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Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.

Slack RD, Ku TC, Cao J, Giancola JB, Bonifazi A, Loland CJ, Gadiano A, Lam J, Rais R, Slusher BS, Coggiano M, Tanda G, Newman AH.

J Med Chem. 2019 Nov 14. doi: 10.1021/acs.jmedchem.9b01188. [Epub ahead of print]


Newly Developed Dopamine D3 Receptor Antagonists, R-VK4-40 and R-VK4-116, Do Not Potentiate Cardiovascular Effects of Cocaine or Oxycodone in Rats.

Jordan CJ, Humburg BA, Thorndike EB, Shaik AB, Xi ZX, Baumann MH, Newman AH, Schindler CW.

J Pharmacol Exp Ther. 2019 Dec;371(3):602-614. doi: 10.1124/jpet.119.259390. Epub 2019 Sep 27.


Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D3 Receptor Antagonists and Partial Agonists.

Shaik AB, Kumar V, Bonifazi A, Guerrero AM, Cemaj SL, Gadiano A, Lam J, Xi ZX, Rais R, Slusher BS, Newman AH.

J Med Chem. 2019 Oct 24;62(20):9061-9077. doi: 10.1021/acs.jmedchem.9b00607. Epub 2019 Oct 15.


2016 Philip S. Portoghese Medicinal Chemistry Lectureship: Designing Bivalent or Bitopic Molecules for G-Protein Coupled Receptors. The Whole Is Greater Than the Sum of Its Parts.

Newman AH, Battiti FO, Bonifazi A.

J Med Chem. 2019 Sep 24. doi: 10.1021/acs.jmedchem.9b01105. [Epub ahead of print]


A Novel Bromine-Containing Paroxetine Analogue Provides Mechanistic Clues for Binding Ambiguity at the Central Primary Binding Site of the Serotonin Transporter.

Slack RD, Abramyan AM, Tang H, Meena S, Davis BA, Bonifazi A, Giancola JB, Deschamps JR, Naing S, Yano H, Singh SK, Newman AH, Shi L.

ACS Chem Neurosci. 2019 Sep 18;10(9):3946-3952. doi: 10.1021/acschemneuro.9b00375. Epub 2019 Aug 22.


The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D3 Receptor (D3R) Selective Agonists.

Battiti FO, Cemaj SL, Guerrero AM, Shaik AB, Lam J, Rais R, Slusher BS, Deschamps JR, Imler GH, Newman AH, Bonifazi A.

J Med Chem. 2019 Jul 11;62(13):6287-6314. doi: 10.1021/acs.jmedchem.9b00702. Epub 2019 Jul 1.


How to rescue misfolded SERT, DAT and NET: targeting conformational intermediates with atypical inhibitors and partial releasers.

Bhat S, Newman AH, Freissmuth M.

Biochem Soc Trans. 2019 Jun 28;47(3):861-874. doi: 10.1042/BST20180512. Epub 2019 May 7. Review.


Progress in agonist therapy for substance use disorders: Lessons learned from methadone and buprenorphine.

Jordan CJ, Cao J, Newman AH, Xi ZX.

Neuropharmacology. 2019 Nov 1;158:107609. doi: 10.1016/j.neuropharm.2019.04.015. Epub 2019 Apr 19. Review.


Synaptic Vesicle Recycling Pathway Determines Neurotransmitter Content and Release Properties.

Silm K, Yang J, Marcott PF, Asensio CS, Eriksen J, Guthrie DA, Newman AH, Ford CP, Edwards RH.

Neuron. 2019 May 22;102(4):786-800.e5. doi: 10.1016/j.neuron.2019.03.031. Epub 2019 Apr 16.


The highly selective dopamine D3R antagonist, R-VK4-40 attenuates oxycodone reward and augments analgesia in rodents.

Jordan CJ, Humburg B, Rice M, Bi GH, You ZB, Shaik AB, Cao J, Bonifazi A, Gadiano A, Rais R, Slusher B, Newman AH, Xi ZX.

Neuropharmacology. 2019 Nov 1;158:107597. doi: 10.1016/j.neuropharm.2019.04.003. Epub 2019 Apr 8.


Biased G Protein-Independent Signaling of Dopamine D1-D3 Receptor Heteromers in the Nucleus Accumbens.

Guitart X, Moreno E, Rea W, Sánchez-Soto M, Cai NS, Quiroz C, Kumar V, Bourque L, Cortés A, Canela EI, Bishop C, Newman AH, Casadó V, Ferré S.

Mol Neurobiol. 2019 Oct;56(10):6756-6769. doi: 10.1007/s12035-019-1564-8. Epub 2019 Mar 27.


Opioid-galanin receptor heteromers mediate the dopaminergic effects of opioids.

Cai NS, Quiroz C, Bonaventura J, Bonifazi A, Cole TO, Purks J, Billing AS, Massey E, Wagner M, Wish ED, Guitart X, Rea W, Lam S, Moreno E, Casadó-Anguera V, Greenblatt AD, Jacobson AE, Rice KC, Casadó V, Newman AH, Winkelman JW, Michaelides M, Weintraub E, Volkow ND, Belcher AM, Ferré S.

J Clin Invest. 2019 Mar 26;129(7):2730-2744. doi: 10.1172/JCI126912.


Dopamine D4 Receptor-Selective Compounds Reveal Structure-Activity Relationships that Engender Agonist Efficacy.

Keck TM, Free RB, Day MM, Brown SL, Maddaluna MS, Fountain G, Cooper C, Fallon B, Holmes M, Stang CT, Burkhardt R, Bonifazi A, Ellenberger MP, Newman AH, Sibley DR, Wu C, Boateng CA.

J Med Chem. 2019 Apr 11;62(7):3722-3740. doi: 10.1021/acs.jmedchem.9b00231. Epub 2019 Apr 1.


Selective D2 and D3 receptor antagonists oppositely modulate cocaine responses in mice via distinct postsynaptic mechanisms in nucleus accumbens.

Manvich DF, Petko AK, Branco RC, Foster SL, Porter-Stransky KA, Stout KA, Newman AH, Miller GW, Paladini CA, Weinshenker D.

Neuropsychopharmacology. 2019 Jul;44(8):1445-1455. doi: 10.1038/s41386-019-0371-2. Epub 2019 Mar 16.


Translating the atypical dopamine uptake inhibitor hypothesis toward therapeutics for treatment of psychostimulant use disorders.

Newman AH, Cao J, Keighron JD, Jordan CJ, Bi GH, Liang Y, Abramyan AM, Avelar AJ, Tschumi CW, Beckstead MJ, Shi L, Tanda G, Xi ZX.

Neuropsychopharmacology. 2019 Jul;44(8):1435-1444. doi: 10.1038/s41386-019-0366-z. Epub 2019 Mar 11.


Novel and Potent Dopamine D2 Receptor Go-Protein Biased Agonists.

Bonifazi A, Yano H, Guerrero AM, Kumar V, Hoffman AF, Lupica CR, Shi L, Newman AH.

ACS Pharmacol Transl Sci. 2019 Feb 8;2(1):52-65. doi: 10.1021/acsptsci.8b00060. Epub 2019 Jan 14.


Effects of ( R)-Modafinil and Modafinil Analogues on Dopamine Dynamics Assessed by Voltammetry and Microdialysis in the Mouse Nucleus Accumbens Shell.

Keighron JD, Quarterman JC, Cao J, DeMarco EM, Coggiano MA, Gleaves A, Slack RD, Zanettini C, Newman AH, Tanda G.

ACS Chem Neurosci. 2019 Apr 17;10(4):2012-2021. doi: 10.1021/acschemneuro.8b00340. Epub 2019 Jan 31.


Multitarget 1,4-Dioxane Compounds Combining Favorable D2-like and 5-HT1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.

Del Bello F, Ambrosini D, Bonifazi A, Newman AH, Keck TM, Giannella M, Giorgioni G, Piergentili A, Cappellacci L, Cilia A, Franchini S, Quaglia W.

ACS Chem Neurosci. 2019 May 15;10(5):2222-2228. doi: 10.1021/acschemneuro.8b00677. Epub 2019 Jan 9.


Dopamine D3R antagonist VK4-116 attenuates oxycodone self-administration and reinstatement without compromising its antinociceptive effects.

You ZB, Bi GH, Galaj E, Kumar V, Cao J, Gadiano A, Rais R, Slusher BS, Gardner EL, Xi ZX, Newman AH.

Neuropsychopharmacology. 2019 Jul;44(8):1415-1424. doi: 10.1038/s41386-018-0284-5. Epub 2018 Nov 27.


Pharmacological classification of centrally acting drugs using EEG in freely moving rats: an old tool to identify new atypical dopamine uptake inhibitors.

Zanettini C, Scaglione A, Keighron JD, Giancola JB, Lin SC, Newman AH, Tanda G.

Neuropharmacology. 2019 Dec 15;161:107446. doi: 10.1016/j.neuropharm.2018.11.034. Epub 2018 Nov 24.


Distinct effects of (R)-modafinil and its (R)- and (S)-fluoro-analogs on mesolimbic extracellular dopamine assessed by voltammetry and microdialysis in rats.

Keighron JD, Giancola JB, Shaffer RJ, DeMarco EM, Coggiano MA, Slack RD, Newman AH, Tanda G.

Eur J Neurosci. 2019 Aug;50(3):2045-2053. doi: 10.1111/ejn.14256. Epub 2018 Dec 1.


Computation-guided analysis of paroxetine binding to hSERT reveals functionally important structural elements and dynamics.

Abramyan AM, Slack RD, Meena S, Davis BA, Newman AH, Singh SK, Shi L.

Neuropharmacology. 2019 Dec 15;161:107411. doi: 10.1016/j.neuropharm.2018.10.040. Epub 2018 Nov 1.


[O-methyl-11C]N-(4-(4-(3-Chloro-2-methoxyphenyl)-piperazin-1-yl)butyl)-1H-indole-2-carboxamide ([11C]BAK4-51) Is an Efflux Transporter Substrate and Ineffective for PET Imaging of Brain D₃ Receptors in Rodents and Monkey.

Liow JS, Morse CL, Lu S, Frankland M, Tye GL, Zoghbi SS, Gladding RL, Shaik AB, Innis RB, Newman AH, Pike VW.

Molecules. 2018 Oct 23;23(11). pii: E2737. doi: 10.3390/molecules23112737.


Identification of the benztropine analog [125I]GA II 34 binding site on the human dopamine transporter.

Tomlinson MJ, Krout D, Pramod AB, Lever JR, Newman AH, Henry LK, Vaughan RA.

Neurochem Int. 2019 Feb;123:34-45. doi: 10.1016/j.neuint.2018.08.008. Epub 2018 Aug 17.


Regional Heterogeneity of D2-Receptor Signaling in the Dorsal Striatum and Nucleus Accumbens.

Marcott PF, Gong S, Donthamsetti P, Grinnell SG, Nelson MN, Newman AH, Birnbaumer L, Martemyanov KA, Javitch JA, Ford CP.

Neuron. 2018 May 2;98(3):575-587.e4. doi: 10.1016/j.neuron.2018.03.038. Epub 2018 Apr 12.


Yawning elicited by intravenous ethanol in rhesus monkeys with experience self-administering cocaine and ethanol: Involvement of dopamine D3 receptors.

Czoty PW, John WS, Newman AH, Nader MA.

Alcohol. 2018 Jun;69:1-5. doi: 10.1016/j.alcohol.2017.10.003. Epub 2017 Oct 17.


Effects of the nicotinic agonist varenicline, nicotinic antagonist r-bPiDI, and DAT inhibitor (R)-modafinil on co-use of ethanol and nicotine in female P rats.

Maggio SE, Saunders MA, Baxter TA, Nixon K, Prendergast MA, Zheng G, Crooks P, Dwoskin LP, Slack RD, Newman AH, Bell RL, Bardo MT.

Psychopharmacology (Berl). 2018 May;235(5):1439-1453. doi: 10.1007/s00213-018-4853-4. Epub 2018 Feb 18.


Pharmacological profiling of sigma 1 receptor ligands by novel receptor homomer assays.

Yano H, Bonifazi A, Xu M, Guthrie DA, Schneck SN, Abramyan AM, Fant AD, Hong WC, Newman AH, Shi L.

Neuropharmacology. 2018 May 1;133:264-275. doi: 10.1016/j.neuropharm.2018.01.042. Epub 2018 Jan 31.


Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.

Zou MF, Cao J, Abramyan AM, Kopajtic T, Zanettini C, Guthrie DA, Rais R, Slusher BS, Shi L, Loland CJ, Newman AH.

J Med Chem. 2017 Dec 28;60(24):10172-10187. doi: 10.1021/acs.jmedchem.7b01454. Epub 2017 Dec 11.


Atypical dopamine transporter inhibitors attenuate compulsive-like methamphetamine self-administration in rats.

Tunstall BJ, Ho CP, Cao J, Vendruscolo JCM, Schmeichel BE, Slack RD, Tanda G, Gadiano AJ, Rais R, Slusher BS, Koob GF, Newman AH, Vendruscolo LF.

Neuropharmacology. 2018 Mar 15;131:96-103. doi: 10.1016/j.neuropharm.2017.12.006. Epub 2017 Dec 5.


Targeting hypersensitive corticostriatal terminals in restless legs syndrome.

Yepes G, Guitart X, Rea W, Newman AH, Allen RP, Earley CJ, Quiroz C, Ferré S.

Ann Neurol. 2017 Dec;82(6):951-960. doi: 10.1002/ana.25104. Epub 2017 Dec 7.


The novel dopamine D3 receptor antagonists/partial agonists CAB2-015 and BAK4-54 inhibit oxycodone-taking and oxycodone-seeking behavior in rats.

You ZB, Gao JT, Bi GH, He Y, Boateng C, Cao J, Gardner EL, Newman AH, Xi ZX.

Neuropharmacology. 2017 Nov;126:190-199. doi: 10.1016/j.neuropharm.2017.09.007. Epub 2017 Sep 6.


Inhibitor mechanisms in the S1 binding site of the dopamine transporter defined by multi-site molecular tethering of photoactive cocaine analogs.

Krout D, Pramod AB, Dahal RA, Tomlinson MJ, Sharma B, Foster JD, Zou MF, Boatang C, Newman AH, Lever JR, Vaughan RA, Henry LK.

Biochem Pharmacol. 2017 Oct 15;142:204-215. doi: 10.1016/j.bcp.2017.07.015. Epub 2017 Jul 19.


Targeting of dopamine transporter to filopodia requires an outward-facing conformation of the transporter.

Ma S, Cheng MH, Guthrie DA, Newman AH, Bahar I, Sorkin A.

Sci Rep. 2017 Jul 14;7(1):5399. doi: 10.1038/s41598-017-05637-x.


Atypical dopamine transporter inhibitors R-modafinil and JHW 007 differentially affect D2 autoreceptor neurotransmission and the firing rate of midbrain dopamine neurons.

Avelar AJ, Cao J, Newman AH, Beckstead MJ.

Neuropharmacology. 2017 Sep 1;123:410-419. doi: 10.1016/j.neuropharm.2017.06.016. Epub 2017 Jun 15.


A Novel PKC Inhibitor Shows Promise for Amphetamine Use Disorders.

Newman AH.

Neuropsychopharmacology. 2017 Sep;42(10):1929-1930. doi: 10.1038/npp.2017.116. Epub 2017 Jun 8. No abstract available.


Novel Bivalent Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine D2 Receptor (D2R) Biased Agonism.

Bonifazi A, Yano H, Ellenberger MP, Muller L, Kumar V, Zou MF, Cai NS, Guerrero AM, Woods AS, Shi L, Newman AH.

J Med Chem. 2017 Apr 13;60(7):2890-2907. doi: 10.1021/acs.jmedchem.6b01875. Epub 2017 Mar 16.


The Novel Modafinil Analog, JJC8-016, as a Potential Cocaine Abuse Pharmacotherapeutic.

Zhang HY, Bi GH, Yang HJ, He Y, Xue G, Cao J, Tanda G, Gardner EL, Newman AH, Xi ZX.

Neuropsychopharmacology. 2017 Aug;42(9):1871-1883. doi: 10.1038/npp.2017.41. Epub 2017 Mar 7.


Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R).

Kumar V, Moritz AE, Keck TM, Bonifazi A, Ellenberger MP, Sibley CD, Free RB, Shi L, Lane JR, Sibley DR, Newman AH.

J Med Chem. 2017 Feb 23;60(4):1478-1494. doi: 10.1021/acs.jmedchem.6b01688. Epub 2017 Feb 10.


Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor.

Michino M, Boateng CA, Donthamsetti P, Yano H, Bakare OM, Bonifazi A, Ellenberger MP, Keck TM, Kumar V, Zhu C, Verma R, Deschamps JR, Javitch JA, Newman AH, Shi L.

J Med Chem. 2017 Jan 26;60(2):580-593. doi: 10.1021/acs.jmedchem.6b01148. Epub 2017 Jan 5.


Novel and High Affinity 2-[(Diphenylmethyl)sulfinyl]acetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors.

Cao J, Slack RD, Bakare OM, Burzynski C, Rais R, Slusher BS, Kopajtic T, Bonifazi A, Ellenberger MP, Yano H, He Y, Bi GH, Xi ZX, Loland CJ, Newman AH.

J Med Chem. 2016 Dec 8;59(23):10676-10691. Epub 2016 Nov 28.


The unique psychostimulant profile of (±)-modafinil: investigation of behavioral and neurochemical effects in mice.

Mereu M, Chun LE, Prisinzano TE, Newman AH, Katz JL, Tanda G.

Eur J Neurosci. 2017 Jan;45(1):167-174. doi: 10.1111/ejn.13376. Epub 2016 Sep 11.


Highly Selective Dopamine D3 Receptor (D3R) Antagonists and Partial Agonists Based on Eticlopride and the D3R Crystal Structure: New Leads for Opioid Dependence Treatment.

Kumar V, Bonifazi A, Ellenberger MP, Keck TM, Pommier E, Rais R, Slusher BS, Gardner E, You ZB, Xi ZX, Newman AH.

J Med Chem. 2016 Aug 25;59(16):7634-50. doi: 10.1021/acs.jmedchem.6b00860. Epub 2016 Aug 10.


Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.

Zou MF, Keck TM, Kumar V, Donthamsetti P, Michino M, Burzynski C, Schweppe C, Bonifazi A, Free RB, Sibley DR, Janowsky A, Shi L, Javitch JA, Newman AH.

J Med Chem. 2016 Apr 14;59(7):2973-88. doi: 10.1021/acs.jmedchem.5b01612. Epub 2016 Apr 1.


A Novel Class of Dopamine D4 Receptor Ligands Bearing an Imidazoline Nucleus.

Mammoli V, Bonifazi A, Dal Ben D, Giannella M, Giorgioni G, Piergentili A, Pigini M, Quaglia W, Thomas A, Newman AH, Ferré S, Sanchez-Soto M, Keck TM, Del Bello F.

ChemMedChem. 2016 Aug 19;11(16):1819-28. doi: 10.1002/cmdc.201600022. Epub 2016 Mar 15.


Evidence for Noncanonical Neurotransmitter Activation: Norepinephrine as a Dopamine D2-Like Receptor Agonist.

Sánchez-Soto M, Bonifazi A, Cai NS, Ellenberger MP, Newman AH, Ferré S, Yano H.

Mol Pharmacol. 2016 Apr;89(4):457-66. doi: 10.1124/mol.115.101808. Epub 2016 Feb 3.


Membrane potential shapes regulation of dopamine transporter trafficking at the plasma membrane.

Richardson BD, Saha K, Krout D, Cabrera E, Felts B, Henry LK, Swant J, Zou MF, Newman AH, Khoshbouei H.

Nat Commun. 2016 Jan 25;7:10423. doi: 10.1038/ncomms10423.


Differential Internalization Rates and Postendocytic Sorting of the Norepinephrine and Dopamine Transporters Are Controlled by Structural Elements in the N Termini.

Vuorenpää A, Jørgensen TN, Newman AH, Madsen KL, Scheinin M, Gether U.

J Biol Chem. 2016 Mar 11;291(11):5634-51. doi: 10.1074/jbc.M115.702050. Epub 2016 Jan 19.


Nanopharmacological Force Sensing to Reveal Allosteric Coupling in Transporter Binding Sites.

Zhu R, Sinwel D, Hasenhuetl PS, Saha K, Kumar V, Zhang P, Rankl C, Holy M, Sucic S, Kudlacek O, Karner A, Sandtner W, Stockner T, Gruber HJ, Freissmuth M, Newman AH, Sitte HH, Hinterdorfer P.

Angew Chem Int Ed Engl. 2016 Jan 26;55(5):1719-22. doi: 10.1002/anie.201508755. Epub 2015 Dec 22.


Binding Mode Selection Determines the Action of Ecstasy Homologs at Monoamine Transporters.

Sandtner W, Stockner T, Hasenhuetl PS, Partilla JS, Seddik A, Zhang YW, Cao J, Holy M, Steinkellner T, Rudnick G, Baumann MH, Ecker GF, Newman AH, Sitte HH.

Mol Pharmacol. 2016 Jan;89(1):165-75. doi: 10.1124/mol.115.101394. Epub 2015 Oct 30.

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