1 cells. Circulation Research 78, 274-282.
32. Li, Y.-W. and Guyenet, P.G. (1996) The GABAA receptor agonist baclofen activates an inwardly rectifying
potassiumconductance in bulbospinal neurons in the rat rostral ventrolateral medulla. American Journal of
Physiology,271: R1304-1310.
33. Guyenet, P.G., Koshiya, N., Huangfu, D.-H., Baraban, S.C., Stornetta, R.L. and Li, Y.-W. (1996) Role of
medulla oblongata in generation of sympathetic and vagal outflows. Progress in Brain Ressearch, 107, 127-
144.
34. Li, Y.-W. and Guyenet, P.G. (1997) Effect of substance Pon C1 and otherbulbospinal cells of the RVLM in
neonatal rats. American Journal of Physiology,273, R805-813.
35. Bayliss, D.A., Li, Y.-W. and Talley, E.M. (1997) Effects of serotonin on caudal raphe neurons:Activation of
an inwardly-rectifying potassiumconductance.Journal of Neurophysiology,77, 1349-1461.
36. Bayliss, D.A., Li, Y.-W. and Talley, E.M. (1997) Effects of serotonin on caudal raphe neurons:Inhibition of
N- and P/Q-type calcium channels and the afterhyperpolarization. Journal of Neurophysiology,77, 1362-
1374.
37. Guyenet, P.G., Li, Y.-W., Huangfu, D.-H., and Schreihofer, A.M. (1997) Bulbospinal C1-adrenergic
neurons:Electrophysiolgical properties in the neonate rat. Advances in Pharmacology. Catecholamines.
Bridging Basic Science With Clinical Medicine. p638-641, Academic Press, Dan Diego.
38. Li, Y.-W., and Bayliss, D.A. (1998) Activation of alpha 2-adrenoceptors causes inhibition of calcium
channels but does not modulate inwardly-rectifying K+ channels in caudal raphe neurons. Neuroscience,82,
753-765.
39. Li, Y.-W., Guyenet, P.G. and Bayliss, D.A. (1998) Voltage-dependent calcium currents in bulbospinal
neurons of neonatal rat rostral ventrolateral medulla: modulation by 2-adrenergic receptors. Journal of
Neurophysiology,79, 583-594.
40. Li, Y.-W., and Bayliss, D.A. (1998) Electrophysiological properties, synaptic transmission and
neuromodulation in serotonergic caudal raphe neurons.Journal of Clinical Physiology and Pharmacology
25, 468-473.
41. Li, Y.-W. and Bayliss, D.A. (1998) Glutamatergic excitatory synaptic transmission between serotonergic
caudal raphe neurons:properties and presynaptic inhibition by 5-HT1B receptors.Journal of Physiology
(Lond.) 510, 121-134.

8. 8
42. Guyenet, P.G., Li, Y.-W, Huangfu, D, Schreihofer, A.M. (1998) Bulbospinal C1-adrenergic neurons:
electrophysiological properties in the neonate rat. Advances in Pharmacology 42, 638-41.
42. Paton, F.R., Li, Y.-W., Kasparov, S. and Deuchars, J. (1999) Pharyngoesophagealreceptive solitary tract
neurons:convergence from peripheral chemoreceptors in arterially-perfused rats. Neuroscience.93, 143-154.
43. Deuchars, J., Li, Y.-W., Kasparov, S, Schwaber, J.S. and Paton, F.R. (2000) Morphological and
electrophysiological properties of physiologically characterized baroreceptive neurons in the dorsal vagal
complex of the rat. Journal of Comparative Neurology.417(2), 233-249.
44. Paton, F.R., Li, Y.-W., Kasparov, S. and Deuchars, J. (2000) Properties of solitary tract neurons receiving
inputs from the sub-diaphragmatic vagus nerve. Neuroscience.95, 141-153.
45. Paton, F.R., Li, Y.-W. and Schwaber. J. (2001) Response properties of NTS baroreceptive neruons. The
AnnalsNew York Academic Science.940, 157-168.
46 Li, Y.-W., Hill, G.R., Wong, H., Kelly, N., Ward, K., Pierdomenico, M., Ren, S., Gilligan, P.J., Grossman,
S.J., Trainor, G.L., Taub, R., McElroy, J. and Zazcek, R. (2003) Receptor occupancy of non-peptide CRF1
antagonist DMP696: correlation with drug exposure and anxiolytic efficacy. Journal Pharmacology and
Experimental Therapies. 305, 86-96.
47 Zhang, G, Huang, N, Li, Y.-W., Qi, X., Marshall, A.P., Yan, X.X., Hill, G., Rominger, C., Prakash, S.R.,
Bakthavatchalam, R., Rominger, D.H., Gilligan, P.J. and Zaczek, R. (2003) Pharmacological
characterization of a novel non-peptide antagonist radioligand, (+/-)-N-[2-methyl-4-methoxyphenyl]-1-(1-
(methoxymethyl) propyl)-6-methyl-1H-1, 2, 3 -triazolo[4,5-c] pyridin-4-amine ([3H]SN003) for
corticotropin-releasing factor1 (CRF1) receptors. Journal Pharmacology and Experimental Therapies. 305,
57-69.
48 Lelas, S, Wong,H, Li, Y.-W , Ward, K, Zeller, K, Sieracki, K, Godonis, H, Ren, S, Yan X.-X, Grossman, S,
Trainor, G, Taub, R., Zazcek, R, Gilligan, P and McElroy, J. (2003) Anxiolytic effects of the CRF1
antagonist DMP904 administered acutely or chronically at doses occupying central CRF1 receptors in rats.
Journal Pharmacology and Experimental Therapies, 309:293-302.
49 Yan, X.-X., Rominger, C. M., Prakash, S.P., Olson, R.E., Zaczek R. and Li, Y.-W. (2004) Binding sites of -
secretase inhibitors in rat brain: distribution, postnataldevelopment and effect of deafferentation. Journal of
Neuroscience.24;2942-2952.
50 Dzierba, C.D., Takvorian, A.G., Rafalski, M., Kasireeddy-Polam, P., Wong,H., Molski, T.F., Zhang,G., Li,
Y.-W., Lelas, S., Peng , Y., McElroy, J., Zaczek, R. Taub, R., Combs, A.P., Gilligan, P.J. and Trainor G.L.,
(2004) Synthesis,structure-activity relationships and in vivo properties of 3.4-dihydro-1H-pyrido[2,3-
b]pyrazin-2-ones as corticotropin-releasing factor antagonists. Journal ofMedicinal Chemistry. 4;47:5783-
90.
51 Gilligan, P. and Li, Y.-W (2004) Corticotropin-releasing factor antagonists:recent advances in exciting
prospects for the treatment of human diseases. Current Opinion in Drug Discovery & Development. 7;487-
497.
52 Li, Y.-W, Fitzgerald, L., Wong,H., Lelas, S., Zhang, G., Mark D. Lindner, M.D., Wallace, T., McElroy, J.,
Lodge, N., Gilligan, P., and Zaczek R. (2005) The pharmacology of DMP696 and DMP904, non-peptide of
CRF1 receptor antagonists. CNS Drug Reviews. 11;21-52.
53 Wong,H., Dockens, R.D., J., Grace J. E., Vachharajani, N., Stark, A.D., Taub, R.A., Yocca, F.D., Zaczek,
R.C. and Li, Y.-W (2007) 6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of
pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. Drug Metabolismand
Disposition.2007 Aug;35(8):1387-92

9. 9
54 Goldstein ME, Cao Y, Fiedler T, Toyn J, Iben L, Barten DM, Pierdomenico M, Corsa J, Prasad CV, Olson
RE, Li YW, Zaczek R, Albright CF. (2007) Ex vivo occupancy of gamma-secretase inhibitors correlates
with brain beta-amyloid peptide reduction in Tg2576 mice. J Pharmacol Exp Ther. 323(1):102-8.
55 Lengyel K, Pieschl R, Strong T, Molski T, Mattson G, Lodge NJ, Li YW (2008) Ex vivo assessment of
binding site occupancy of monoamine reuptake inhibitors: methodology and biological significance.
Neuropharmacology.55:63-70.
56 Lodge NJ, Li YW. (2008) Ion channels as potential targets for the treatment of depression. Opin Drug
Discov Devel. 11:633-41.
57 Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ,
Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman
R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ. (2009) A strategy to minimize reactive metabolite
formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-
3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent,orally bioavailable corticotropin-releasing
factor-1 receptor antagonist. J Med Chem. 10;52(23):7653-68.
58 Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA,
Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE,
Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ,
Mattson RJ, Macor JE. (2009) Synthesis,structure-activity relationships, and in vivo evaluation of N3-
phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem.
23;52:4173-91.
59 Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW,
Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs
AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE. (2009) In vitro intrinsic clearance-based optimization of
N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists. J Med Chem.
23;52:4161-72.
60 Gilligan PJ, He L, Clarke T, Tivitmahaisoon P, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G,
Marshall A, Krause C, McElroy J, Ward K, Shen H, Wong H, Grossman S, Nemeth G, Zaczek R, Arneric
SP, Hartig P, Robertson DW, Trainor G. (2009) 8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines:
selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists. J Med Chem.
14;52:3073-83.
61 Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A,
Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP,
Hartig P, Robertson D, Trainor G. (2009) Synthesis and structure-activity relationships of 8-(pyrid-3-
yl)pyrazolo[1,5-a]-1,3,5-triazines: potent,orally bioavailable corticotropin releasing factor receptor-1
(CRF1) antagonists. J Med Chem. 14;52:3084-92.
62 Schmitz WD, Brenner AB, Bronson JJ, Ditta JL, Griffin CR, Li YW, Lodge NJ, Molski TF, Olson RE, Zhuo
X, Macor JE. (2010) 5-Arylamino-1,2,4-triazin-6(1H)-one CRF(1) receptor antagonists. Bioorg Med Chem
Lett. 17.
63 Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA,
Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi
M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE. (2012)
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl
phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging
agents.Bioorg Med Chem Lett. 1;22:6651-5.

10. 10
64 Lodge NJ, Lelas S, Li YW, Molski T, Grace J, Sivarao DV, Post-Munson D, Healy F, Bronson JJ, Hartz R,
Macor JE, Zaczek R. (2013) Pharmacological and behavioral characterization of the novel CRF(1)
antagonist BMS-763534. Neuropharmacology.67:284-93.
65 Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry
KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ. (2013) NK1 receptor antagonismlowers
occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.
Neuropharmacology. 73:232-40.
66 Lodge NJ, Li YW, Chin FT, Dischino DD, Zoghbi SS, Deskus JA, Mattson RJ, Imaizumi M, Pieschl R,
Molski TF, Fujita M, Dulac H, Zaczek R, Bronson JJ, Macor JE, Innis RB, Pike VW. (2014) Synthesis and
evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.Nucl Med Biol.
41:524-35.
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