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Christina Dersch

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Malliga R Iyer; Arthur E Jacobson; Christina M Dersch; Richard B Rothman; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 47.(1) Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
Fuying Li; Richard B Rothman; Jason A Deck; Christina M Dersch; Jeffrey R Deschamps; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 46. N-substituted-2,3,4,9,10,10a-hexahydro-1H-1,4a-(epiminoethano)phenanthren-6- and 8-ols - carbocyclic relatives of f-oxide-bridged phenylmorphans.
David J Martin; Richard B Rothman; Ellicott J Sally; Mario Ayestas; Christina M Dersch; Paul E FitzMorris; Bo Li; Amy M Deveau
An efficient synthesis of 3-OBn-6β,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.

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All Publications

2013: Malliga R Iyer; Arthur E Jacobson; Christina M Dersch; Richard B Rothman; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 47.(1) Novel C4a- and N-substituted-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
Bioorganic & medicinal chemistry 2013;21(11):3298-309.
2012: Fuying Li; Richard B Rothman; Jason A Deck; Christina M Dersch; Jeffrey R Deschamps; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 46. N-substituted-2,3,4,9,10,10a-hexahydro-1H-1,4a-(epiminoethano)phenanthren-6- and 8-ols - carbocyclic relatives of f-oxide-bridged phenylmorphans.
European journal of medicinal chemistry 2012;58():557-67.
2012: David J Martin; Richard B Rothman; Ellicott J Sally; Mario Ayestas; Christina M Dersch; Paul E FitzMorris; Bo Li; Amy M Deveau
An efficient synthesis of 3-OBn-6β,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.
Bioorganic & medicinal chemistry letters 2012;22(22):6801-5.
2012: Subramaniam Ananthan; Edward J Bilsky; Christina M Dersch; Denise Giuvelis; Nicholas McGlinchey; Surendra K Saini; Heng Xu; Richard B Rothman
14-Alkoxy- and 14-acyloxypyridomorphinans: μ agonist/δ antagonist opioid analgesics with diminished tolerance and dependence side effects.
Journal of medicinal chemistry 2012;55(19):8350-63.
2012: Malliga R Iyer; Arthur E Jacobson; Yong-Sok Lee; Christina M Dersch; Jeffrey R Deschamps; Richard B Rothman; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 44. Synthesis of an N-substituted 4-hydroxy-5-(3-hydroxyphenyl)morphan with high affinity and selective μ-antagonist activity.
European journal of medicinal chemistry 2012;50():44-54.
2011: Feng Li; Richard B Rothman; Kejun Cheng; Jason A Deck; Christina M Dersch; Jeffrey Deschamps; John E Folk; Arthur E Jacobson; Muneaki Kurimura; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.
Bioorganic & medicinal chemistry 2011;19(14):4330-7.
2011: Jin-Hee Kim; Jeffrey Deschamps; Richard B Rothman; Christina M Dersch; John E Folk; Kejun Cheng; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.
Bioorganic & medicinal chemistry 2011;19(11):3434-43.
2011: Anthony Lozama; Christopher W Cunningham; Michael J Caspers; Justin T Douglas; Christina M Dersch; Richard B Rothman; Thomas E Prisinzano
Opioid receptor probes derived from cycloaddition of the hallucinogen natural product salvinorin A.
Journal of natural products 2011;74(4):718-26.
2011: Kejun Cheng; Yong-Sok Lee; Richard B Rothman; Christina M Dersch; Ross W Bittman; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 41. Unusual inverse μ-agonists and potent μ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.
Journal of medicinal chemistry 2011;54(4):957-69.
2011: Richard B Rothman; Jean Lud Cadet; Christina M Dersch; Michael T McCoy; Elin Lehrmann; Kevin G Becker; Michael Bader; Natalia Alenina; Michael H Baumann
Altered gene expression in pulmonary tissue of tryptophan hydroxylase-1 knockout mice: implications for pulmonary arterial hypertension.
PloS one 2011;6(3):e17735.
2010: Elliott J Sally; Heng Xu; Christina M Dersch; Ling-Wei Hsin; Li-Te Chang; Thomas E Prisinzano; Denise S Simpson; Denise Giuvelis; Kenner C Rice; Arthur E Jacobson; Kejun Cheng; Edward J Bilsky; Richard B Rothman
Identification of a novel "almost neutral" micro-opioid receptor antagonist in CHO cells expressing the cloned human mu-opioid receptor.
Synapse (New York, N.Y.) 2010;64(4):280-8.
2010: Edward J Bilsky; Denise Giuvelis; Melissa D Osborn; Christina M Dersch; Heng Xu; Richard B Rothman
In vitro and in vivo assessment of mu opioid receptor constitutive activity.
Methods in enzymology 2010;484():413-43.
2010: Malliga R Iyer; Yong-Sok Lee; Jeffrey Deschamps; Richard B Rothman; Christina M Dersch; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 40. N-substituted cis-4a-ethyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-8-ols.
Bioorganic & medicinal chemistry 2010;18(1):91-9.
2009: Yi Zhang; Yong-Sok Lee; Richard B Rothman; Christina M Dersch; Jeffrey Deschamps; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 39. Enantiomeric N-substituted benzofuro[2,3-c]pyridin-6-ols: synthesis and topological relationship to oxide-bridged phenylmorphans.
Journal of medicinal chemistry 2009;52(23):7570-9.
2009: Andrea L Pelotte; Ryan M Smith; Mario Ayestas; Christina M Dersch; Edward J Bilsky; Richard B Rothman; Amy M Deveau
Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
Bioorganic & medicinal chemistry letters 2009;19(10):2811-4.
2009: Richard B Rothman; Christina M Dersch; Subramaniam Ananthan; John S Partilla
Studies of the biogenic amine transporters. 13. Identification of "agonist" and "antagonist" allosteric modulators of amphetamine-induced dopamine release.
The Journal of pharmacology and experimental therapeutics 2009;329(2):718-28.
2008: Heng Xu; Xiaoying Wang; John S Partilla; Kristen Bishop-Mathis; tova benaderet; Christina M Dersch; Denise S Simpson; Thomas E Prisinzano; Richard B Rothman
Differential effects of opioid agonists on G protein expression in CHO cells expressing cloned human opioid receptors.
Brain research bulletin 2008;77(1):49-54.
2008: Josef Zezula; Lisa Singer; Anna K Przybył; Akihiro Hashimoto; Christina M Dersch; Richard B Rothman; Jeffrey Deschamps; Yong-Sok Lee; Arthur E Jacobson; Kenner C Rice
Synthesis and pharmacological effects of the enantiomers of the N-phenethyl analogues of the ortho and para e- and f-oxide-bridged phenylmorphans.
Organic & biomolecular chemistry 2008;6(16):2868-83.
2008: John M Rutherford; Jia Bei Wang; Heng Xu; Christina M Dersch; John S Partilla; Kenner C Rice; Richard B Rothman
Evidence for a mu-delta opioid receptor complex in CHO cells co-expressing mu and delta opioid peptide receptors.
Peptides 2008;29(8):1424-31.
2008: Joseph J Pariser; John S Partilla; Christina M Dersch; Subramaniam Ananthan; Richard B Rothman
Studies of the biogenic amine transporters. 12. Identification of novel partial inhibitors of amphetamine-induced dopamine release.
The Journal of pharmacology and experimental therapeutics 2008;326(1):286-95.
2008: Kevin Tidgewell; Chad E Groer; Wayne W Harding; Anthony Lozama; Matthew Schmidt; Alfred Marquam; Jessica Hiemstra; John S Partilla; Christina M Dersch; Richard B Rothman; Laura M Bohn; Thomas E Prisinzano
Herkinorin analogues with differential beta-arrestin-2 interactions.
Journal of medicinal chemistry 2008;51(8):2421-31.
2007: Xiaoying Wang; Michael H Baumann; Christina M Dersch; Richard B Rothman
Restoration of 3,4-methylenedioxymethamphetamine-induced 5-HT depletion by the administration of L-5-hydroxytryptophan.
Neuroscience 2007;148(1):212-20.
2007: Anne-Cécile Hiebel; Yong-Sok Lee; Edward J Bilsky; Denise Giuvelis; Jeffrey Deschamps; Damon Parrish; Mario D Aceto; Everette L May; Louis S Harris; Andrew Coop; Christina M Dersch; John S Partilla; Richard B Rothman; Kejun Cheng; Arthur E Jacobson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
Journal of medicinal chemistry 2007;50(16):3765-76.
2007: Denise S Simpson; Peter L Katavic; Anthony Lozama; Wayne W Harding; Damon Parrish; Jeffrey Deschamps; Christina M Dersch; John S Partilla; Richard B Rothman; Hernan Navarro; Thomas E Prisinzano
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
Journal of medicinal chemistry 2007;50(15):3596-603.
2007: Kejun Cheng; In Jong Kim; Mei-Jing Lee; Steven A Adah; Tyler J Raymond; Edward J Bilsky; Mario D Aceto; Everette L May; Louis S Harris; Andrew Coop; Christina M Dersch; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a micro-agonist delta-antagonist and delta-inverse agonists.
Organic & biomolecular chemistry 2007;5(8):1177-90.
2007: Richard B Rothman; Daniel L Murphy; Heng Xu; Jonathan A Godin; Christina M Dersch; John S Partilla; Kevin Tidgewell; Matthew Schmidt; Thomas E Prisinzano
Salvinorin A: allosteric interactions at the mu-opioid receptor.
The Journal of pharmacology and experimental therapeutics 2007;320(2):801-10.
2007: Kathleen M Gilbert; Terrence L Boos; Christina M Dersch; Elisabeth Greiner; Arthur E Jacobson; David Lewis; Dorota Matecka; Thomas E Prisinzano; Ying Zhang; Richard B Rothman; Kenner C Rice; Carol A Venanzi
DAT/SERT selectivity of flexible GBR 12909 analogs modeled using 3D-QSAR methods.
Bioorganic & medicinal chemistry 2007;15(2):1146-59.
2006: Santosh S Kulkarni; Barbara Nightingale; Christina M Dersch; Richard B Rothman; Amy Hauck Newman
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
Bioorganic & medicinal chemistry letters 2006;16(13):3371-5.
2006: Wayne W Harding; Matthew Schmidt; Kevin Tidgewell; Pavitra Kannan; Kenneth G Holden; Christina M Dersch; Richard B Rothman; Thomas E Prisinzano
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: selective modification of the furan ring.
Bioorganic & medicinal chemistry letters 2006;16(12):3170-4.
2006: Kevin Tidgewell; Wayne W Harding; Anthony Lozama; Howard Cobb; Kushal Shah; Pavitra Kannan; Christina M Dersch; Damon Parrish; Jeffrey Deschamps; Richard B Rothman; Thomas E Prisinzano
Synthesis of salvinorin A analogues as opioid receptor probes.
Journal of natural products 2006;69(6):914-8.
2006: Terrence L Boos; Elisabeth Greiner; W Jason Calhoun; Thomas E Prisinzano; Barbara Nightingale; Christina M Dersch; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Structure-activity relationships of substituted N-benzyl piperidines in the GBR series: Synthesis of 4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(2-trifluoromethylbenzyl)piperidine, an allosteric modulator of the serotonin transporter.
Bioorganic & medicinal chemistry 2006;14(11):3967-73.
2006: Elisabeth Greiner; Terrence L Boos; Thomas E Prisinzano; Maria G De Martino; Brian Zeglis; Christina M Dersch; Jamila Marcus; John S Partilla; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity.
Journal of medicinal chemistry 2006;49(5):1766-72.
2005: Barbara Nightingale; Christina M Dersch; Terrence L Boos; Elisabeth Greiner; William J Calhoun; Arthur E Jacobson; Kenner C Rice; Richard B Rothman
Studies of the biogenic amine transporters. XI. Identification of a 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR12909) analog that allosterically modulates the serotonin transporter.
The Journal of pharmacology and experimental therapeutics 2005;314(2):906-15.
2005: Wayne W Harding; Kevin Tidgewell; Nathan Byrd; Howard Cobb; Christina M Dersch; Eduardo R Butelman; Richard B Rothman; Thomas E Prisinzano
Neoclerodane diterpenes as a novel scaffold for mu opioid receptor ligands.
Journal of medicinal chemistry 2005;48(15):4765-71.
2005: Wayne W Harding; Kevin Tidgewell; Matthew Schmidt; Kushal Shah; Christina M Dersch; John Snyder; Damon Parrish; Jeffrey Deschamps; Richard B Rothman; Thomas E Prisinzano
Salvinicins A and B, new neoclerodane diterpenes from Salvia divinorum.
Organic letters 2005;7(14):3017-20.
2004: Richard B Rothman; Subramaniam Jayanthi; Jean Lud Cadet; Xiaoying Wang; Christina M Dersch; Michael H Baumann
Substituted amphetamines that produce long-term serotonin depletion in rat brain ("neurotoxicity") do not decrease serotonin transporter protein expression.
Annals of the New York Academy of Sciences 2004;1025():151-61.
2004: Ayon Nandi; Christina M Dersch; Manish Kulshrestha; Subramaniam Ananthan; Richard B Rothman
Identification and characterization of a novel allosteric modulator (SoRI-6238) of the serotonin transporter.
Synapse (New York, N.Y.) 2004;53(3):176-83.
2004: In Jong Kim; Christina M Dersch; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
A critical structural determinant of opioid receptor interaction with phenolic 5-phenylmorphans.
Bioorganic & medicinal chemistry 2004;12(16):4543-50.
2004: Han Yu; In Jong Kim; John E Folk; Xinrong Tian; Richard B Rothman; Michael H Baumann; Christina M Dersch; Judith L Flippen-Anderson; Damon Parrish; Arthur E Jacobson; Kenner C Rice
Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
Journal of medicinal chemistry 2004;47(10):2624-34.
2004: Subramaniam Ananthan; Naveen K Khare; Surendra K Saini; Lainne E Seitz; Jeffrey L Bartlett; Peg Davis; Christina M Dersch; Frank Porreca; Richard B Rothman; Edward J Bilsky
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Journal of medicinal chemistry 2004;47(6):1400-12.
2004: James B Thomas; Scott E Fix; Richard B Rothman; Wayne Mascarella; Christina M Dersch; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
Importance of phenolic address groups in opioid kappa receptor selective antagonists.
Journal of medicinal chemistry 2004;47(4):1070-3.
2003: Richard B Rothman; Subramaniam Jayanthi; Xiaoying Wang; Christina M Dersch; Jean Lud Cadet; Thomas E Prisinzano; Kenner C Rice; Michael H Baumann
High-dose fenfluramine administration decreases serotonin transporter binding, but not serotonin transporter protein levels, in rat forebrain.
Synapse (New York, N.Y.) 2003;50(3):233-9.
2003: In Jong Kim; Thomas Ullrich; James Janetka; M Scott Furness; Arthur E Jacobson; Richard B Rothman; Christina M Dersch; Judith L Flippen-Anderson; Clifford George; Kenner C Rice
Diaryldimethylpiperazine ligands with mu- and delta-opioid receptor affinity: Synthesis of (+)-4-[(alphaR)-alpha-(4-allyl-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide and (-)-4-[(alphaR)-alpha-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide.
Bioorganic & medicinal chemistry 2003;11(22):4761-8.
2003: Subramaniam Ananthan; Naveen K Khare; Surendra K Saini; Peg Davis; Christina M Dersch; Frank Porreca; Richard B Rothman
Novel ligands for the opioid receptors: synthesis and structure-activity relationships among 5'-aryl and 5'-heteroaryl 17-cyclopropylmethyl-4,5 alpha-epoxypyrido[2',3':6,7]morphinans.
Bioorganic & medicinal chemistry 2003;11(18):4143-54.
2003: James B Thomas; Robert N Atkinson; N Ariane Vinson; Jennifer L Catanzaro; Carin L Perretta; Scott E Fix; Wayne Mascarella; Richard B Rothman; Heng Xu; Christina M Dersch; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Journal of medicinal chemistry 2003;46(14):3127-37.
2003: Elisabeth Greiner; Thomas E Prisinzano; Edward M Johnson; Christina M Dersch; Jamila Marcus; John S Partilla; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.
Journal of medicinal chemistry 2003;46(8):1465-9.
2003: David Lewis; Ying Zhang; Thomas E Prisinzano; Christina M Dersch; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.
Bioorganic & medicinal chemistry letters 2003;13(7):1385-9.
2003: Ling-Wei Hsin; Thomas E Prisinzano; Chavon R Wilkerson; Christina M Dersch; Robert Horel; Arthur E Jacobson; Richard B Rothman; Kenner C Rice
Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.
Bioorganic & medicinal chemistry letters 2003;13(3):553-6.
2003: Subramaniam Ananthan; Hollis S Kezar; Surendra K Saini; Naveen K Khare; Peg Davis; Christina M Dersch; Frank Porreca; Richard B Rothman
Synthesis, opioid receptor binding, and functional activity of 5'-substituted 17-cyclopropylmethylpyrido[2',3':6,7]morphinans.
Bioorganic & medicinal chemistry letters 2003;13(3):529-32.
2002: Johannes Schütz; Christina M Dersch; Robert Horel; Mariana Spetea; Martin Koch; Ruth Meditz; Elisabeth Greiner; Richard B Rothman; Helmut Schmidhammer
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
Journal of medicinal chemistry 2002;45(24):5378-83.
2002: Akihiro Hashimoto; Arthur E Jacobson; Richard B Rothman; Christina M Dersch; Clifford George; Judith L Flippen-Anderson; Kenner C Rice
Probes for narcotic receptor mediated phenomena. Part 28: new opioid antagonists from enantiomeric analogues of 5-(3-hydroxyphenyl)-N-phenylethylmorphan.
Bioorganic & medicinal chemistry 2002;10(10):3319-29.
2002: Thomas E Prisinzano; Elisabeth Greiner; Edward M Johnson; Christina M Dersch; Jamila Marcus; John S Partilla; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter.
Journal of medicinal chemistry 2002;45(19):4371-4.
2002: Subramaniam Ananthan; Surendra K Saini; Rashmi Khare; Sarah D Clayton; Christina M Dersch; Richard B Rothman
Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines.
Bioorganic & medicinal chemistry letters 2002;12(16):2225-8.
2002: James B Thomas; Robert N Atkinson; Nivedita Namdev; Richard B Rothman; Kenneth M Gigstad; Scott E Fix; Wayne Mascarella; Jason P Burgess; N Ariane Vinson; Heng Xu; Christina M Dersch; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.
Journal of medicinal chemistry 2002;45(16):3524-30.
2002: Richard B Rothman; Marina Katsnelson; Nga Vu; John S Partilla; Christina M Dersch; Bruce E Blough; Michael H Baumann
Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain.
European journal of pharmacology 2002;447(1):51-7.
2002: Richard B Rothman; Frank carroll; Marisela Morales; Daniel L Rowley; Kenner C Rice; Christina M Dersch; David M Donovan
Studies of the biogenic amine transporters. 10. Characterization of a novel cocaine binding site in brain membranes prepared from dopamine transporter knockout mice.
Synapse (New York, N.Y.) 2002;44(2):94-105.
2002: Richard B Rothman; Christina M Dersch; Frank carroll; Subramaniam Ananthan
Studies of the biogenic amine transporters. VIII: identification of a novel partial inhibitor of dopamine uptake and dopamine transporter binding.
Synapse (New York, N.Y.) 2002;43(4):268-74.
2002: Ling-Wei Hsin; Christina M Dersch; Michael H Baumann; David Stafford; John R Glowa; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine.
Journal of medicinal chemistry 2002;45(6):1321-9.
2002: Han Yu; Thomas E Prisinzano; Christina M Dersch; Jamila Marcus; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Synthesis and biological activity of 8beta-substituted hydrocodone indole and hydromorphone indole derivatives.
Bioorganic & medicinal chemistry letters 2002;12(2):165-8.
2001: Ying Zhang; D B Joseph; Wayne D Bowen; Judith L Flippen-Anderson; Christina M Dersch; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
Journal of medicinal chemistry 2001;44(23):3937-45.
2001: Thomas Ullrich; Christina M Dersch; Richard B Rothman; Arthur E Jacobson; Kenner C Rice
Derivatives of 17-(2-methylallyl)-substituted noroxymorphone: variation of the delta address and its effects on affinity and selectivity for the delta opioid receptor.
Bioorganic & medicinal chemistry letters 2001;11(21):2883-5.
2001: James B Thomas; Robert N Atkinson; Richard B Rothman; Scott E Fix; Wayne Mascarella; N Ariane Vinson; Heng Xu; Christina M Dersch; Y Lu; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Journal of medicinal chemistry 2001;44(17):2687-90.
2001: Michael H Baumann; Mario A Ayestas; Christina M Dersch; Richard B Rothman
1-(m-chlorophenyl)piperazine (mCPP) dissociates in vivo serotonin release from long-term serotonin depletion in rat brain.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 2001;24(5):492-501.
2001: S McLamore; Thomas Ullrich; Richard B Rothman; HAN XU; Christina M Dersch; Andrew Coop; P Davis; F Porreca; Arthur E Jacobson; Kenner C Rice
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and efficacy.
Journal of medicinal chemistry 2001;44(9):1471-4.
2001: James B Thomas; XM Herault; Richard B Rothman; Robert N Atkinson; Jason P Burgess; Wayne Mascarella; Christina M Dersch; Heng Xu; Judith L Flippen-Anderson; CF George; Frank carroll
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides.
Journal of medicinal chemistry 2001;44(6):972-87.
2001: Richard B Rothman; Michael H Baumann; Christina M Dersch; D V Romero; Kenner C Rice; Frank carroll; John S Partilla
Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin.
Synapse (New York, N.Y.) 2001;39(1):32-41.
2000: Xiao-Hui Gu; Han Yu; Arthur E Jacobson; Richard B Rothman; Christina M Dersch; C George; Judith L Flippen-Anderson; Kenner C Rice
Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
Journal of medicinal chemistry 2000;43(25):4868-76.
2000: Ying Zhang; Richard B Rothman; Christina M Dersch; B R de Costa; Arthur E Jacobson; Kenner C Rice
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).
Journal of medicinal chemistry 2000;43(25):4840-9.
2000: John S Partilla; Christina M Dersch; H Yu; Kenner C Rice; Richard B Rothman
Neurochemical neutralization of amphetamine-type stimulants in rat brain by the indatraline analog (-)-HY038.
Brain research bulletin 2000;53(6):821-6.
2000: Han Yu; Richard B Rothman; Christina M Dersch; John S Partilla; Kenner C Rice
Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters.
Bioorganic & medicinal chemistry 2000;8(12):2689-92.
2000: Michael H Baumann; Mario A Ayestas; Christina M Dersch; John S Partilla; Richard B Rothman
Serotonin transporters, serotonin release, and the mechanism of fenfluramine neurotoxicity.
Annals of the New York Academy of Sciences 2000;914():172-86.
2000: Richard B Rothman; John S Partilla; Christina M Dersch; Frank carroll; Kenner C Rice; Michael H Baumann
Methamphetamine dependence: medication development efforts based on the dual deficit model of stimulant addiction.
Annals of the New York Academy of Sciences 2000;914():71-81.
2000: M Scott Furness; Xiaoyan Zhang; Andrew Coop; Arthur E Jacobson; Richard B Rothman; Christina M Dersch; HAN XU; F Porreca; Kenner C Rice
Probes for narcotic receptor-mediated phenomena. 27. Synthesis and pharmacological evaluation of selective delta-opioid receptor agonists from 4-[(alphaR)-alpha-(2S,5R)-4-substituted-2, 5-dimethyl-1-piperazinyl-3-methoxybenzyl]-N,N-diethylbenzamides and their enantiomers.
Journal of medicinal chemistry 2000;43(16):3193-6.
2000: James B Thomas; Robert N Atkinson; Richard B Rothman; Jason P Burgess; Wayne Mascarella; Christina M Dersch; Heng Xu; Frank carroll
4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.
Bioorganic & medicinal chemistry letters 2000;10(11):1281-4.
2000: Michael H Baumann; Mario A Ayestas; Christina M Dersch; A Brockington; Kenner C Rice; Richard B Rothman
Effects of phentermine and fenfluramine on extracellular dopamine and serotonin in rat nucleus accumbens: therapeutic implications.
Synapse (New York, N.Y.) 2000;36(2):102-13.
2000: Richard B Rothman; John S Partilla; Michael H Baumann; Christina M Dersch; Frank carroll; Kenner C Rice
Neurochemical neutralization of methamphetamine with high-affinity nonselective inhibitors of biogenic amine transporters: a pharmacological strategy for treating stimulant abuse.
Synapse (New York, N.Y.) 2000;35(3):222-7.
1999: Xiaoyan Zhang; Kenner C Rice; SN Calderon; H Kayakiri; L Smith; Andrew Coop; Arthur E Jacobson; Richard B Rothman; P Davis; Christina M Dersch; F Porreca
Probes for narcotic receptor mediated phenomena. 26. Synthesis and biological evaluation of diarylmethylpiperazines and diarylmethylpiperidines as novel, nonpeptidic delta opioid receptor ligands.
Journal of medicinal chemistry 1999;42(26):5455-63.
1999: Andrew Coop; J Pinto; L Wang; K McCullough; Richard B Rothman; Christina M Dersch; Arthur E Jacobson; Kenner C Rice
Delta opioid binding selectivity of 3-ether analogs of naltrindole.
Bioorganic & medicinal chemistry letters 1999;9(24):3435-8.
1999: James B Thomas; Robert N Atkinson; XM Herault; Richard B Rothman; Wayne Mascarella; Christina M Dersch; Heng Xu; Robert Horel; Frank carroll
Optically pure (-)-4-[(N-allyl-3-methyl-4-piperidinyl)phenyl-amino]-N,N-diethylbenzami de displays selective binding and full agonist activity for the delta opioid receptor.
Bioorganic & medicinal chemistry letters 1999;9(23):3347-50.
1999: D B Lewis; Dorota Matecka; Ying Zhang; Ling-Wei Hsin; Christina M Dersch; David Stafford; John R Glowa; Richard B Rothman; Kenner C Rice
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.
Journal of medicinal chemistry 1999;42(24):5029-42.
1999: James B Thomas; XM Herault; Richard B Rothman; Jason P Burgess; Wayne Mascarella; Heng Xu; Robert Horel; Christina M Dersch; Frank carroll
(+/-)-4-[(N-allyl-cis-3-methyl-4-piperidinyl)phenylamino]-N,N-diethylbenzamide displays selective binding for the delta opioid receptor.
Bioorganic & medicinal chemistry letters 1999;9(20):3053-6.
1999: Subramaniam Ananthan; Hollis S Kezar; R L Carter; Surendra K Saini; Kenner C Rice; J L Wells; Peg Davis; Heng Xu; Christina M Dersch; Edward J Bilsky; Frank Porreca; Richard B Rothman
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Journal of medicinal chemistry 1999;42(18):3527-38.
1999: Richard B Rothman; Michael H Baumann; Christina M Dersch; J Appel; R A Houghten
Discovery of novel peptidic dopamine transporter ligands by screening a positional scanning combinatorial hexapeptide library.
Synapse (New York, N.Y.) 1999;33(3):239-46.
1999: SY Yeh; Christina M Dersch; R Rothman; Jean Lud Cadet
Effects of antihistamines on 3, 4-methylenedioxymethamphetamine-induced depletion of serotonin in rats.
Synapse (New York, N.Y.) 1999;33(3):207-17.
1999: Richard B Rothman; Mario A Ayestas; Christina M Dersch; Michael H Baumann
Aminorex, fenfluramine, and chlorphentermine are serotonin transporter substrates. Implications for primary pulmonary hypertension.
Circulation 1999;100(8):869-75.
1999: Andrew Coop; Richard B Rothman; Christina M Dersch; John S Partilla; F Porreca; P Davis; Arthur E Jacobson; Kenner C Rice
delta Opioid affinity and selectivity of 4-hydroxy-3-methoxyindolomorphinan analogues related to naltrindole.
Journal of medicinal chemistry 1999;42(9):1673-9.
1998: James B Thomas; M J Fall; J B Cooper; Richard B Rothman; Wayne Mascarella; Heng Xu; John S Partilla; Christina M Dersch; KB McCullough; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
Identification of an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Journal of medicinal chemistry 1998;41(26):5188-97.
1998: James B Thomas; X Zheng; Wayne Mascarella; Richard B Rothman; Christina M Dersch; John S Partilla; Judith L Flippen-Anderson; CF George; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
N-Substituted 9beta-methyl-5-(3-hydroxyphenyl)morphans are opioid receptor pure antagonists.
Journal of medicinal chemistry 1998;41(21):4143-9.
1998: James B Thomas; Wayne Mascarella; Richard B Rothman; John S Partilla; Heng Xu; KB McCullough; Christina M Dersch; Buddy E Cantrell; Dennis M Zimmerman; Frank carroll
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Journal of medicinal chemistry 1998;41(11):1980-90.
1998: H Kubota; Richard B Rothman; Christina M Dersch; K McCullough; J Pinto; Kenner C Rice
Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives.
Bioorganic & medicinal chemistry letters 1998;8(7):799-804.
1998: Richard B Rothman; M L Silverthorn; John R Glowa; Dorota Matecka; Kenner C Rice; Frank carroll; John S Partilla; George R. Uhl; David J Vandenbergh; Christina M Dersch
Studies of the biogenic amine transporters. VII. Characterization of a novel cocaine binding site identified with [125I]RTI-55 in membranes prepared from human, monkey and guinea pig caudate.
Synapse (New York, N.Y.) 1998;28(4):322-38.
1997: Dorota Matecka; David Lewis; Richard B Rothman; Christina M Dersch; F H Wojnicki; John R Glowa; AC DeVries; A Pert; Kenner C Rice
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
Journal of medicinal chemistry 1997;40(5):705-16.
1996: Dorota Matecka; Richard B Rothman; L Radesca; B R de Costa; Christina M Dersch; John S Partilla; A Pert; John R Glowa; F H Wojnicki; Kenner C Rice
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
Journal of medicinal chemistry 1996;39(24):4704-16.
1995: M L Silverthorn; Christina M Dersch; Michael H Baumann; Jean Lud Cadet; John S Partilla; Kenner C Rice; Frank carroll; K M Becketts; A Brockington; Richard B Rothman
Studies of the biogenic amine transporters. V. Demonstration of two binding sites for the cocaine analog [125I]RTI-55 associated with the 5-HT transporter in rat brain membranes.
The Journal of pharmacology and experimental therapeutics 1995;273(1):213-22.
1994: H C Akunne; Christina M Dersch; Jean Lud Cadet; Michael H Baumann; G U Char; John S Partilla; B R de Costa; Kenner C Rice; Frank carroll; Richard B Rothman
Studies of the biogenic amine transporters. III. Demonstration of two binding sites for [3H]GBR12935 and [3H]BTCP in rat caudate membranes.
The Journal of pharmacology and experimental therapeutics 1994;268(3):1462-75.
1994: Christina M Dersch; H C Akunne; John S Partilla; G U Char; B R de Costa; Kenner C Rice; Frank carroll; Richard B Rothman
Studies of the biogenic amine transporters. 1. Dopamine reuptake blockers inhibit [3H]mazindol binding to the dopamine transporter by a competitive mechanism: preliminary evidence for different binding domains.
Neurochemical research 1994;19(2):201-8.
1993: Richard B Rothman; B Lewis; Christina M Dersch; Heng Xu; L Radesca; B R de Costa; Kenner C Rice; R B Kilburn; H C Akunne; A Pert
Identification of a GBR12935 homolog, LR1111, which is over 4,000-fold selective for the dopamine transporter, relative to serotonin and norepinephrine transporters.
Synapse (New York, N.Y.) 1993;14(1):34-9.
1993: Richard B Rothman; K M Becketts; L R Radesca; B R de Costa; Kenner C Rice; Frank carroll; Christina M Dersch
Studies of the biogenic amine transporters. II. A brief study on the use of [3H]DA-uptake-inhibition to transporter-binding-inhibition ratios for the in vitro evaluation of putative cocaine antagonists.
Life sciences 1993;53(17):PL267-72.