Shainnel O Eans

Shainnel O Eans,

Biological Scientist III

Department: Pharmacodynamics
Business Email: shaieans@ufl.edu

Publications

2024
A µ-opioid receptor modulator that works cooperatively with naloxone.
Nature. 631(8021):686-693 [DOI] 10.1038/s41586-024-07587-7. [PMID] 38961287.
2024
Signaling Modulation Mediated by Ligand Water Interactions with the Sodium Site at μOR.
ACS central science. 10(8):1490-1503 [DOI] 10.1021/acscentsci.4c00525. [PMID] 39220695.
2024
SRI-30827, a novel allosteric modulator of the dopamine transporter, alleviates HIV-1 Tat-induced potentiation of cocaine conditioned place preference in mice.
NeuroImmune pharmacology and therapeutics. 3(1):1-6 [DOI] 10.1515/nipt-2023-0022. [PMID] 38711842.
2024
Structure-Guided Design of Partial Agonists at an Opioid Receptor.
Research square. [DOI] 10.21203/rs.3.rs-4664764/v1. [PMID] 39070616.
2023
Identification and Pharmacological Characterization of a Low-Liability Antinociceptive Bifunctional MOR/DOR Cyclic Peptide.
Molecules (Basel, Switzerland). 28(22) [DOI] 10.3390/molecules28227548. [PMID] 38005269.
2023
Solid-Phase Synthesis of the Bicyclic Peptide OL-CTOP Containing Two Disulfide Bridges, and an Assessment of Its In Vivo μ-Opioid Receptor Antagonism after Nasal Administration.
Molecules (Basel, Switzerland). 28(4) [DOI] 10.3390/molecules28041822. [PMID] 36838810.
2023
Structure-based design of bitopic ligands for the µ-opioid receptor.
Nature. 613(7945):767-774 [DOI] 10.1038/s41586-022-05588-y. [PMID] 36450356.
2023
Tryptophan Substitution in CJ-15,208 (cyclo[Phe-D-Pro-Phe-Trp]) Introduces δ-Opioid Receptor Antagonism, Preventing Antinociceptive Tolerance and Stress-Induced Reinstatement of Extinguished Cocaine-Conditioned Place Preference.
Pharmaceuticals (Basel, Switzerland). 16(9) [DOI] 10.3390/ph16091218. [PMID] 37765026.
2022
An analog of [d-Trp]CJ-15,208 exhibits kappa opioid receptor antagonism following oral administration and prevents stress-induced reinstatement of extinguished morphine conditioned place preference.
Pharmacology, biochemistry, and behavior. 217 [DOI] 10.1016/j.pbb.2022.173405. [PMID] 35584724.
2022
Bis-Cyclic Guanidine Heterocyclic Peptidomimetics as Opioid Ligands with Mixed μ-, κ- and δ-Opioid Receptor Interactions: A Potential Approach to Novel Analgesics.
International journal of molecular sciences. 23(17) [DOI] 10.3390/ijms23179623. [PMID] 36077029.
2022
Characterization of CM-398, a Novel Selective Sigma-2 Receptor Ligand, as a Potential Therapeutic for Neuropathic Pain.
Molecules (Basel, Switzerland). 27(11) [DOI] 10.3390/molecules27113617. [PMID] 35684553.
2022
Examination of the Novel Sigma-1 Receptor Antagonist, SI 1/28, for Antinociceptive and Anti-allodynic Efficacy against Multiple Types of Nociception with Fewer Liabilities of Use.
International journal of molecular sciences. 23(2) [DOI] 10.3390/ijms23020615. [PMID] 35054797.
2022
Expression of Human Immunodeficiency Virus Transactivator of Transcription (HIV-Tat1-86) Protein Alters Nociceptive Processing that is Sensitive to Anti-Oxidant and Anti-Inflammatory Interventions.
Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology. 17(1-2):152-164 [DOI] 10.1007/s11481-021-09985-4. [PMID] 33619645.
2022
SRI-32743, a novel allosteric modulator, attenuates HIV-1 Tat protein-induced inhibition of the dopamine transporter and alleviates the potentiation of cocaine reward in HIV-1 Tat transgenic mice.
Neuropharmacology. 220 [DOI] 10.1016/j.neuropharm.2022.109239. [PMID] 36126727.
2021
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.
Journal of medicinal chemistry. 64(18):13873-13892 [DOI] 10.1021/acs.jmedchem.1c01273. [PMID] 34505767.
2021
Binge ethanol consumption-associated behavioral impairments in male mice using a gelatin-based drinking-in-the dark model.
Alcohol (Fayetteville, N.Y.). 95:25-36 [DOI] 10.1016/j.alcohol.2021.05.001. [PMID] 34029701.
2021
Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site.
eLife. 10 [DOI] 10.7554/eLife.56519. [PMID] 33555255.
2021
Kratom Alkaloids as Probes for Opioid Receptor Function: Pharmacological Characterization of Minor Indole and Oxindole Alkaloids from Kratom.
ACS chemical neuroscience. 12(14):2661-2678 [DOI] 10.1021/acschemneuro.1c00149. [PMID] 34213886.
2021
Kratom Alkaloids, Natural and Semi-Synthetic, Show Less Physical Dependence and Ameliorate Opioid Withdrawal.
Cellular and molecular neurobiology. 41(5):1131-1143 [DOI] 10.1007/s10571-020-01034-7. [PMID] 33433723.
2021
Oxidative Metabolism as a Modulator of Kratom’s Biological Actions.
Journal of medicinal chemistry. 64(22):16553-16572 [DOI] 10.1021/acs.jmedchem.1c01111. [PMID] 34783240.
2021
Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects.
Proceedings of the National Academy of Sciences of the United States of America. 118(16) [DOI] 10.1073/pnas.2000017118. [PMID] 33846240.
2020
Design, Synthesis, and Characterization of the Macrocyclic Tetrapeptide cyclo[Pro-Sar-Phe-d-Phe]: A Mixed Opioid Receptor Agonist-Antagonist Following Oral Administration.
ACS chemical neuroscience. 11(9):1324-1336 [DOI] 10.1021/acschemneuro.0c00086. [PMID] 32251585.
2020
Lyophilized Kratom Tea as a Therapeutic Option for Opioid Dependence.
Drug and alcohol dependence. 216 [DOI] 10.1016/j.drugalcdep.2020.108310. [PMID] 33017752.
2020
Multifunctional opioid receptor agonism and antagonism by a novel macrocyclic tetrapeptide prevents reinstatement of morphine-seeking behaviour.
British journal of pharmacology. 177(18):4209-4222 [DOI] 10.1111/bph.15165. [PMID] 32562259.
2020
Phenylalanine Stereoisomers of CJ-15,208 and [d-Trp]CJ-15,208 Exhibit Distinctly Different Opioid Activity Profiles.
Molecules (Basel, Switzerland). 25(17) [DOI] 10.3390/molecules25173999. [PMID] 32887303.
2020
Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine’s Biological Activity.
Journal of medicinal chemistry. 63(10):5119-5138 [DOI] 10.1021/acs.jmedchem.9b01924. [PMID] 31913038.
2019
Antinociceptive activity of thiazole-containing cyclized DAMGO and Leu-(Met) enkephalin analogs.
Organic & biomolecular chemistry. 17(21):5305-5315 [DOI] 10.1039/c9ob00882a. [PMID] 31094391.
2019
Characterization of Sigma 1 Receptor Antagonist CM-304 and Its Analog, AZ-66: Novel Therapeutics Against Allodynia and Induced Pain.
Frontiers in pharmacology. 10 [DOI] 10.3389/fphar.2019.00678. [PMID] 31258480.
2018
A stable isotope dilution tandem mass spectrometry method of major kavalactones and its applications.
PloS one. 13(5) [DOI] 10.1371/journal.pone.0197940. [PMID] 29795658.
2017
A one-pot multicomponent approach to a new series of morphine derivatives and their biological evaluation.
Organic & biomolecular chemistry. 15(37):7796-7801 [DOI] 10.1039/c7ob01924f. [PMID] 28875208.
2017
Conditional Human Immunodeficiency Virus Transactivator of Transcription Protein Expression Induces Depression-like Effects and Oxidative Stress.
Biological psychiatry. Cognitive neuroscience and neuroimaging. 2(7):599-609 [DOI] 10.1016/j.bpsc.2017.04.002. [PMID] 29057370.
2017
Selective κ receptor partial agonist HS666 produces potent antinociception without inducing aversion after i.c.v. administration in mice.
British journal of pharmacology. 174(15):2444-2456 [DOI] 10.1111/bph.13854. [PMID] 28494108.
2016
Direct Phenotypic Screening in Mice: Identification of Individual, Novel Antinociceptive Compounds from a Library of 734,821 Pyrrolidine Bis-piperazines.
ACS combinatorial science. 18(1):51-64 [DOI] 10.1021/acscombsci.5b00126. [PMID] 26651386.
2016
Mitragynine/Corynantheidine Pseudoindoxyls As Opioid Analgesics with Mu Agonism and Delta Antagonism, Which Do Not Recruit β-Arrestin-2.
Journal of medicinal chemistry. 59(18):8381-97 [DOI] 10.1021/acs.jmedchem.6b00748. [PMID] 27556704.
2015
Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors.
Journal of medicinal chemistry. 58(12):4905-17 [DOI] 10.1021/jm501637c. [PMID] 25996309.
2015
Synthesis and characterization of a dual kappa-delta opioid receptor agonist analgesic blocking cocaine reward behavior.
ACS chemical neuroscience. 6(11):1813-24 [DOI] 10.1021/acschemneuro.5b00153. [PMID] 26325040.
2014
HIV-1 Tat protein exposure potentiates ethanol reward and reinstates extinguished ethanol-conditioned place preference.
Current HIV research. 12(6):415-23 [PMID] 25760047.
2014
Nonpeptide small molecule agonist and antagonist original leads for neuropeptide FF1 and FF2 receptors.
Journal of medicinal chemistry. 57(21):8903-27 [DOI] 10.1021/jm500989n. [PMID] 25268943.
2014
Stress-induced increases in depression-like and cocaine place-conditioned behaviors are reversed by disruption of memories during reconsolidation.
Behavioural pharmacology. 25(5-6):599-608 [DOI] 10.1097/FBP.0000000000000074. [PMID] 25083575.
2013
Central administration of angiotensin IV rapidly enhances novel object recognition among mice.
Neuropharmacology. 70:247-53 [DOI] 10.1016/j.neuropharm.2013.01.025. [PMID] 23416700.
2013
Discovery of novel antinociceptive α-conotoxin analogues from the direct in vivo screening of a synthetic mixture-based combinatorial library.
ACS combinatorial science. 15(3):153-61 [DOI] 10.1021/co300152x. [PMID] 23414173.
2013
The macrocyclic peptide natural product CJ-15,208 is orally active and prevents reinstatement of extinguished cocaine-seeking behavior.
Journal of natural products. 76(3):433-8 [DOI] 10.1021/np300697k. [PMID] 23327691.
2012
Peptides derived from the prohormone proNPQ/spexin are potent central modulators of cardiovascular and renal function and nociception.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 26(2):947-54 [DOI] 10.1096/fj.11-192831. [PMID] 22038051.
2011
Unexpected opioid activity profiles of analogues of the novel peptide kappa opioid receptor ligand CJ-15,208.
ChemMedChem. 6(9):1739-45 [DOI] 10.1002/cmdc.201100113. [PMID] 21761566.
2009
Isolation and spatial expression analysis of a partial esterase gene of Culex nigripalpus (Diptera: Culicidae).
Journal of medical entomology. 46(6):1370-5 [PMID] 19960682.

Contact Details

Emails:
Business:
shaieans@ufl.edu
Addresses:
Business Mailing:
PO Box 100487
GAINESVILLE FL 32610
Business Street:
1345 CENTER DR RM P2 08
GAINESVILLE FL 32610