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Thomas Heffner

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Thomas R Belliotti; Thomas Capiris; ihoezo Victor ekhato; Jack J Kinsora; mark field; Thomas G Heffner; Leonard T Meltzer; Jacob B Schwarz; Charles P Taylor; Andrew J Thorpe; Mark G Vartanian; Lawrence D Wise; Ti Zhi-Su; Mark L Weber; David J Wustrow
Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein.
Bastiaan J Venhuis; Durk Dijkstra; David J Wustrow; Leonard T Meltzer; Lawrence D Wise; Stephen J Johnson; Thomas G Heffner; Håkan V Wikström
Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity.
Thomas A Pugsley; Yu Hsin Shih; Steven Whetzel; Kim Zoski; Don Van Leeuwen; Hyacinth Akunne; Robert George MacKenzie; Thomas G Heffner; David J Wustrow; Lawrence D Wise
The discovery of PD 89211 and related compounds: selective dopamine D4 receptor antagonists.

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All Publications

2005: Thomas R Belliotti; Thomas Capiris; ihoezo Victor ekhato; Jack J Kinsora; mark field; Thomas G Heffner; Leonard T Meltzer; Jacob B Schwarz; Charles P Taylor; Andrew J Thorpe; Mark G Vartanian; Lawrence D Wise; Ti Zhi-Su; Mark L Weber; David J Wustrow
Structure-activity relationships of pregabalin and analogues that target the alpha(2)-delta protein.
Journal of medicinal chemistry 2005;48(7):2294-307.
2003: Bastiaan J Venhuis; Durk Dijkstra; David J Wustrow; Leonard T Meltzer; Lawrence D Wise; Stephen J Johnson; Thomas G Heffner; Håkan V Wikström
Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: synthesis and pharmacological activity.
Journal of medicinal chemistry 2003;46(4):584-90.
2002: Thomas A Pugsley; Yu Hsin Shih; Steven Whetzel; Kim Zoski; Don Van Leeuwen; Hyacinth Akunne; Robert George MacKenzie; Thomas G Heffner; David J Wustrow; Lawrence D Wise
The discovery of PD 89211 and related compounds: selective dopamine D4 receptor antagonists.
Progress in neuro-psychopharmacology & biological psychiatry 2002;26(2):219-26.
2000: L A van Vliet; Nienke Rodenhuis; Håkan V Wikström; Thomas A Pugsley; Kevin A Serpa; Leonard T Meltzer; Thomas G Heffner; Lawrence D Wise; ME Lajiness; Rita M Huff; Kjell A Svensson; Guido R M M Haenen; Aalt Bast
Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists.
Journal of medicinal chemistry 2000;43(19):3549-57.
2000: L A van Vliet; Nienke Rodenhuis; Durk Dijkstra; Håkan V Wikström; Thomas A Pugsley; Kevin A Serpa; Leonard T Meltzer; Thomas G Heffner; Lawrence D Wise; ME Lajiness; Rita M Huff; Kjell A Svensson; Staffan Sundell; M Lundmark
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).
Journal of medicinal chemistry 2000;43(15):2871-82.
2000: AE Corbin; Leonard T Meltzer; FW Ninteman; JN Wiley; CL Christoffersen; David J Wustrow; Lawrence D Wise; Thomas A Pugsley; Thomas G Heffner
PD 158771, a potential antipsychotic agent with D2/D3 partial agonist and 5-HT(1A) agonist actions. II. Preclinical behavioral effects.
Neuropharmacology 2000;39(7):1211-21.
2000: Hyacinth Akunne; Kim Zoski; Michael Davis; L W Cooke; Leonard T Meltzer; Steven Whetzel; Yu Hsin Shih; David J Wustrow; Lawrence D Wise; Robert George MacKenzie; LM Georgic; Thomas G Heffner; Thomas A Pugsley
PD 158771, a potential antipsychotic agent with D(2)/D(3) partial agonist and 5-HT(1A) agonist actions. I. Neurochemical effects.
Neuropharmacology 2000;39(7):1197-210.
1999: Thomas R Belliotti; David J Wustrow; W A Brink; Kim Zoski; Yu Hsin Shih; Steven Whetzel; LM Georgic; AE Corbin; Hyacinth Akunne; Thomas G Heffner; Thomas A Pugsley; Lawrence D Wise
A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Journal of medicinal chemistry 1999;42(25):5181-7.
1999: Suzanne R Kesten; Thomas G Heffner; Stephen J Johnson; Thomas A Pugsley; Jon L Wright; Lawrence D Wise
Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.
Journal of medicinal chemistry 1999;42(18):3718-25.
1998: David J Wustrow; Thomas Capiris; R Rubin; J A Knobelsdorf; Hyacinth Akunne; Michael Davis; Robert George MacKenzie; Thomas A Pugsley; Kim Zoski; Thomas G Heffner; Lawrence D Wise
Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.
Bioorganic & medicinal chemistry letters 1998;8(16):2067-70.
1998: Thomas R Belliotti; W A Brink; Suzanne R Kesten; John R Rubin; David J Wustrow; Kim Zoski; Steven Whetzel; AE Corbin; Thomas A Pugsley; Thomas G Heffner; Lawrence D Wise
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.
Bioorganic & medicinal chemistry letters 1998;8(12):1499-502.
1998: David J Wustrow; Thomas R Belliotti; SA Glase; S R Kesten; D Johnson; N Colbry; R Rubin; A Blackburn; Hyacinth Akunne; AE Corbin; Michael Davis; LM Georgic; Steven Whetzel; Kim Zoski; Thomas G Heffner; Thomas A Pugsley; L Wise
Aminopyrimidines with high affinity for both serotonin and dopamine receptors.
Journal of medicinal chemistry 1998;41(5):760-71.
1998: AE Corbin; Thomas A Pugsley; Hyacinth Akunne; Steven Whetzel; Kim Zoski; LM Georgic; C B Nelson; Jon L Wright; Lawrence D Wise; Thomas G Heffner
Pharmacological characterization of PD 152255, a novel dimeric benzimidazole dopamine D3 antagonist.
Pharmacology, biochemistry, and behavior 1998;59(2):487-93.
1997: Paul C Unangst; Thomas Capiris; David T Connor; R Doubleday; Thomas G Heffner; Robert George MacKenzie; Steven R Miller; Thomas A Pugsley; Lawrence D Wise
(Aryloxy)alkylamines as selective human dopamine D4 receptor antagonists: potential antipsychotic agents.
Journal of medicinal chemistry 1997;40(25):4026-9.
1997: Paul C Unangst; Thomas Capiris; David T Connor; Thomas G Heffner; Robert George MacKenzie; Steven R Miller; Thomas A Pugsley; Lawrence D Wise
Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents.
Journal of medicinal chemistry 1997;40(17):2688-93.
1997: SA Glase; Hyacinth Akunne; LM Georgic; Thomas G Heffner; Robert George MacKenzie; P J Manley; Thomas A Pugsley; Lawrence D Wise
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.
Journal of medicinal chemistry 1997;40(12):1771-2.
1997: MR Feng; AE Corbin; Y Wang; CL Christoffersen; JN Wiley; CA Strenkoski; E V Tucker; FW Ninteman; Leonard T Meltzer; Thomas G Heffner; DS Wright
Pharmacokinetics and pharmacodynamics of an investigational antipsychotic agent, CI-1007, in rats and monkeys.
Pharmaceutical research 1997;14(3):329-36.
1997: Michael Davis; Thomas G Heffner; L W Cooke
Dopamine agonist-induced inhibition of neurotransmitter release from the awake squirrel monkey putamen as measured by microdialysis.
Journal of neurochemistry 1997;68(2):659-66.
1997: David J Wustrow; W J Smith; AE Corbin; Michael Davis; LM Georgic; Thomas A Pugsley; Steven Whetzel; Thomas G Heffner; Lawrence D Wise
3-[[(4-Aryl-1-piperazinyl)alkyl]cyclohexyl]-1H-indoles as dopamine D2 partial agonists and autoreceptor agonists.
Journal of medicinal chemistry 1997;40(2):250-9.
1997: Hyacinth Akunne; Steven Whetzel; JN Wiley; AE Corbin; FW Ninteman; H Tecle; Y Pei; Thomas A Pugsley; Thomas G Heffner
The pharmacology of the novel and selective sigma ligand, PD 144418.
Neuropharmacology 1997;36(1):51-62.
1996: L A van Vliet; P G Tepper; D Dijkstra; G Damsma; H Wikström; Thomas A Pugsley; Hyacinth Akunne; Thomas G Heffner; S A Glase; Lawrence D Wise
Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.
Journal of medicinal chemistry 1996;39(21):4233-7.
1996: S A Glase; Hyacinth Akunne; Thomas G Heffner; JC Jaen; Robert George MacKenzie; Leonard T Meltzer; Thomas A Pugsley; S J Smith; Lawrence D Wise
Aryl 1-but-3-ynyl-4-phenyl-1,2,3,6-tetrahydropyridines as potential antipsychotic agents: synthesis and structure-activity relationships.
Journal of medicinal chemistry 1996;39(16):3179-87.
1995: Jon L Wright; D M Downing; M R Feng; R N Hayes; Thomas G Heffner; Robert George MacKenzie; Leonard T Meltzer; Thomas A Pugsley; Lawrence D Wise
Identification, characterization and pharmacological profile of three metabolites of (R)-(+)-1,2,3,6-tetrahydro-4-phenyl-1-[(3-phenylcyclohexen-1- yl)methyl]pyridine (CI-1007), a dopamine autoreceptor agonist and potential antipsychotic agent.
Journal of medicinal chemistry 1995;38(26):5007-14.
1995: S A Glase; AE Corbin; Thomas A Pugsley; Thomas G Heffner; Lawrence D Wise
Synthesis and dopaminergic activity of pyridine analogs of 5-hydroxy-2-(di-n-propylamino)tetralin.
Journal of medicinal chemistry 1995;38(16):3132-7.
1995: Leonard T Meltzer; CL Christoffersen; AE Corbin; F W Ninteman; Kevin A Serpa; J N Wiley; Lawrence D Wise; Thomas G Heffner
CI-1007, a dopamine partial agonist and potential antipsychotic agent. II. Neurophysiological and behavioral effects.
The Journal of pharmacology and experimental therapeutics 1995;274(2):912-20.
1995: Hyacinth Akunne; S B Demattos; Steven Whetzel; David J Wustrow; D M Davis; Lawrence D Wise; Wayne L Cody; Thomas A Pugsley; Thomas G Heffner
Agonist properties of a stable hexapeptide analog of neurotensin, N alpha MeArg-Lys-Pro-Trp-tLeu-Leu (NT1).
Biochemical pharmacology 1995;49(8):1147-54.
1995: Thomas A Pugsley; Hyacinth Akunne; Steven Whetzel; S Demattos; AE Corbin; J N Wiley; David J Wustrow; Lawrence D Wise; Thomas G Heffner
Differential effects of the nonpeptide neurotensin antagonist, SR 48692, on the pharmacological effects of neurotensin agonists.
Peptides 1995;16(1):37-44.
1995: Hyacinth Akunne; P Towers; G J Ellis; D Dijkstra; H Wikström; Thomas G Heffner; Lawrence D Wise; Thomas A Pugsley
Characterization of binding of [3H]PD 128907, a selective dopamine D3 receptor agonist ligand, to CHO-K1 cells.
Life sciences 1995;57(15):1401-10.
1994: David J Wustrow; Lawrence D Wise; D M Cody; Robert George MacKenzie; LM Georgic; Thomas A Pugsley; Thomas G Heffner
Studies of the active conformation of a novel series of benzamide dopamine D2 agonists.
Journal of medicinal chemistry 1994;37(24):4251-7.
1994: Jon L Wright; B W Caprathe; D M Downing; S A Glase; Thomas G Heffner; JC Jaen; S J Johnson; S R Kesten; Robert George MacKenzie; Leonard T Meltzer
The discovery and structure-activity relationships of 1,2,3,6-tetrahydro-4-phenyl-1-[(arylcyclohexenyl)alkyl]pyridines. Dopamine autoreceptor agonists and potential antipsychotic agents.
Journal of medicinal chemistry 1994;37(21):3523-33.
1994: D L Heyl; A M Sefler; JX He; T K Sawyer; David J Wustrow; Hyacinth Akunne; Michael Davis; Thomas A Pugsley; Thomas G Heffner; AE Corbin
Structure-activity and conformational studies of a series of modified C-terminal hexapeptide neurotensin analogues.
International journal of peptide and protein research 1994;44(3):233-8.
1993: G Damsma; T Bottema; Ben H C Westerink; P G Tepper; D Dijkstra; Thomas A Pugsley; Robert George MacKenzie; Thomas G Heffner; H Wikström
Pharmacological aspects of R-(+)-7-OH-DPAT, a putative dopamine D3 receptor ligand.
European journal of pharmacology 1993;249(3):R9-10.
1992: Leonard T Meltzer; CL Christoffersen; Kevin A Serpa; Thomas A Pugsley; A Razmpour; Thomas G Heffner
Lack of involvement of haloperidol-sensitive sigma binding sites in modulation of dopamine neuronal activity and induction of dystonias by antipsychotic drugs.
Neuropharmacology 1992;31(9):961-7.
1992: Judith Leopold; Patrick W Vincent; Karen A Beningo; William L. Elliott; Wilbur R Leopold; Thomas G Heffner; J N Wiley; Michael A Stier; M J Suto
Pharmacologic/pharmacokinetic evaluation of emesis induced by analogs of RSU 1069 and its control by antiemetic agents.
International journal of radiation oncology, biology, physics 1992;22(3):549-51.
1991: B W Caprathe; JC Jaen; Lawrence D Wise; Thomas G Heffner; Thomas A Pugsley; Leonard T Meltzer; M Parvez
Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine.
Journal of medicinal chemistry 1991;34(9):2736-46.
1991: JC Jaen; Lawrence D Wise; Thomas G Heffner; Thomas A Pugsley; Leonard T Meltzer
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.
Journal of medicinal chemistry 1991;34(1):248-56.
1990: H A DeWald; Thomas G Heffner; JC Jaen; D M Lustgarten; A T McPhail; Leonard T Meltzer; Thomas A Pugsley; Lawrence D Wise
Synthesis and dopamine agonist properties of (+-)-trans-3,4,4a,10b-tetrahydro-4-propyl-2H,5H-[1]benzopyrano [4,3-b]-1,4-oxazin-9-ol and its enantiomers.
Journal of medicinal chemistry 1990;33(1):445-50.
1990: JC Jaen; Lawrence D Wise; B W Caprathe; Haile Tecle; S Bergmeier; Christine Humblet; Thomas G Heffner; Leonard T Meltzer; Thomas A Pugsley
4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.
Journal of medicinal chemistry 1990;33(1):311-7.
1989: Leonard T Meltzer; J N Wiley; Thomas G Heffner
The alpha 2-adrenoceptor antagonists idazoxan and yohimbine can unmask the postsynaptic dopamine agonist effects of B-HT 920.
European journal of pharmacology 1989;170(1-2):105-7.
1989: Leonard T Meltzer; CL Christoffersen; Thomas G Heffner; A S Freeman; L A Chiodo
CI-943, a potential antipsychotic agent. III. Evaluation of effects on dopamine neuronal activity.
The Journal of pharmacology and experimental therapeutics 1989;251(1):123-30.
1989: Thomas G Heffner; D A Downs; Leonard T Meltzer; J N Wiley; A E Williams
CI-943, a potential antipsychotic agent. I. Preclinical behavioral effects.
The Journal of pharmacology and experimental therapeutics 1989;251(1):105-12.
1989: Thomas G Heffner; J N Wiley; A E Williams; R F Bruns; L L Coughenour; D A Downs
Comparison of the behavioral effects of adenosine agonists and dopamine antagonists in mice.
Psychopharmacology 1989;98(1):31-7.
1988: JC Jaen; Lawrence D Wise; Thomas G Heffner; Thomas A Pugsley; Leonard T Meltzer
Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines.
Journal of medicinal chemistry 1988;31(8):1621-5.
1988: Lawrence D Wise; H A DeWald; E S Hawkins; D M Reynolds; Thomas G Heffner; Leonard T Meltzer; Thomas A Pugsley
6- and 8-hydroxy-3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans. Dopamine agonists with autoreceptor selectivity.
Journal of medicinal chemistry 1988;31(3):688-91.
1988: H A DeWald; N W Beeson; F M Hershenson; Lawrence D Wise; D A Downs; Thomas G Heffner; L L Coughenour; Thomas A Pugsley
Synthesis and potential antipsychotic activity of 1H-imidazo[1,2-c]pyrazolo[3,4-e]pyrimidines.
Journal of medicinal chemistry 1988;31(2):454-61.
1988: Leonard T Meltzer; J N Wiley; A E Williams; Thomas G Heffner
Evidence for postsynaptic dopamine agonist effects of B-HT 920 in the presence of the dopamine D-1 agonist SKF 38393.
Psychopharmacology 1988;95(3):329-32.
1987: Lawrence D Wise; D E Butler; H A DeWald; D M Lustgarten; I C Pattison; D N Schweiss; L L Coughenour; D A Downs; Thomas G Heffner; Thomas A Pugsley
1,3-Dialkyl-4-(iminoarylmethyl)-1H-pyrazol-5-ols. A series of novel potential antipsychotic agents.
Journal of medicinal chemistry 1987;30(10):1807-12.
1987: Alexander J Bridges; W H Moos; D L Szotek; Bharat K Trivedi; J A Bristol; Thomas G Heffner; R F Bruns; D A Downs
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
Journal of medicinal chemistry 1987;30(10):1709-11.
1986: Lawrence D Wise; D E Butler; H A DeWald; D Lustgarten; L L Coughenour; D A Downs; Thomas G Heffner; Thomas A Pugsley
(5-Amino-1,3-dimethyl-1H-pyrazol-4-yl)(2-fluorophenyl)methanones . A series of novel potential antipsychotic agents.
Journal of medicinal chemistry 1986;29(9):1628-37.
1986: M D Taylor; W H Moos; Harriet W Hamilton; D S Szotek; WC Patt; E W Badger; J A Bristol; R F Bruns; Thomas G Heffner; T E Mertz
Ribose-modified adenosine analogues as adenosine receptor agonists.
Journal of medicinal chemistry 1986;29(3):346-53.