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Robert Zaczek

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Nicholas J Lodge; John E Macor; Thaddeus Molski; Debra Post-Munson; Digavalli V Sivarao; Joanne J Bronson; James Grace; Richard A Hartz; Francine Healy; Snjezana Lelas; Yu-Wen Li; Robert Zaczek
Pharmacological and behavioral characterization of the novel CRF(1) antagonist BMS-763534.
Carolyn D Dzierba; Amy Galka; Paul J Gilligan; Tricia L Johnson; Padmaja Kasireddy-Polam; Nicholas J Lodge; Argyrios G Arvanitis; Joanne J Bronson; Andrew P Combs; Bireshwar Dasgupta; Thaddeus F Molski; Maria Rafalski; Thais M Sielecki; Amy Takvorian; George L Trainor; Shikha Vig; Harvey Wong; Robert Zaczek; Ge Zhang; John E Macor
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Richard A Hartz; Vijay T Ahuja; Xiaoliang Zhuo; Ronald J Mattson; Derek J Denhart; Jeffrey A Deskus; Vivekananda M Vrudhula; Senliang Pan; Jonathan L Ditta; Yue-Zhong Shu; James E Grace; Kimberley A Lentz; Snjezana Lelas; Yu-Wen Li; Thaddeus F Molski; Subramaniam Krishnananthan; Henry Wong; Jingfang Qian-Cutrone; Richard Schartman; Rex Denton; Nicholas J Lodge; Robert Zaczek; John E Macor; Joanne J Bronson
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.

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All Publications

2013: Nicholas J Lodge; John E Macor; Thaddeus Molski; Debra Post-Munson; Digavalli V Sivarao; Joanne J Bronson; James Grace; Richard A Hartz; Francine Healy; Snjezana Lelas; Yu-Wen Li; Robert Zaczek
Pharmacological and behavioral characterization of the novel CRF(1) antagonist BMS-763534.
Neuropharmacology 2013;67():284-93.
2012: Carolyn D Dzierba; Amy Galka; Paul J Gilligan; Tricia L Johnson; Padmaja Kasireddy-Polam; Nicholas J Lodge; Argyrios G Arvanitis; Joanne J Bronson; Andrew P Combs; Bireshwar Dasgupta; Thaddeus F Molski; Maria Rafalski; Thais M Sielecki; Amy Takvorian; George L Trainor; Shikha Vig; Harvey Wong; Robert Zaczek; Ge Zhang; John E Macor
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2012;22(15):4986-9.
2009: Richard A Hartz; Vijay T Ahuja; Xiaoliang Zhuo; Ronald J Mattson; Derek J Denhart; Jeffrey A Deskus; Vivekananda M Vrudhula; Senliang Pan; Jonathan L Ditta; Yue-Zhong Shu; James E Grace; Kimberley A Lentz; Snjezana Lelas; Yu-Wen Li; Thaddeus F Molski; Subramaniam Krishnananthan; Henry Wong; Jingfang Qian-Cutrone; Richard Schartman; Rex Denton; Nicholas J Lodge; Robert Zaczek; John E Macor; Joanne J Bronson
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.
Journal of medicinal chemistry 2009;52(23):7653-68.
2009: Richard A Hartz; Vijay T Ahuja; Argyrios G Arvanitis; Maria Rafalski; Eddy W Yue; Derek J Denhart; William D Schmitz; Jonathan L Ditta; Jeffrey A Deskus; Allison B Brenner; Frank W Hobbs; Joseph Payne; Snjezana Lelas; Yu-Wen Li; Thaddeus F Molski; Gail K Mattson; Yong Peng; Harvey Wong; James E Grace; Kimberley A Lentz; Jingfang Qian-Cutrone; Xiaoliang Zhuo; Yue-Zhong Shu; Nicholas J Lodge; Robert Zaczek; Andrew P Combs; Richard E Olson; Joanne J Bronson; Ronald J Mattson; John E Macor
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Journal of medicinal chemistry 2009;52(14):4173-91.
2009: Richard A Hartz; Vijay T Ahuja; Maria Rafalski; William D Schmitz; Allison B Brenner; Derek J Denhart; Jonathan L Ditta; Jeffrey A Deskus; Eddy W Yue; Argyrios G Arvanitis; Snjezana Lelas; Yu-Wen Li; Thaddeus F Molski; Harvey Wong; James E Grace; Kimberley A Lentz; Jianqing Li; Nicholas J Lodge; Robert Zaczek; Andrew P Combs; Richard E Olson; Ronald J Mattson; Joanne J Bronson; John E Macor
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Journal of medicinal chemistry 2009;52(14):4161-72.
2007: Lawrence Iben; Richard E Olson; Lynn A Balanda; Sukhanya Jayachandra; Barbara J Robertson; Vanessa Hay; John Corradi; C V C Prasad; Robert Zaczek; Charles F Albright; Jeremy H Toyn
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.
The Journal of biological chemistry 2007;282(51):36829-36.
2007: Margi E Goldstein; Yang Cao; Tracey Fiedler; Jeremy H Toyn; Lawrence Iben; Donna M Barten; Maria Pierdomenico; Jason A Corsa; C V C Prasad; Richard E Olson; Yu-Wen Li; Robert Zaczek; Charles F Albright
Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice.
The Journal of pharmacology and experimental therapeutics 2007;323(1):102-8.
2007: Harvey Wong; Randy C Dockens; Lori Pajor; Suresh Yeola; James E Grace; Arlene D Stark; Rebecca A Taub; Frank D Yocca; Robert Zaczek; Yu-Wen Li
6-Hydroxybuspirone is a major active metabolite of buspirone: assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats.
Drug metabolism and disposition: the biological fate of chemicals 2007;35(8):1387-92.
2007: Michael G Yang; Jian-Liang Shi; Dilip P Modi; Jennifer Wells; Brian M Cochran; Mark A Wolf; Lorin A Thompson; Mercy M Ramanjulu; Arthur H Roach; Robert Zaczek; David W Robertson; Ruth R Wexler; Richard E Olson
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(14):3910-5.
2007: Carolyn D Dzierba; Andrew J Tebben; Richard G Wilde; Amy Takvorian; Maria Rafalski; Padmaja Kasireddy-Polam; John D Klaczkiewicz; Anthony D Pechulis; Amy L Davis; Mark P Sweet; Alex M Woo; Zhicai Yang; Sarah M Ebeltoft; Thaddeus F Molski; Ge Zhang; Robert Zaczek; George L Trainor; Andrew P Combs; Paul J Gilligan
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.
Journal of medicinal chemistry 2007;50(9):2269-72.
2006: Lorin A Thompson; Ann Y Liauw; Mercy M Ramanjulu; Padmaja Kasireddy-Polam; Stephen E Mercer; Thomas Maduskuie; Marcie Glicksman; Arthur H Roach; Jere E Meredith; Rui-Qin Liu; Andrew P Combs; Jeffrey N Higaki; Barbara Cordell; Dietmar Seiffert; Robert Zaczek; David W Robertson; Richard E Olson
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(9):2357-63.
2006: Donna M Barten; Jere E Meredith; Robert Zaczek; John G Houston; Charles F Albright
Gamma-secretase inhibitors for Alzheimer's disease: balancing efficacy and toxicity.
Drugs in R&D 2006;7(2):87-97.
2005: Yu-Wen Li; Lawrence Fitzgerald; Harvey Wong; Snjezana Lelas; Ge Zhang; Mark D Lindner; Tanya Wallace; John F McElroy; Nicholas J Lodge; Paul J Gilligan; Robert Zaczek
The pharmacology of DMP696 and DMP904, non-peptidergic CRF1 receptor antagonists.
CNS drug reviews 2005;11(1):21-52.
2004: Carolyn D Dzierba; Amy Takvorian; Maria Rafalski; Padmaja Kasireddy-Polam; Harvey Wong; Thaddeus F Molski; Ge Zhang; Yu-Wen Li; Snjezana Lelas; Yong Peng; John F McElroy; Robert Zaczek; Rebecca A Taub; Andrew P Combs; Paul J Gilligan; George L Trainor
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
Journal of medicinal chemistry 2004;47(23):5783-90.
2004: Richard A Hartz; Kausik K Nanda; Charles L Ingalls; Vijay T Ahuja; Thaddeus F Molski; Ge Zhang; Harvey Wong; Yong Peng; Michelle Kelley; Nicholas J Lodge; Robert Zaczek; Paul J Gilligan; George L Trainor
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.
Journal of medicinal chemistry 2004;47(19):4741-54.
2004: Snjezana Lelas; Harvey Wong; Yu-Wen Li; Karen L Heman; Kathryn A Ward; Kim L Zeller; Kristine K Sieracki; Joseph L Polino; Helen E Godonis; Shelly X Ren; Xiao-Xin Yan; Stephen P Arneric; David W Robertson; Paul R Hartig; Scott Grossman; George L Trainor; Rebecca A Taub; Robert Zaczek; Paul J Gilligan; John F McElroy
Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats.
The Journal of pharmacology and experimental therapeutics 2004;309(1):293-302.
2004: Xiao-Xin Yan; Tong Li; Cynthia M Rominger; Shimoga R Prakash; Philip C Wong; Richard E Olson; Robert Zaczek; Yu-Wen Li
Binding sites of gamma-secretase inhibitors in rodent brain: distribution, postnatal development, and effect of deafferentation.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2004;24(12):2942-52.
2003: Ge Zhang; Ning Huang; Yu-Wen Li; Xiaoping Qi; Anne P Marshall; Xiao-Xin Yan; Geraldine Hill; Cynthia M Rominger; Shimoga R Prakash; Rajagopal Bakthavatchalam; David H Rominger; Paul J Gilligan; Robert Zaczek
Pharmacological characterization of a novel nonpeptide 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 receptors.
The Journal of pharmacology and experimental therapeutics 2003;305(1):57-69.
2003: Argyrios G Arvanitis; Joseph T Rescinito; Charles R Arnold; Richard G Wilde; Lawrence W Fitzgerald; Robert Zaczek; Paul R Hartig; Scott Grossman; Stephen P Arneric; Paul J Gilligan; Richard E Olson; David W Robertson
Imidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands.
Bioorganic & medicinal chemistry letters 2003;13(1):129-31.
2003: Argyrios G Arvanitis; Joseph T Rescinito; Charles R Arnold; Richard G Wilde; Gary A Cain; Jung-Hui Sun; Jia-Sheng Yan; Christopher A Teleha; Lawrence W Fitzgerald; John F McElroy; Robert Zaczek; Paul R Hartig; Scott Grossman; Stephen P Arneric; Paul J Gilligan; Richard E Olson; David W Robertson
Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
Bioorganic & medicinal chemistry letters 2003;13(1):125-8.
2002: Jere E Meredith; Qian Wang; Thomas J Mitchell; Richard E Olson; Robert Zaczek; Andrew M Stern; Dietmar Seiffert
Gamma-secretase activity is not involved in presenilin-mediated regulation of beta-catenin.
Biochemical and biophysical research communications 2002;299(5):744-50.
2000: Dietmar Seiffert; Jodi D Bradley; Cynthia M Rominger; David H Rominger; F Yang; Jere E Meredith; Qian Wang; Arthur H Roach; Lorin A Thompson; Susan M Spitz; Jeffrey N Higaki; Shimoga R Prakash; Andrew P Combs; Robert Copeland; Stephen P Arneric; Paul R Hartig; David W Robertson; Barbara Cordell; Andrew M Stern; Richard E Olson; Robert Zaczek
Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.
The Journal of biological chemistry 2000;275(44):34086-91.
2000: Paul J Gilligan; David W Robertson; Robert Zaczek
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.
Journal of medicinal chemistry 2000;43(9):1641-60.
2000: L He; Paul J Gilligan; Robert Zaczek; Lawrence W Fitzgerald; John F McElroy; H S Shen; JA Saye; N H Kalin; S Shelton; D Christ; George L Trainor; Paul R Hartig
4-(1,3-Dimethoxyprop-2-ylamino)-2,7-dimethyl-8-(2, 4-dichlorophenyl)pyrazolo[1,5-a]-1,3,5-triazine: a potent, orally bioavailable CRF(1) receptor antagonist.
Journal of medicinal chemistry 2000;43(3):449-56.
2000: Paul J Gilligan; C Baldauf; AJ Cocuzza; DR Chidester; Robert Zaczek; Lawrence W Fitzgerald; John F McElroy; Mark A Smith; H S Shen; JA Saye; D Christ; George L Trainor; David W Robertson; Paul R Hartig
The discovery of 4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1 ,5-a]-pyrimidine: a corticotropin-releasing factor (hCRF1) antagonist.
Bioorganic & medicinal chemistry 2000;8(1):181-9.
1999: JP Beck; M A Curry; RJ Chorvat; Lawrence W Fitzgerald; Paul J Gilligan; Robert Zaczek; George L Trainor
Thiazolo[4,5-d]pyrimidine thiones and -ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Bioorganic & medicinal chemistry letters 1999;9(8):1185-8.
1999: JP Beck; Argyrios G Arvanitis; M A Curry; Joseph T Rescinito; Lawrence W Fitzgerald; Paul J Gilligan; Robert Zaczek; George L Trainor
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Bioorganic & medicinal chemistry letters 1999;9(7):967-72.
1999: RJ Chorvat; Rajagopal Bakthavatchalam; JP Beck; Paul J Gilligan; Richard G Wilde; AJ Cocuzza; Frank W Hobbs; RS Cheeseman; M Curry; Joseph P Rescinito; PJ Krenitsky; DR Chidester; J A Yarem; John D Klaczkiewicz; Carl Nicholas Hodge; P E Aldrich; Z R Wasserman; C H Fernandez; Robert Zaczek; Lawrence W Fitzgerald; S M Huang; H L Shen; Y N Wong; B M Chien; Argyrios G Arvanitis
Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.
Journal of medicinal chemistry 1999;42(5):833-48.
1998: Richard A Earl; Robert Zaczek; Christopher A Teleha; B N Fisher; C M Maciag; M E Marynowski; A R Logue; S William Tam; W J Tinker; S M Huang; RJ Chorvat
2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action.
Journal of medicinal chemistry 1998;41(23):4615-22.
1998: David H Rominger; Cynthia M Rominger; Lawrence W Fitzgerald; Reinhard Grzanna; Brian L Largent; Robert Zaczek
Characterization of [125I]sauvagine binding to CRH2 receptors: membrane homogenate and autoradiographic studies.
The Journal of pharmacology and experimental therapeutics 1998;286(1):459-68.
1998: Robert Zaczek; RJ Chorvat; JA Saye; M E Pierdomenico; C M Maciag; A R Logue; B N Fisher; David H Rominger; Richard A Earl
Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine.
The Journal of pharmacology and experimental therapeutics 1998;285(2):724-30.
1998: RJ Chorvat; Robert Zaczek; B S Brown
Ion channel modulators that enhance acetylcholine release: potential therapies for Alzheimer's disease.
Expert opinion on investigational drugs 1998;7(4):499-518.
1996: J A Saydoff; Robert Zaczek
Blockade of N- and Q-type Ca2+ channels inhibit K(+)-evoked [3H]acetylcholine release in rat hippocampal slices.
Brain research bulletin 1996;40(4):283-6.
1995: A M Persico; Charles W Schindler; Robert Zaczek; M T Brannock; George R. Uhl
Brain transcription factor gene expression, neurotransmitter levels, and novelty response behaviors: alterations during rat amphetamine withdrawal and following chronic injection stress.
Synapse (New York, N.Y.) 1995;19(3):212-27.
1995: S William Tam; Robert Zaczek
Linopirdine. A depolarization-activated releaser of transmitters for treatment of dementia.
Advances in experimental medicine and biology 1995;363():47-56.
1994: C M Maciag; A R Logue; W J Tinker; J A Saydoff; S William Tam; Robert Zaczek
Studies on the role of K+, Cl- and Na+ ion permeabilities in the acetylcholine release enhancing effects of linopirdine (DuP 996) in rat cortical slices.
The Journal of pharmacology and experimental therapeutics 1994;271(2):891-7.
1993: Robert Zaczek; W J Tinker; S William Tam
Unique properties of norepinephrine release from terminals arising from the locus coeruleus: high potassium sensitivity and lack of linopirdine (DuP 996) enhancement.
Neuroscience letters 1993;155(1):107-11.
1992: J Lehmann; E B DeSouza; S Culp; Robert Zaczek
Regional distribution to recovery of 5-HT levels after administration of "atrophins" MDMA and D,L-fenfluramine. Stereospecificity and comparison with 5,7-dihydroxytryptamine.
Annals of the New York Academy of Sciences 1992;648():291-5.
1991: E B De Souza; Robert Zaczek; S Culp; N M Appel; J F Contrera
Comparison of the effects of repeated oral versus subcutaneous fenfluramine administration on rat brain monoamine neurons: pharmacokinetic and dose-response data.
Pharmacology, biochemistry, and behavior 1991;39(4):963-9.
1991: N M Appel; M J Owens; S Culp; Robert Zaczek; J F Contrera; Garth Bissette; Charles Nemeroff; E B De Souza
Role for brain corticotropin-releasing factor in the weight-reducing effects of chronic fenfluramine treatment in rats.
Endocrinology 1991;128(6):3237-46.
1991: Robert Zaczek; S Culp; E B De Souza
Interactions of [3H]amphetamine with rat brain synaptosomes. II. Active transport.
The Journal of pharmacology and experimental therapeutics 1991;257(2):830-5.
1991: Robert Zaczek; S Culp; H Goldberg; D J Mccann; E B De Souza
Interactions of [3H]amphetamine with rat brain synaptosomes. I. Saturable sequestration.
The Journal of pharmacology and experimental therapeutics 1991;257(2):820-9.
1991: George R. Uhl; B O'Hara; S Shimada; Robert Zaczek; J DiGiorgianni; T Nishimori
Dopamine transporter: expression in Xenopus oocytes.
Brain research. Molecular brain research 1991;9(1-2):23-9.
1990: M C Ritz; J W Boja; D Grigoriadis; Robert Zaczek; Frank carroll; A H Lewis; Michael J Kuhar
[3H]WIN 35,065-2: a ligand for cocaine receptors in striatum.
Journal of neurochemistry 1990;55(5):1556-62.
1990: Robert Zaczek; J M Fritschy; S Culp; E B De Souza; R Grzanna
Differential effects of DSP-4 on noradrenaline axons in cerebral cortex and hypothalamus may reflect heterogeneity of noradrenaline uptake sites.
Brain research 1990;522(2):308-14.
1990: Robert Zaczek; G Battaglia; S Culp; N M Appel; J F Contrera; E B De Souza
Effects of repeated fenfluramine administration on indices of monoamine function in rat brain: pharmacokinetic, dose response, regional specificity and time course data.
The Journal of pharmacology and experimental therapeutics 1990;253(1):104-12.
1990: Robert Zaczek; S Culp; E B De Souza
Intrasynaptosomal sequestration of [3H]amphetamine and [3H]methylenedioxyamphetamine: characterization suggests the presence of a factor responsible for maintaining sequestration.
Journal of neurochemistry 1990;54(1):195-204.
1989: D E Grigoriadis; Robert Zaczek; D M Pearsall; E B De Souza
Solubilization of high affinity corticotropin-releasing factor receptors from rat brain: characterization of an active digitonin-solubilized receptor complex.
Endocrinology 1989;125(6):3068-77.
1989: Robert Zaczek; G Battaglia; J F Contrera; S Culp; E B De Souza
Methylphenidate and pemoline do not cause depletion of rat brain monoamine markers similar to that observed with methamphetamine.
Toxicology and applied pharmacology 1989;100(2):227-33.
1989: Robert Zaczek; S Hurt; S Culp; E B De Souza
Characterization of brain interactions with methylenedioxyamphetamine and methylenedioxymethamphetamine.
NIDA research monograph 1989;94():223-39.