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Further exploration of the structure-activity relationship of imidazoquinolines; identification of potent C7-substituted imidazoquinolines.

Hunt JR, Kleindl PA, Moulder KR, Prisinzano TE, Forrest ML.

Bioorg Med Chem Lett. 2019 Nov 9:126788. doi: 10.1016/j.bmcl.2019.126788. [Epub ahead of print]


Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine.

Kaski SW, White AN, Gross JD, Trexler KR, Wix K, Harland AA, Prisinzano TE, Aubé J, Kinsey SG, Kenakin T, Siderovski DP, Setola V.

J Pharmacol Exp Ther. 2019 Nov;371(2):487-499. doi: 10.1124/jpet.118.255661. Epub 2019 Sep 6.


Discovery of Small-Molecule Inhibitors Targeting the E3 Ubiquitin Ligase Activity of the Herpes Simplex Virus 1 ICP0 Protein Using an In Vitro High-Throughput Screening Assay.

Deschamps T, Waisner H, Dogrammatzis C, Roy A, Chacko S, Perera C, Prisinzano TE, Kalamvoki M.

J Virol. 2019 Jun 14;93(13). pii: e00619-19. doi: 10.1128/JVI.00619-19. Print 2019 Jul 1.


Impact of Pharmacological Manipulation of the κ-Opioid Receptor System on Self-grooming and Anhedonic-like Behaviors in Male Mice.

Butelman ER, McElroy BD, Prisinzano TE, Kreek MJ.

J Pharmacol Exp Ther. 2019 Jul;370(1):1-8. doi: 10.1124/jpet.119.256354. Epub 2019 Apr 11.


Stuffed Methyltransferase Catalyzes the Penultimate Step of Pyochelin Biosynthesis.

Ronnebaum TA, McFarlane JS, Prisinzano TE, Booker SJ, Lamb AL.

Biochemistry. 2019 Feb 12;58(6):665-678. doi: 10.1021/acs.biochem.8b00716. Epub 2018 Dec 27.


Kappa Opioid Receptor Agonist Mesyl Sal B Attenuates Behavioral Sensitization to Cocaine with Fewer Aversive Side-Effects than Salvinorin A in Rodents.

Kivell BM, Paton KF, Kumar N, Morani AS, Culverhouse A, Shepherd A, Welsh SA, Biggerstaff A, Crowley RS, Prisinzano TE.

Molecules. 2018 Oct 11;23(10). pii: E2602. doi: 10.3390/molecules23102602.


Assessment of rimonabant-like adverse effects of purported CB1R neutral antagonist / CB2R agonist aminoalkylindole derivatives in mice.

Tai S, Vasiljevik T, Sherwood AM, Eddington S, Wilson CD, Prisinzano TE, Fantegrossi WE.

Drug Alcohol Depend. 2018 Nov 1;192:285-293. doi: 10.1016/j.drugalcdep.2018.08.011. Epub 2018 Sep 25.


Scalable Regioselective and Stereoselective Synthesis of Functionalized (E)-4-Iodobut-3-en-1-ols: Gram-Scale Total Synthesis of Fungal Decanolides and Derivatives.

Sherwood AM, Williamson SE, Johnson SN, Yilmaz A, Day VW, Prisinzano TE.

J Org Chem. 2018 Jan 19;83(2):980-992. doi: 10.1021/acs.joc.7b02324. Epub 2018 Jan 8.


Novel psychotherapeutics - a cautiously optimistic focus on Hallucinogens.

Sherwood AM, Prisinzano TE.

Expert Rev Clin Pharmacol. 2018 Jan;11(1):1-3. doi: 10.1080/17512433.2018.1415755. Epub 2017 Dec 17. No abstract available.


Modular Approach to pseudo-Neoclerodanes as Designer κ-Opioid Ligands.

Sherwood AM, Williamson SE, Crowley RS, Abbott LM, Day VW, Prisinzano TE.

Org Lett. 2017 Oct 6;19(19):5414-5417. doi: 10.1021/acs.orglett.7b02684. Epub 2017 Sep 14.


Semisynthesis and Kappa-Opioid Receptor Activity of Derivatives of Columbin, a Furanolactone Diterpene.

Yilmaz A, Crowley RS, Sherwood AM, Prisinzano TE.

J Nat Prod. 2017 Jul 28;80(7):2094-2100. doi: 10.1021/acs.jnatprod.7b00327. Epub 2017 Jul 18.


Correction to "Structure-Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias".

Lovell KM, Frankowski KJ, Stahl EL, Slauson SR, Yoo E, Prisinzano TE, Aubé J, Bohn LM.

ACS Chem Neurosci. 2017 Jul 19;8(7):1628. doi: 10.1021/acschemneuro.7b00157. Epub 2017 May 25. No abstract available.


The C-2 derivatives of salvinorin A, ethoxymethyl ether Sal B and β-tetrahydropyran Sal B, have anti-cocaine properties with minimal side effects.

Ewald AWM, Bosch PJ, Culverhouse A, Crowley RS, Neuenswander B, Prisinzano TE, Kivell BM.

Psychopharmacology (Berl). 2017 Aug;234(16):2499-2514. doi: 10.1007/s00213-017-4637-2. Epub 2017 May 23.


Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability.

Sherwood AM, Crowley RS, Paton KF, Biggerstaff A, Neuenswander B, Day VW, Kivell BM, Prisinzano TE.

J Med Chem. 2017 May 11;60(9):3866-3878. doi: 10.1021/acs.jmedchem.7b00148. Epub 2017 Apr 19.


Synthesis and Opioid Activity of Tyr1 -ψ[(Z)CF=CH]-Gly2 and Tyr1 -ψ[(S)/(R)-CF3 CH-NH]-Gly2 Leu-enkephalin Fluorinated Peptidomimetics.

Karad SN, Pal M, Crowley RS, Prisinzano TE, Altman RA.

ChemMedChem. 2017 Apr 20;12(8):571-576. doi: 10.1002/cmdc.201700103. Epub 2017 Apr 5.


Synergistic blockade of alcohol escalation drinking in mice by a combination of novel kappa opioid receptor agonist Mesyl Salvinorin B and naltrexone.

Zhou Y, Crowley RS, Ben K, Prisinzano TE, Kreek MJ.

Brain Res. 2017 May 1;1662:75-86. doi: 10.1016/j.brainres.2017.02.027. Epub 2017 Mar 2.


The analgesic and anti-inflammatory effects of Salvinorin A analogue β-tetrahydropyran Salvinorin B in mice.

Paton KF, Kumar N, Crowley RS, Harper JL, Prisinzano TE, Kivell BM.

Eur J Pain. 2017 Jul;21(6):1039-1050. doi: 10.1002/ejp.1002. Epub 2017 Feb 3.


Synthetic Studies of Neoclerodane Diterpenes from Salvia divinorum: Identification of a Potent and Centrally Acting μ Opioid Analgesic with Reduced Abuse Liability.

Crowley RS, Riley AP, Sherwood AM, Groer CE, Shivaperumal N, Biscaia M, Paton K, Schneider S, Provasi D, Kivell BM, Filizola M, Prisinzano TE.

J Med Chem. 2016 Dec 22;59(24):11027-11038. doi: 10.1021/acs.jmedchem.6b01235. Epub 2016 Dec 13.


Holo Structure and Steady State Kinetics of the Thiazolinyl Imine Reductases for Siderophore Biosynthesis.

Meneely KM, Ronnebaum TA, Riley AP, Prisinzano TE, Lamb AL.

Biochemistry. 2016 Sep 27;55(38):5423-33. doi: 10.1021/acs.biochem.6b00735. Epub 2016 Sep 15.


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.


Role of Ventral Subiculum in Context-Induced Relapse to Alcohol Seeking after Punishment-Imposed Abstinence.

Marchant NJ, Campbell EJ, Whitaker LR, Harvey BK, Kaganovsky K, Adhikary S, Hope BT, Heins RC, Prisinzano TE, Vardy E, Bonci A, Bossert JM, Shaham Y.

J Neurosci. 2016 Mar 16;36(11):3281-94. doi: 10.1523/JNEUROSCI.4299-15.2016.


Time course of pharmacokinetic and hormonal effects of inhaled high-dose salvinorin A in humans.

Johnson MW, MacLean KA, Caspers MJ, Prisinzano TE, Griffiths RR.

J Psychopharmacol. 2016 Apr;30(4):323-9. doi: 10.1177/0269881116629125. Epub 2016 Feb 15.


Investigation of the role of βarrestin2 in kappa opioid receptor modulation in a mouse model of pruritus.

Morgenweck J, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM.

Neuropharmacology. 2015 Dec;99:600-9. doi: 10.1016/j.neuropharm.2015.08.027. Epub 2015 Aug 25.


Functional selectivity of kappa opioid receptor agonists in peripheral sensory neurons.

Jamshidi RJ, Jacobs BA, Sullivan LC, Chavera TA, Saylor RM, Prisinzano TE, Clarke WP, Berg KA.

J Pharmacol Exp Ther. 2015 Nov;355(2):174-82. doi: 10.1124/jpet.115.225896. Epub 2015 Aug 21.


Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting.

Zhou L, Stahl EL, Lovell KM, Frankowski KJ, Prisinzano TE, Aubé J, Bohn LM.

Neuropharmacology. 2015 Dec;99:131-41. doi: 10.1016/j.neuropharm.2015.07.001. Epub 2015 Jul 6.


Behavioral and Physiological Effects of a Novel Kappa-Opioid Receptor-Based DREADD in Rats.

Marchant NJ, Whitaker LR, Bossert JM, Harvey BK, Hope BT, Kaganovsky K, Adhikary S, Prisinzano TE, Vardy E, Roth BL, Shaham Y.

Neuropsychopharmacology. 2016 Jan;41(2):402-9. doi: 10.1038/npp.2015.149. Epub 2015 May 28.


Structure-activity relationship studies of functionally selective kappa opioid receptor agonists that modulate ERK 1/2 phosphorylation while preserving G protein over βarrestin2 signaling bias.

Lovell KM, Frankowski KJ, Stahl EL, Slauson SR, Yoo E, Prisinzano TE, Aubé J, Bohn LM.

ACS Chem Neurosci. 2015 Aug 19;6(8):1411-9. doi: 10.1021/acschemneuro.5b00092. Epub 2015 May 1. Erratum in: ACS Chem Neurosci. 2017 Jul 19;8(7):1628.


Azaphilones inhibit tau aggregation and dissolve tau aggregates in vitro.

Paranjape SR, Riley AP, Somoza AD, Oakley CE, Wang CC, Prisinzano TE, Oakley BR, Gamblin TC.

ACS Chem Neurosci. 2015 May 20;6(5):751-60. doi: 10.1021/acschemneuro.5b00013. Epub 2015 Apr 15.


N-acetyl-S-(N,N-diethylcarbamoyl) cysteine in rat nucleus accumbens, medial prefrontal cortex, and in rat and human plasma after disulfiram administration.

Winefield RD, Heemskerk AA, Kaul S, Williams TD, Caspers MJ, Prisinzano TE, McCance-Katz EF, Lunte CE, Faiman MD.

J Pharm Biomed Anal. 2015 Mar 25;107:518-25. doi: 10.1016/j.jpba.2015.01.036. Epub 2015 Jan 25.


Modafinil and its metabolites enhance the anticonvulsant action of classical antiepileptic drugs in the mouse maximal electroshock-induced seizure model.

Zolkowska D, Andres-Mach M, Prisinzano TE, Baumann MH, Luszczki JJ.

Psychopharmacology (Berl). 2015 Jul;232(14):2463-79. doi: 10.1007/s00213-015-3884-3. Epub 2015 Feb 21.


Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif.

Frankowski KJ, Slauson SR, Lovell KM, Phillips AM, Streicher JM, Zhou L, Whipple DA, Schoenen FJ, Prisinzano TE, Bohn LM, Aubé J.

Bioorg Med Chem. 2015 Jul 15;23(14):3948-56. doi: 10.1016/j.bmc.2014.12.033. Epub 2014 Dec 23.


Synthesis and κ-opioid receptor activity of furan-substituted salvinorin A analogues.

Riley AP, Groer CE, Young D, Ewald AW, Kivell BM, Prisinzano TE.

J Med Chem. 2014 Dec 26;57(24):10464-75. doi: 10.1021/jm501521d. Epub 2014 Dec 9.


Expanding the results of a high throughput screen against an isochorismate-pyruvate lyase to enzymes of a similar scaffold or mechanism.

Meneely KM, Luo Q, Riley AP, Taylor B, Roy A, Stein RL, Prisinzano TE, Lamb AL.

Bioorg Med Chem. 2014 Nov 1;22(21):5961-9. doi: 10.1016/j.bmc.2014.09.010. Epub 2014 Sep 16.


Salvinorin A regulates dopamine transporter function via a kappa opioid receptor and ERK1/2-dependent mechanism.

Kivell B, Uzelac Z, Sundaramurthy S, Rajamanickam J, Ewald A, Chefer V, Jaligam V, Bolan E, Simonson B, Annamalai B, Mannangatti P, Prisinzano TE, Gomes I, Devi LA, Jayanthi LD, Sitte HH, Ramamoorthy S, Shippenberg TS.

Neuropharmacology. 2014 Nov;86:228-40. doi: 10.1016/j.neuropharm.2014.07.016. Epub 2014 Aug 10.


Studies toward the Development of Antiproliferative Neoclerodanes from Salvinorin A.

Vasiljevik T, Groer CE, Lehner K, Navarro H, Prisinzano TE.

J Nat Prod. 2014 Aug 22;77(8):1817-24. doi: 10.1021/np5002048. Epub 2014 Jul 30.


Pharmacology and anti-addiction effects of the novel κ opioid receptor agonist Mesyl Sal B, a potent and long-acting analogue of salvinorin A.

Simonson B, Morani AS, Ewald AW, Walker L, Kumar N, Simpson D, Miller JH, Prisinzano TE, Kivell BM.

Br J Pharmacol. 2015 Jan;172(2):515-31. doi: 10.1111/bph.12692. Epub 2014 Jul 1.


Salvinorin A analogs and other κ-opioid receptor compounds as treatments for cocaine abuse.

Kivell BM, Ewald AW, Prisinzano TE.

Adv Pharmacol. 2014;69:481-511. doi: 10.1016/B978-0-12-420118-7.00012-3. Review.


Assessment of the kappa opioid agonist, salvinorin A, as a punisher of drug self-administration in monkeys.

Freeman KB, Naylor JE, Prisinzano TE, Woolverton WL.

Psychopharmacology (Berl). 2014 Jul;231(14):2751-8. doi: 10.1007/s00213-014-3436-2. Epub 2014 Jan 31.


LC-MS/MS quantification of salvinorin A from biological fluids.

Caspers MJ, Williams TD, Lovell KM, Lozama A, Butelman ER, Kreek MJ, Johnson M, Griffiths R, Maclean K, Prisinzano TE.

Anal Methods. 2013 Dec 21;5(24). doi: 10.1039/C3AY40810H.


Palladium-catalyzed transformations of salvinorin A, a neoclerodane diterpene from Salvia divinorum.

Riley AP, Day VW, Navarro HA, Prisinzano TE.

Org Lett. 2013 Dec 6;15(23):5936-9. doi: 10.1021/ol4027528. Epub 2013 Nov 18.


The 2-methoxy methyl analogue of salvinorin A attenuates cocaine-induced drug seeking and sucrose reinforcements in rats.

Morani AS, Ewald A, Prevatt-Smith KM, Prisinzano TE, Kivell BM.

Eur J Pharmacol. 2013 Nov 15;720(1-3):69-76. doi: 10.1016/j.ejphar.2013.10.050. Epub 2013 Nov 4.


Development of functionally selective, small molecule agonists at kappa opioid receptors.

Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl E, Schmid CL, Hodder P, Madoux F, Cameron MD, Prisinzano TE, Aubé J, Bohn LM.

J Biol Chem. 2013 Dec 20;288(51):36703-16. doi: 10.1074/jbc.M113.504381. Epub 2013 Nov 1.


A Cell Based HTS Approach for the Discovery of New Inhibitors of RSV.

Noah JW, Severson W, Chung DH, Moore B, Jia F, Xu X, Maddox C, Rasmussen L, Sosa MI, Tower NA, Ananthan S, White EL, Jonsson C, Matharu DS, Golden JE, Prisinzano TE, Aubé J.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 15 [updated 2013 Feb 28].


Modafinil alone and in combination with low dose amphetamine does not establish conditioned place preference in male Sprague-Dawley rats.

Quisenberry AJ, Prisinzano TE, Baker LE.

Exp Clin Psychopharmacol. 2013 Jun;21(3):252-8. doi: 10.1037/a0031832. Epub 2013 May 6.


Design, synthesis, and biological evaluation of aminoalkylindole derivatives as cannabinoid receptor ligands with potential for treatment of alcohol abuse.

Vasiljevik T, Franks LN, Ford BM, Douglas JT, Prather PL, Fantegrossi WE, Prisinzano TE.

J Med Chem. 2013 Jun 13;56(11):4537-50. doi: 10.1021/jm400268b. Epub 2013 May 22.


Neoclerodanes as atypical opioid receptor ligands.

Prisinzano TE.

J Med Chem. 2013 May 9;56(9):3435-43. doi: 10.1021/jm400388u. Epub 2013 Apr 18. Review.


Discovery of a novel selective kappa-opioid receptor agonist using crystal structure-based virtual screening.

Negri A, Rives ML, Caspers MJ, Prisinzano TE, Javitch JA, Filizola M.

J Chem Inf Model. 2013 Mar 25;53(3):521-6. doi: 10.1021/ci400019t. Epub 2013 Mar 13.


Special issue in honor of Lester A. Mitscher.

Timmermann BN, Prisinzano TE.

J Nat Prod. 2013 Mar 22;76(3):303-4. doi: 10.1021/np400090f. Epub 2013 Feb 7. No abstract available.


Cannabinoid agonists increase the interaction between β-Arrestin 2 and ERK1/2 and upregulate β-Arrestin 2 and 5-HT(2A) receptors.

Franklin JM, Vasiljevik T, Prisinzano TE, Carrasco GA.

Pharmacol Res. 2013 Feb;68(1):46-58. doi: 10.1016/j.phrs.2012.11.002. Epub 2012 Nov 19.


Dose-related effects of salvinorin A in humans: dissociative, hallucinogenic, and memory effects.

MacLean KA, Johnson MW, Reissig CJ, Prisinzano TE, Griffiths RR.

Psychopharmacology (Berl). 2013 Mar;226(2):381-92. doi: 10.1007/s00213-012-2912-9. Epub 2012 Nov 8.

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