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Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3R)-7-Hydroxy-N-[(1S)-2-methyl-1-(piperidin-1-ylmethyl)propyl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (PDTic).

Ondachi PW, Kormos CM, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI.

J Med Chem. 2018 Aug 17. doi: 10.1021/acs.jmedchem.8b00673. [Epub ahead of print]


A Double-Blind, Placebo-Controlled Trial Demonstrating the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of RTI-336.

Carroll FI, Kosten TR, Buda JJ, Wang L, Walters BB.

Front Pharmacol. 2018 Jul 10;9:712. doi: 10.3389/fphar.2018.00712. eCollection 2018.


Potent and Selective Tetrahydroisoquinoline Kappa Opioid Receptor Antagonists of Lead Compound (3R)-N-[(1R)-1-(Cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (CDTic).

Kormos CM, Ondachi PW, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Fennell TR, Snyder RW, Carroll FI.

J Med Chem. 2018 Jul 22. doi: 10.1021/acs.jmedchem.8b00674. [Epub ahead of print]


New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.

Bagdas D, Alkhlaif Y, Jackson A, Carroll FI, Ditre JW, Damaj MI.

Neuropharmacology. 2018 Aug;138:72-79. doi: 10.1016/j.neuropharm.2018.05.025. Epub 2018 May 21.


Effect of nicotine and alpha-7 nicotinic modulators on visceral pain-induced conditioned place aversion in mice.

Bagdas D, Meade JA, Alkhlaif Y, Muldoon PP, Carroll FI, Damaj MI.

Eur J Pain. 2018 Apr 10. doi: 10.1002/ejp.1231. [Epub ahead of print]


Opioid Dose- and Route-Dependent Efficacy of Oxycodone and Heroin Vaccines in Rats.

Raleigh MD, Laudenbach M, Baruffaldi F, Peterson SJ, Roslawski MJ, Birnbaum AK, Carroll FI, Runyon SP, Winston S, Pentel PR, Pravetoni M.

J Pharmacol Exp Ther. 2018 May;365(2):346-353. doi: 10.1124/jpet.117.247049. Epub 2018 Mar 13.


The κ-opioid receptor antagonist JDTic decreases ethanol intake in alcohol-preferring AA rats.

Uhari-Väänänen J, Raasmaja A, Bäckström P, Oinio V, Carroll FI, Airavaara M, Kiianmaa K, Piepponen P.

Psychopharmacology (Berl). 2018 May;235(5):1581-1591. doi: 10.1007/s00213-018-4868-x. Epub 2018 Feb 28.


Sex Differences in the Effects of a Kappa Opioid Receptor Antagonist in the Forced Swim Test.

Laman-Maharg A, Williams AV, Zufelt MD, Minie VA, Ramos-Maciel S, Hao R, Ordoñes Sanchez E, Copeland T, Silverman JL, Leigh A, Snyder R, Carroll FI, Fennell TR, Trainor BC.

Front Pharmacol. 2018 Feb 14;9:93. doi: 10.3389/fphar.2018.00093. eCollection 2018.


Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor.

Che T, Majumdar S, Zaidi SA, Ondachi P, McCorvy JD, Wang S, Mosier PD, Uprety R, Vardy E, Krumm BE, Han GW, Lee MY, Pardon E, Steyaert J, Huang XP, Strachan RT, Tribo AR, Pasternak GW, Carroll FI, Stevens RC, Cherezov V, Katritch V, Wacker D, Roth BL.

Cell. 2018 Jan 11;172(1-2):55-67.e15. doi: 10.1016/j.cell.2017.12.011. Epub 2018 Jan 4.


Safety and efficacy of an oxycodone vaccine: Addressing some of the unique considerations posed by opioid abuse.

Raleigh MD, Peterson SJ, Laudenbach M, Baruffaldi F, Carroll FI, Comer SD, Navarro HA, Langston TL, Runyon SP, Winston S, Pravetoni M, Pentel PR.

PLoS One. 2017 Dec 1;12(12):e0184876. doi: 10.1371/journal.pone.0184876. eCollection 2017.


Caged Naloxone: Synthesis, Characterization, and Stability of 3- O-(4,5-Dimethoxy-2-nitrophenyl)carboxymethyl Naloxone (CNV-NLX).

Lewin AH, Fix SE, Zhong D, Mayer LD, Burgess JP, Mascarella SW, Reddy PA, Seltzman HH, Carroll FI.

ACS Chem Neurosci. 2018 Mar 21;9(3):563-567. doi: 10.1021/acschemneuro.7b00378. Epub 2017 Dec 8.


Dissociable effects of the kappa opioid receptor agonist nalfurafine on pain/itch-stimulated and pain/itch-depressed behaviors in male rats.

Lazenka ML, Moerke MJ, Townsend EA, Freeman KB, Carroll FI, Negus SS.

Psychopharmacology (Berl). 2018 Jan;235(1):203-213. doi: 10.1007/s00213-017-4758-7. Epub 2017 Oct 24.


Simple Tetrahydroisoquinolines Are Potent and Selective Kappa Opioid Receptor Antagonists.

Kormos CM, Ondachi PW, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Carroll FI.

ACS Med Chem Lett. 2017 May 25;8(7):742-745. doi: 10.1021/acsmedchemlett.7b00115. eCollection 2017 Jul 13.


Effects of Chronic Social Defeat Stress on Sleep and Circadian Rhythms Are Mitigated by Kappa-Opioid Receptor Antagonism.

Wells AM, Ridener E, Bourbonais CA, Kim W, Pantazopoulos H, Carroll FI, Kim KS, Cohen BM, Carlezon WA Jr.

J Neurosci. 2017 Aug 9;37(32):7656-7668. doi: 10.1523/JNEUROSCI.0885-17.2017. Epub 2017 Jul 3.


In silico design of novel probes for the atypical opioid receptor MRGPRX2.

Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL.

Nat Chem Biol. 2017 May;13(5):529-536. doi: 10.1038/nchembio.2334. Epub 2017 Mar 13.


In vivo interactions between α7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α: Implication for nicotine dependence.

Jackson A, Bagdas D, Muldoon PP, Lichtman AH, Carroll FI, Greenwald M, Miles MF, Damaj MI.

Neuropharmacology. 2017 May 15;118:38-45. doi: 10.1016/j.neuropharm.2017.03.005. Epub 2017 Mar 7.


Probing the Allosteric Role of the α5 Subunit of α3β4α5 Nicotinic Acetylcholine Receptors by Functionally Selective Modulators and Ligands.

Ray C, Soderblom EJ, Bai Y, Carroll FI, Caron MG, Barak LS.

ACS Chem Biol. 2017 Mar 17;12(3):702-714. doi: 10.1021/acschembio.6b01117. Epub 2017 Jan 24.


Design, Synthesis, and Biological Evaluation of Structurally Rigid Analogues of 4-(3-Hydroxyphenyl)piperidine Opioid Receptor Antagonists.

Runyon SP, Kormos CM, Gichinga MG, Mascarella SW, Navarro HA, Deschamps JR, Imler GH, Carroll FI.

J Org Chem. 2016 Nov 4;81(21):10383-10391. Epub 2016 Aug 2.


Sex Differences and Drug Dose Influence the Role of the α7 Nicotinic Acetylcholine Receptor in the Mouse Dextran Sodium Sulfate-Induced Colitis Model.

AlSharari SD, Bagdas D, Akbarali HI, Lichtman PA, Raborn ES, Cabral GA, Carroll FI, McGee EA, Damaj MI.

Nicotine Tob Res. 2017 Apr 1;19(4):460-468. doi: 10.1093/ntr/ntw245.


Synthesis, Nicotinic Acetylcholine Receptor Binding, and in Vitro and in Vivo Pharmacological Properties of 2'-Fluoro-(substituted thiophenyl)deschloroepibatidine Analogues.

Ondachi PW, Castro AH, Sherman B, Luetje CW, Damaj MI, Mascarella SW, Navarro HA, Carroll FI.

ACS Chem Neurosci. 2017 Jan 18;8(1):115-127. doi: 10.1021/acschemneuro.6b00252. Epub 2016 Oct 20.


Pharmacodynamic Relationships between Duration of Action of JDTic-like Kappa-Opioid Receptor Antagonists and Their Brain and Plasma Pharmacokinetics in Rats.

Owens SM, Pollard GT, Howard JL, Fennell TR, Snyder RW, Carroll FI.

ACS Chem Neurosci. 2016 Dec 21;7(12):1737-1745. doi: 10.1021/acschemneuro.6b00249. Epub 2016 Oct 4.


Attenuated nicotine-like effects of varenicline but not other nicotinic ACh receptor agonists in monkeys receiving nicotine daily.

Cunningham CS, Moerke MJ, Javors MA, Carroll FI, McMahon LR.

Br J Pharmacol. 2016 Dec;173(24):3454-3466. doi: 10.1111/bph.13635. Epub 2016 Nov 6.


Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of replacement of the 3-hydroxyphenyl group with pyridine or thiophene bioisosteres.

Kormos CM, Gichinga MG, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA, Carroll FI.

Bioorg Med Chem. 2016 Aug 15;24(16):3842-8. doi: 10.1016/j.bmc.2016.06.029. Epub 2016 Jun 15.


Synthesis, Nicotinic Acetylcholine Binding, and in Vitro and in Vivo Pharmacological Properties of 2'-Fluoro-(carbamoylpyridinyl)deschloroepibatidine Analogues.

Ondachi PW, Castro AH, Luetje CW, Wageman CR, Marks MJ, Damaj MI, Mascarella SW, Navarro HA, Carroll FI.

ACS Chem Neurosci. 2016 Jul 20;7(7):1004-12. doi: 10.1021/acschemneuro.6b00107. Epub 2016 May 19.


Early adolescent nicotine exposure affects later-life cocaine reward in mice.

Alajaji M, Lazenka MF, Kota D, Wise LE, Younis RM, Carroll FI, Levine A, Selley DE, Sim-Selley LJ, Damaj MI.

Neuropharmacology. 2016 Jun;105:308-317. doi: 10.1016/j.neuropharm.2016.01.032. Epub 2016 Jan 22.


Nicotine Enhances the Hypnotic and Hypothermic Effects of Alcohol in the Mouse.

Slater CA, Jackson A, Muldoon PP, Dawson A, O'Brien M, Soll LG, Abdullah R, Carroll FI, Tapper AR, Miles MF, Banks ML, Bettinger JC, Damaj IM.

Alcohol Clin Exp Res. 2016 Jan;40(1):62-72. doi: 10.1111/acer.12918.


Expression and pharmacological modulation of visceral pain-induced conditioned place aversion in mice.

Bagdas D, Muldoon PP, AlSharari S, Carroll FI, Negus SS, Damaj MI.

Neuropharmacology. 2016 Mar;102:236-43. doi: 10.1016/j.neuropharm.2015.11.024. Epub 2015 Nov 27.


Comparison of effects produced by nicotine and the α4β2-selective agonist 5-I-A-85380 on intracranial self-stimulation in rats.

Freitas K, Carroll FI, Negus SS.

Exp Clin Psychopharmacol. 2016 Feb;24(1):65-75. doi: 10.1037/pha0000055.


The frequency of early-activated hapten-specific B cell subsets predicts the efficacy of vaccines for nicotine dependence.

Laudenbach M, Tucker AM, Runyon SP, Carroll FI, Pravetoni M.

Vaccine. 2015 Nov 17;33(46):6332-9. doi: 10.1016/j.vaccine.2015.09.015. Epub 2015 Sep 26.


Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198).

Chang SD, Brieaddy LE, Harvey JD, Lewin AH, Mascarella SW, Seltzman HH, Reddy PA, Decker AM, McElhinny CJ Jr, Zhong D, Peterson EE, Navarro HA, Bruchas MR, Carroll FI.

ACS Chem Neurosci. 2015 Dec 16;6(12):1956-64. doi: 10.1021/acschemneuro.5b00208. Epub 2015 Sep 30.


Effects of nicotinic acetylcholine receptor agonists in assays of acute pain-stimulated and pain-depressed behaviors in rats.

Freitas KC, Carroll FI, Negus SS.

J Pharmacol Exp Ther. 2015 Nov;355(2):341-50. doi: 10.1124/jpet.115.226803.


Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.

Carroll FI, Gichinga MG, Kormos CM, Maitra R, Runyon SP, Thomas JB, Mascarella SW, Decker AM, Navarro HA.

Bioorg Med Chem. 2015 Oct 1;23(19):6379-88. doi: 10.1016/j.bmc.2015.08.025. Epub 2015 Aug 25.


Synthesis, nicotinic acetylcholine receptor binding, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs.

Ondachi PW, Ye Z, Castro AH, Luetje CW, Damaj MI, Mascarella SW, Navarro HA, Carroll FI.

Bioorg Med Chem. 2015 Sep 1;23(17):5693-701. doi: 10.1016/j.bmc.2015.07.021. Epub 2015 Jul 17.


Pituitary Adenylate Cyclase-Activating Polypeptide Disrupts Motivation, Social Interaction, and Attention in Male Sprague Dawley Rats.

Donahue RJ, Venkataraman A, Carroll FI, Meloni EG, Carlezon WA Jr.

Biol Psychiatry. 2016 Dec 15;80(12):955-964. doi: 10.1016/j.biopsych.2015.06.013. Epub 2015 Jun 19.


Quantitative Signaling and Structure-Activity Analyses Demonstrate Functional Selectivity at the Nociceptin/Orphanin FQ Opioid Receptor.

Chang SD, Mascarella SW, Spangler SM, Gurevich VV, Navarro HA, Carroll FI, Bruchas MR.

Mol Pharmacol. 2015 Sep;88(3):502-11. doi: 10.1124/mol.115.099150. Epub 2015 Jul 1.


Effects of acute and chronic social defeat stress are differentially mediated by the dynorphin/kappa-opioid receptor system.

Donahue RJ, Landino SM, Golden SA, Carroll FI, Russo SJ, Carlezon WA Jr.

Behav Pharmacol. 2015 Oct;26(7 Spec No):654-63. doi: 10.1097/FBP.0000000000000155.


Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302 on nicotine withdrawal in mice.

Jackson KJ, Jackson A, Carroll FI, Damaj MI.

Neuropharmacology. 2015 Oct;97:270-4. doi: 10.1016/j.neuropharm.2015.05.023. Epub 2015 Jun 1.


Combining Active Immunization with Monoclonal Antibody Therapy To Facilitate Early Initiation of a Long-Acting Anti-Methamphetamine Antibody Response.

Hambuchen MD, Carroll FI, Rüedi-Bettschen D, Hendrickson HP, Hennings LJ, Blough BE, Brieaddy LE, Pidaparthi RR, Owens SM.

J Med Chem. 2015 Jun 11;58(11):4665-77. doi: 10.1021/acs.jmedchem.5b00220. Epub 2015 May 22.


Abnormal error processing in depressive states: a translational examination in humans and rats.

Beard C, Donahue RJ, Dillon DG, Van't Veer A, Webber C, Lee J, Barrick E, Hsu KJ, Foti D, Carroll FI, Carlezon WA Jr, Björgvinsson T, Pizzagalli DA.

Transl Psychiatry. 2015 May 12;5:e564. doi: 10.1038/tp.2015.54.


In vitro and in vivo neuronal nicotinic receptor properties of (+)- and (-)-pyrido[3,4]homotropane [(+)- and (-)-PHT]: (+)-PHT is a potent and selective full agonist at α6β2 containing neuronal nicotinic acetylcholine receptors.

Carroll FI, Navarro HA, Mascarella SW, Castro AH, Luetje CW, Wageman CR, Marks MJ, Jackson A, Damaj MI.

ACS Chem Neurosci. 2015 Jun 17;6(6):920-6. doi: 10.1021/acschemneuro.5b00077. Epub 2015 Apr 30.


Effects of ketoprofen, morphine, and kappa opioids on pain-related depression of nesting in mice.

Negus SS, Neddenriep B, Altarifi AA, Carroll FI, Leitl MD, Miller LL.

Pain. 2015 Jun;156(6):1153-60. doi: 10.1097/j.pain.0000000000000171.


Examination of the metabolite hydroxybupropion in the reinforcing and aversive stimulus effects of nicotine in rats.

Malcolm E, Carroll FI, Blough B, Damaj MI, Shoaib M.

Psychopharmacology (Berl). 2015 Aug;232(15):2763-71. doi: 10.1007/s00213-015-3908-z. Epub 2015 Mar 13.


A Double-Blind, Placebo-Controlled Trial to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of JDTic.

Buda JJ, Carroll FI, Kosten TR, Swearingen D, Walters BB.

Neuropsychopharmacology. 2015 Aug;40(9):2059-65. doi: 10.1038/npp.2015.27. Epub 2015 Jan 23.


Simple radiometric method for accurately quantitating epitope densities of hapten-protein conjugates with sulfhydryl linkages.

Peterson EC, Hambuchen MD, Tawney RL, Gunnell MG, Cowell JL, Lay JO Jr, Blough BE, Carroll FI, Owens SM.

Bioconjug Chem. 2014 Dec 17;25(12):2112-5. doi: 10.1021/bc500456z. Epub 2014 Dec 4.


Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.

Kormos CM, Gichinga MG, Maitra R, Runyon SP, Thomas JB, Brieaddy LE, Mascarella SW, Navarro HA, Carroll FI.

J Med Chem. 2014 Sep 11;57(17):7367-81. doi: 10.1021/jm5008177. Epub 2014 Aug 25.


A thermostable bacterial cocaine esterase rapidly eliminates cocaine from brain in nonhuman primates.

Howell LL, Nye JA, Stehouwer JS, Voll RJ, Mun J, Narasimhan D, Nichols J, Sunahara R, Goodman MM, Carroll FI, Woods JH.

Transl Psychiatry. 2014 Jul 1;4:e407. doi: 10.1038/tp.2014.48.


The discovery and development of the N-substituted trans-3,4-dimethyl-4-(3'-hydroxyphenyl)piperidine class of pure opioid receptor antagonists.

Carroll FI, Dolle RE.

ChemMedChem. 2014 Aug;9(8):1638-54. doi: 10.1002/cmdc.201402142. Epub 2014 Jun 30. Review.


Anti-nociception mediated by a κ opioid receptor agonist is blocked by a δ receptor agonist.

Taylor AM, Roberts KW, Pradhan AA, Akbari HA, Walwyn W, Lutfy K, Carroll FI, Cahill CM, Evans CJ.

Br J Pharmacol. 2015 Jan;172(2):691-703. doi: 10.1111/bph.12810. Epub 2014 Sep 5.


Discriminative stimulus and hypothermic effects of some derivatives of the nAChR agonist epibatidine in mice.

Rodriguez JS, Cunningham CS, Moura FB, Ondachi P, Carroll FI, McMahon LR.

Psychopharmacology (Berl). 2014 Dec;231(23):4455-66. doi: 10.1007/s00213-014-3589-z. Epub 2014 May 7.


Effect of the 3- and 4-methyl groups on the opioid receptor properties of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines.

Kormos CM, Cueva JP, Gichinga MG, Runyon SP, Thomas JB, Brieaddy LE, Mascarella SW, Gilmour BP, Navarro HA, Carroll FI.

J Med Chem. 2014 Apr 10;57(7):3140-7. doi: 10.1021/jm500184j. Epub 2014 Mar 26.

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