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Jon Hawkinson

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Darren B Dressen; Albert W Garofalo; Jon E Hawkinson; Dennis Hom; Jacek Jagodzinski; Jennifer L Marugg; Martin L Neitzel; Michael A Pleiss; Balazs Szoke; jay tung; David W G Wone; Jing Wu; Heather Zhang
Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.
Jon E Hawkinson; Balazs G Szoke; Albert W Garofalo; Dennis S Hom; Hongbing Zhang; Mark Dreyer; Juri Y Fukuda; Linda Chen; Bhushan Samant; Stellanie Simmonds; Karla P Zeitz; Angie Wadsworth; Anna Liao; Raymond A Chavez; Wes Zmolek; Lany Ruslim; Michael P Bova; Ryan Holcomb; Eduardo R Butelman; Mei-Chuan Ko; Annika B Malmberg
Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958.
Zhang-Lin Zhou; Sunil M Kher; Sui Xiong Cai; Edward R Whittemore; Stephen A Espitia; Jon E Hawkinson; Minhtam Tran; Richard M Woodward; Eckard Weber; John F W Keana
Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists.

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All Publications

2007: Darren B Dressen; Albert W Garofalo; Jon E Hawkinson; Dennis Hom; Jacek Jagodzinski; Jennifer L Marugg; Martin L Neitzel; Michael A Pleiss; Balazs Szoke; jay tung; David W G Wone; Jing Wu; Heather Zhang
Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.
Journal of medicinal chemistry 2007;50(21):5161-7.
2007: Jon E Hawkinson; Balazs G Szoke; Albert W Garofalo; Dennis S Hom; Hongbing Zhang; Mark Dreyer; Juri Y Fukuda; Linda Chen; Bhushan Samant; Stellanie Simmonds; Karla P Zeitz; Angie Wadsworth; Anna Liao; Raymond A Chavez; Wes Zmolek; Lany Ruslim; Michael P Bova; Ryan Holcomb; Eduardo R Butelman; Mei-Chuan Ko; Annika B Malmberg
Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958.
The Journal of pharmacology and experimental therapeutics 2007;322(2):619-30.
2003: Zhang-Lin Zhou; Sunil M Kher; Sui Xiong Cai; Edward R Whittemore; Stephen A Espitia; Jon E Hawkinson; Minhtam Tran; Richard M Woodward; Eckard Weber; John F W Keana
Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists.
Bioorganic & medicinal chemistry 2003;11(8):1769-80.
2001: Zhang-Lin Zhou; J M Navratil; Sui Xiong Cai; Edward R Whittemore; Stephen A Espitia; Jon E Hawkinson; Minhtam Tran; Richard M Woodward; Eckard Weber; John F W Keana
Synthesis and SAR of 5-, 6-, 7- and 8-aza analogues of 3-aryl-4-hydroxyquinolin-2(1H)-one as NMDA/glycine site antagonists.
Bioorganic & medicinal chemistry 2001;9(8):2061-71.
2000: KE Vanover; Sharon Rosenzweig-Lipson; Jon E Hawkinson; NC Lan; James D Belluzzi; Larry Stein; James E Barrett; PL Wood; Richard Carter
Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors.
The Journal of pharmacology and experimental therapeutics 2000;295(1):337-45.
2000: A P Guzikowski; AP Tamiz; M Acosta-Burruel; S Hong-Bae; Sui Xiong Cai; Jon E Hawkinson; John F W Keana; Suzanne R Kesten; C T Shipp; Minhtam Tran; Edward R Whittemore; Richard M Woodward; Jon L Wright; Zhang-Lin Zhou
Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.
Journal of medicinal chemistry 2000;43(5):984-94.
2000: Jon E Hawkinson; M Acosta-Burruel; Stephen A Espitia
Opioid activity profiles indicate similarities between the nociceptin/orphanin FQ and opioid receptors.
European journal of pharmacology 2000;389(2-3):107-14.
1999: Zhang-Lin Zhou; Sui Xiong Cai; Edward R Whittemore; CS Konkoy; Stephen A Espitia; Minhtam Tran; D M Rock; L L Coughenour; Jon E Hawkinson; Peter A Boxer; CF Bigge; Lawrence D Wise; Eckard Weber; Richard M Woodward; John F W Keana
4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Journal of medicinal chemistry 1999;42(15):2993-3000.
1999: Jon L Wright; Tracy Gregory; CF Bigge; Peter A Boxer; Kevin A Serpa; Leonard T Meltzer; Lawrence D Wise; Sui Xiong Cai; Jon E Hawkinson; CS Konkoy; Edward R Whittemore; Richard M Woodward; Zhang-Lin Zhou
Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.
Journal of medicinal chemistry 1999;42(13):2469-77.
1998: Jon E Hawkinson; M Acosta-Burruel; K C Yang; Derk J Hogenkamp; J S Chen; NC Lan; John Drewe; Edward R Whittemore; Richard M Woodward; Richard Carter; RB Upasani
Substituted 3beta-phenylethynyl derivatives of 3alpha-hydroxy-5alpha-pregnan-20-one: remarkably potent neuroactive steroid modulators of gamma-aminobutyric acidA receptors.
The Journal of pharmacology and experimental therapeutics 1998;287(1):198-207.
1997: S Wieland; James D Belluzzi; Jon E Hawkinson; Derk J Hogenkamp; RB Upasani; Larry Stein; PL Wood; Kelvin W Gee; NC Lan
Anxiolytic and anticonvulsant activity of a synthetic neuroactive steroid Co 3-0593.
Psychopharmacology 1997;134(1):46-54.
1997: Sui Xiong Cai; Jin-Cheng Huang; Stephen A Espitia; Minhtam Tran; Victor I Ilyin; Jon E Hawkinson; Richard M Woodward; Eckard Weber; John F W Keana
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Journal of medicinal chemistry 1997;40(22):3679-86.
1997: Jon E Hawkinson; M Acosta-Burruel; N D Ta; PL Wood
Novel phosphoserine phosphatase inhibitors.
European journal of pharmacology 1997;337(2-3):315-24.
1997: Dale M Edgar; WF Seidel; Kelvin W Gee; NC Lan; G Field; H Xia; Jon E Hawkinson; S Wieland; Richard Carter; PL Wood
CCD-3693: an orally bioavailable analog of the endogenous neuroactive steroid, pregnanolone, demonstrates potent sedative hypnotic actions in the rat.
The Journal of pharmacology and experimental therapeutics 1997;282(1):420-9.
1997: Jon E Hawkinson; Stephen A Espitia
Effects of thiocyanate and AMPA receptor ligands on (S)-5-fluorowillardiine, (S)-AMPA and (R,S)-AMPA binding.
European journal of pharmacology 1997;329(2-3):213-21.
1997: PL Wood; Jon E Hawkinson
N-methyl-D-aspartate antagonists for stroke and head trauma.
Expert opinion on investigational drugs 1997;6(4):389-97.
1997: Richard Carter; PL Wood; S Wieland; Jon E Hawkinson; Delia Belelli; Jeremy J Lambert; H S White; H H Wolf; S Mirsadeghi; S H Tahir; M B Bolger; NC Lan; Kelvin W Gee
Characterization of the anticonvulsant properties of ganaxolone (CCD 1042; 3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one), a selective, high-affinity, steroid modulator of the gamma-aminobutyric acid(A) receptor.
The Journal of pharmacology and experimental therapeutics 1997;280(3):1284-95.
1997: Sui Xiong Cai; S M Kher; Zhang-Lin Zhou; Victor I Ilyin; Stephen A Espitia; Minhtam Tran; Jon E Hawkinson; Richard M Woodward; Eckard Weber; John F W Keana
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.
Journal of medicinal chemistry 1997;40(5):730-8.
1997: Jon E Hawkinson; K R Huber; P S Sahota; H Han Hsu; E Weber; M J Whitehouse
The N-methyl-D-aspartate (NMDA) receptor glycine site antagonist ACEA 1021 does not produce pathological changes in rat brain.
Brain research 1997;744(2):227-34.
1997: RB Upasani; K C Yang; M Acosta-Burruel; CS Konkoy; J A McLellan; Richard M Woodward; NC Lan; Richard Carter; Jon E Hawkinson
3 alpha-Hydroxy-3 beta-(phenylethynyl)-5 beta-pregnan-20-ones: synthesis and pharmacological activity of neuroactive steroids with high affinity for GABAA receptors.
Journal of medicinal chemistry 1997;40(1):73-84.
1997: Derk J Hogenkamp; S H Tahir; Jon E Hawkinson; RB Upasani; M Alauddin; C L Kimbrough; M Acosta-Burruel; Edward R Whittemore; Richard M Woodward; NC Lan; Kelvin W Gee; M B Bolger
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.
Journal of medicinal chemistry 1997;40(1):61-72.
1996: Sui Xiong Cai; Zhang-Lin Zhou; Jin-Cheng Huang; Edward R Whittemore; Z O Egbuwoku; Jon E Hawkinson; Richard M Woodward; E Weber; John F W Keana
Structure-activity relationships of 4-hydroxy-3-nitroquinolin-2(1H)-ones as novel antagonists at the glycine site of N-methyl-D-aspartate receptors.
Journal of medicinal chemistry 1996;39(23):4682-6.
1996: A P Guzikowski; Sui Xiong Cai; Stephen A Espitia; Jon E Hawkinson; J E Huettner; D F Nogales; Minhtam Tran; Richard M Woodward; E Weber; John F W Keana
Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Journal of medicinal chemistry 1996;39(23):4643-53.
1996: Michael B Bolger; S Wieland; Jon E Hawkinson; H Xia; RB Upasani; NC Lan
In vitro and in vivo activity of 16,17-dehydro-epipregnanolones: 17,20-bond torsional energy analysis and D-ring conformation.
Pharmaceutical research 1996;13(10):1488-94.
1996: P L Wood; Jon E Hawkinson; D B Goodnough
Formation of D-serine from L-phosphoserine in brain synaptosomes.
Journal of neurochemistry 1996;67(4):1485-90.
1996: Sui Xiong Cai; Zhang-Lin Zhou; Jin-Cheng Huang; Edward R Whittemore; Z O Egbuwoku; Y Lü; Jon E Hawkinson; Richard M Woodward; E Weber; John F W Keana
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydroquinoline-2,3,4-trione 3-oximes: novel and highly potent antagonists for NMDA receptor glycine site.
Journal of medicinal chemistry 1996;39(17):3248-55.
1996: Jon E Hawkinson; M Acosta-Burruel; P L Wood
The metabotropic glutamate receptor antagonist L-2-amino-3-phosphonopropionic acid inhibits phosphoserine phosphatase.
European journal of pharmacology 1996;307(2):219-25.
1996: Jon E Hawkinson; M Acosta-Burruel; C L Kimbrough; D B Goodnough; P L Wood
Steroid inhibition of [3H]SR 95531 binding to the GABAA recognition site.
European journal of pharmacology 1996;304(1-3):141-6.
1996: Jon E Hawkinson; John Drewe; C L Kimbrough; J S Chen; Derk J Hogenkamp; NC Lan; Kelvin W Gee; Ke-Zhong Shen; Edward R Whittemore; Richard M Woodward
3 alpha-Hydroxy-3 beta-trifluoromethyl-5 alpha-pregnan-20-one (Co 2-1970): a partial agonist at the neuroactive steroid site of the gamma-aminobutyric acidA receptor.
Molecular pharmacology 1996;49(5):897-906.
1995: L D McCauley; V Liu; J S Chen; Jon E Hawkinson; NC Lan; Kelvin W Gee
Selective actions of certain neuroactive pregnanediols at the gamma-aminobutyric acid type A receptor complex in rat brain.
Molecular pharmacology 1995;47(2):354-62.
1995: D B Goodnough; Jon E Hawkinson
Neuroactive steroid modulation of [3H]muscimol binding to the GABAA receptor complex in rat cortex.
European journal of pharmacology 1995;288(2):157-62.
1994: Jon E Hawkinson; C L Kimbrough; Delia Belelli; Jeremy J Lambert; R H Purdy; NC Lan
Correlation of neuroactive steroid modulation of [35S]t-butylbicyclophosphorothionate and [3H]flunitrazepam binding and gamma-aminobutyric acidA receptor function.
Molecular pharmacology 1994;46(5):977-85.
1994: Jon E Hawkinson; C L Kimbrough; L D McCauley; Michael B Bolger; NC Lan; Kelvin W Gee
The neuroactive steroid 3 alpha-hydroxy-5 beta-pregnan-20-one is a two-component modulator of ligand binding to the GABAA receptor.
European journal of pharmacology 1994;269(2):157-63.