Christopher R McCurdy

Christopher R McCurdy, Ph.D., F.A.A.P.S. 

Director And Professor

Department: Medicinal Chemistry
Business Phone: (352) 294-8691
Business Email: cmccurdy@cop.ufl.edu

About Christopher R McCurdy

Christopher R. McCurdy, Ph.D., FAAPS, is a broadly trained medicinal chemist, behavioral pharmacologist and pharmacist whose research focuses on the design, synthesis and development of drugs to treat pain and drug abuse. For over 20 years, much of his research has focused on opioid, Neuropeptide FF and sigma receptor ligand/probe design, synthesis, pharmacological evaluation and development. He has been successful in discovering unique and selective tools for sigma receptors, NPFF receptors and opioid receptors. He is an internationally recognized expert on Kratom (Mitragyna speciosa), that is under investigation for opioid withdrawal syndrome. A significant portion of his career has been dedicated to the development of novel sigma receptor ligands, in collaboration with a variety of interdisciplinary groups, to generate and optimize selective ligands which could serve as critical experimental tools, and more recently, as potential medication development leads to attenuate the effects of cocaine, methamphetamine and pain. Most notably, he has developed a PET/MR imaging diagnostic agent for visualizing the origins of chronic, neuropathic pain by interacting with sigma receptors at the site of nerve damage. First-in-human studies are currently underway in a Phase 0 trial. In addition to his discovery chemistry roles, McCurdy serves as the director of the UF Translational Drug Development Core.  Dr. McCurdy previously served as President of the American Association of Pharmaceutical Scientists (AAPS) and also serves as the Co-Chair of the Special Interest Group on Drug Design and Discovery (DDD) of the International Pharmaceutical Federation (FIP).

Accomplishments

Appointed Consultant
2017-Current · US FDA Drug Safety and Risk Management (DSaRM) Advisory Committee
Elected President
2016-Current · American Association of Pharmaceutical Scientists (AAPS)
Member
2015-Current · American Foundation for Pharmaceutical Education, Board of Grants
Member
2015-Current · United States Pharmacopeial Convention, AAPS Voting Delegate
Inaugural recipient of Drug Discovery and Development Interface (DDDI) Section Service Award
2015 · The American Association of Pharmaceutical Scientists (AAPS)
Speaker
2015 · TEDxUM
Fellow
2014 · American Association of Pharmaceutical Scientists (AAPS)
Elected Member-At-Large
2013-2016 · American Association of Pharmaceutical Scientists
Faculty Achievement Award
2010 · University of Mississippi
Teacher of the Year, PY2 Class
2010 · University of Mississippi
Faculty Service Award
2009 · University of Mississippi
Dean’s Advisory Committee Distinguished Teaching Scholar
2008-2011 · University of Mississippi
Faculty Research Award
2007 · University of Mississippi
Member
2007 · Phi Kappa Phi
Teacher of the Year by the third-year pharmacy class
2006 · University of Mississippi
Elected Vice-Chair of Drug Design and Discovery (DDD) section
2005-2011 · American Association of Pharmaceutical Scientists (AAPS)
Academic Leadership Fellow
2005-2008 · American Association of Colleges of Pharmacy
Inaugural Dean’s Advisory Committee Distinguished Teaching Scholar
2005-2008 · University of Mississippi
Distinguished Alumnus of the Year, Phi Delta Chi, Alpha Upsilon Chapter
2005 · Ohio Northern University
Teacher of the Year by third-year pharmacy class
2003 · University of Mississippi
New Investigator Award
2002 · AACP
Recipient
2002 · Glaxo/Albert B. Prescott Leadership Award
Training Fellow Award
1998-2001 · University of Minnesota
Member
1998 · Sigma Xi Research Society
Member
1997 · Rho Chi Society
Pre-Doctoral Fellowship
1994-1998 · University of Georgia
Recipient
1994 · Allen and Hanburys/Glaxo Pride in Pharmacy Award
Member
1992 · Phi Lambda Sigma
Member
1992 · Mortar Board
Member
1992 · Omicron Delta Kappa
Outstanding Member of the Year Award
1992 · Phi Delta Chi
Dean’s Award
1989-1993 · Ohio Northern University

Research Profile

In 2005, McCurdy began collaborative work with Rae R. Matsumoto, Ph.D. (Dean of Touro College of Pharmacy, California) at the University of Mississippi, which led to the development of patented highly selective sigma receptor ligands. From this series of compounds emerged CM304/FTC146 that has advanced into human clinical trials in collaboration with Fredrick T. Chin, Ph.D. and Sandip Biswal, M.D. at Stanford University Medical Center. This compound is currently being investigated in human chronic pain populations to pinpoint sites of nerve damage, utilizing state-of-the-art Positron Emission Tomography and Magnetic Resonance Imaging (PET/MRI) multimodal technology. Currently, there is no diagnostic tool for Complex Regional Pain Syndrome and CM304/FTC146 shows early promise as a potential first-in-class diagnostic. Moreover, collaboration with Jay P. McLaughlin, Ph.D. (preeminence faculty) has resulted in a department of defense funded project to study this same class of compounds as potential therapeutic agents for chronic neuropathic pain.

McCurdy has also been a leader in the generation of non-peptide small molecules as pharmacological tools for the study of Neuropeptide FF receptors. This work has been funded, in collaboration with Jay P. McLaughlin, Ph.D. and Bonnie A. Avery, Ph.D. by the National Institute on Drug Abuse. In addition, this work has led to the development of potential novel pain killers with reduced tolerance and side-effect profiles.

Notably, McCurdy is recognized as one of the foremost International experts on Mitragyna speciosa (KRATOM), a tree from South East Asia that has traditionally been utilized as a means to ween opium addicts. For more than a decade, McCurdy has collaborated with Edward W. Boyer, M.D., Ph.D. (Harvard/Brigham and Women’s Hospital), Bonnie A. Avery, Ph.D., Stephen J. Cutler, Ph.D. (Dean, University of South Carolina College of Pharmacy), and Scott E. Hemby, Ph.D. (High Point University School of Pharmacy) on investigations into the therapeutic potential for kratom in opioid dependence and withdrawal.

Overall, McCurdy is the leader of a multidisciplinary drug discovery and development team, aimed at finding alternative treatments for pain and addiction. He has published more than 100 peer-reviewed papers, multiple book chapters, presented many invited talks at international meetings and educated hundreds of pharmacists and pharmaceutical scientists.

Areas of Interest
  • Anxiety
  • Drug abuse
  • Drug addiction
  • Drug development
  • Lead optimization
  • Medicinal chemistry
  • Natural products
  • Pain

Publications

2021
Activity of Mitragyna speciosa (“Kratom”) Alkaloids at Serotonin Receptors.
Journal of medicinal chemistry. 64(18):13510-13523 [DOI] 10.1021/acs.jmedchem.1c00726. [PMID] 34467758.
2021
Acute morphine blocks spinal respiratory motor plasticity via long-latency mechanisms that require toll-like receptor 4 signalling.
The Journal of physiology. 599(15):3771-3797 [DOI] 10.1113/JP281362. [PMID] 34142718.
2021
Assessing the therapeutic potential and toxicity of Mitragyna speciosa in opioid use disorder.
Expert opinion on drug metabolism & toxicology. 17(3):255-257 [DOI] 10.1080/17425255.2021.1853706. [PMID] 33213215.
2021
Characterization of a mouse neuropathic pain model caused by the highly active antiviral therapy (HAART) Stavudine.
Pharmacological reports : PR. 73(5):1457-1464 [DOI] 10.1007/s43440-021-00262-y. [PMID] 33860918.
2021
Correction to “Novel Approaches, Drug Candidates, and Targets in Pain Drug Discovery”.
Journal of medicinal chemistry. 64(15) [DOI] 10.1021/acs.jmedchem.1c01159. [PMID] 34264657.
2021
Effects of the sigma-1 receptor agonist blarcamesine in a murine model of fragile X syndrome: neurobehavioral phenotypes and receptor occupancy.
Scientific reports. 11(1) [DOI] 10.1038/s41598-021-94079-7. [PMID] 34433831.
2021
Exploring the Chemistry of Alkaloids from Malaysian Mitragyna speciosa (Kratom) and the Role of Oxindoles on Human Opioid Receptors.
Journal of natural products. 84(4):1034-1043 [DOI] 10.1021/acs.jnatprod.0c01055. [PMID] 33635670.
2021
Identification and characterization of MAM03055A: A novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity.
European journal of pharmacology. 906 [DOI] 10.1016/j.ejphar.2021.174263. [PMID] 34144027.
2021
In vitro and in vivo sigma 1 receptor imaging studies in different disease states.
RSC medicinal chemistry. 12(2):154-177 [DOI] 10.1039/d0md00186d. [PMID] 34046607.
2021
Novel Approaches, Drug Candidates, and Targets in Pain Drug Discovery.
Journal of medicinal chemistry. 64(10):6523-6548 [DOI] 10.1021/acs.jmedchem.1c00028. [PMID] 33956427.
2021
Oral Pharmacokinetics in Beagle Dogs of the Mitragynine Metabolite, 7-Hydroxymitragynine.
European journal of drug metabolism and pharmacokinetics. 46(3):459-463 [DOI] 10.1007/s13318-021-00684-2. [PMID] 33847897.
2021
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.
Journal of natural products. 84(4):1104-1112 [DOI] 10.1021/acs.jnatprod.0c01163. [PMID] 33620222.
2021
Pharmacological Comparison of Mitragynine and 7-Hydroxymitragynine: In Vitro Affinity and Efficacy for μ-Opioid Receptor and Opioid-Like Behavioral Effects in Rats.
The Journal of pharmacology and experimental therapeutics. 376(3):410-427 [DOI] 10.1124/jpet.120.000189. [PMID] 33384303.
2021
Preclinical pharmacokinetic study of speciociliatine, a kratom alkaloid, in rats using an UPLC-MS/MS method.
Journal of pharmaceutical and biomedical analysis. 194 [DOI] 10.1016/j.jpba.2020.113778. [PMID] 33277117.
2021
The use of hypercapnic conditions to assess opioid-induced respiratory depression in rats.
Journal of pharmacological and toxicological methods. 111 [DOI] 10.1016/j.vascn.2021.107101. [PMID] 34242797.
2020
Adolescent nicotine and tobacco smoke exposure enhances nicotine self-administration in female rats.
Neuropharmacology. 176 [DOI] 10.1016/j.neuropharm.2020.108243. [PMID] 32702403.
2020
Bioanalytical method development and pharmacokinetics of MCI-92, a sigma-1 receptor ligand.
Journal of pharmaceutical and biomedical analysis. 191 [DOI] 10.1016/j.jpba.2020.113610. [PMID] 32971495.
2020
Bioanalytical method development and validation of corynantheidine, a kratom alkaloid, using UPLC-MS/MS, and its application to preclinical pharmacokinetic studies.
Journal of pharmaceutical and biomedical analysis. 180 [DOI] 10.1016/j.jpba.2019.113019. [PMID] 31838282.
2020
Current and Future Potential Impact of COVID-19 on Kratom (Mitragyna speciosa Korth.) Supply and Use.
Frontiers in psychiatry. 11 [DOI] 10.3389/fpsyt.2020.574483. [PMID] 33324252.
2020
Development of Cannabinoids in Flowers of Industrial Hemp (Cannabis sativa L.): A Pilot Study.
Journal of agricultural and food chemistry. 68(22):6058-6064 [DOI] 10.1021/acs.jafc.0c01211. [PMID] 32392412.
2020
Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one (CM398), with Drug-Like Properties and Antinociceptive Effects In Vivo.
The AAPS journal. 22(5) [DOI] 10.1208/s12248-020-00472-x. [PMID] 32691179.
2020
Effects of Nutrient Fertility on Growth and Alkaloidal Content in Mitragyna speciosa (Kratom).
Frontiers in plant science. 11 [DOI] 10.3389/fpls.2020.597696. [PMID] 33408731.
2020
Evaluation of 18F-IAM6067 as a sigma-1 receptor PET tracer for neurodegeneration in vivo in rodents and in human tissue.
Theranostics. 10(18):7938-7955 [DOI] 10.7150/thno.47585. [PMID] 32724451.
2020
Evaluation of the rewarding effects of mitragynine and 7-hydroxymitragynine in an intracranial self-stimulation procedure in male and female rats.
Drug and alcohol dependence. 215 [DOI] 10.1016/j.drugalcdep.2020.108235. [PMID] 32889450.
2020
Exploration of cytochrome P450 inhibition mediated drug-drug interaction potential of kratom alkaloids.
Toxicology letters. 319:148-154 [DOI] 10.1016/j.toxlet.2019.11.005. [PMID] 31707106.
2020
Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[d]thiazol-2(3H)one σ receptor ligands.
Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents. 29(9):1697-1706 [DOI] 10.1007/s00044-020-02597-2. [PMID] 33584084.
2020
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
Journal of medicinal chemistry. 63(1):433-439 [DOI] 10.1021/acs.jmedchem.9b01465. [PMID] 31834797.
2020
Kratom (Mitragyna speciosa): worldwide issues.
Current opinion in psychiatry. 33(4):312-318 [DOI] 10.1097/YCO.0000000000000621. [PMID] 32452943.
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
Metabolism of a Kratom Alkaloid Metabolite in Human Plasma Increases Its Opioid Potency and Efficacy.
ACS pharmacology & translational science. 3(6):1063-1068 [DOI] 10.1021/acsptsci.0c00075. [PMID] 33344889.
2020
Patterns and reasons for kratom (Mitragyna speciosa) use among current and former opioid poly-drug users.
Journal of ethnopharmacology. 249 [DOI] 10.1016/j.jep.2019.112462. [PMID] 31816368.
2020
Pharmacokinetics and Safety of Mitragynine in Beagle Dogs.
Planta medica. 86(17):1278-1285 [DOI] 10.1055/a-1212-5475. [PMID] 32693425.
2020
Regulatory sampling of industrial hemp plant samples (Cannabis sativa L.) using UPLC-MS/MS method for detection and quantification of twelve cannabinoids.
Journal of cannabis research. 2(1) [DOI] 10.1186/s42238-020-00050-0. [PMID] 33526142.
2019
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity.
Nature medicine. 25(12):1938-1947 [DOI] 10.1038/s41591-019-0668-z. [PMID] 31792461.
2019
Abuse liability and therapeutic potential of the Mitragyna speciosa (kratom) alkaloids mitragynine and 7-hydroxymitragynine.
Addiction biology. 24(5):874-885 [DOI] 10.1111/adb.12639. [PMID] 29949228.
2019
Benzimidazolone-based selective σ2 receptor ligands: Synthesis and pharmacological evaluation.
European journal of medicinal chemistry. 165:250-257 [DOI] 10.1016/j.ejmech.2019.01.019. [PMID] 30685525.
2019
Bioanalytical method development and validation of MES207, a neuropeptide FF receptor antagonist, and its application in preclinical pharmacokinetics.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 1134-1135 [DOI] 10.1016/j.jchromb.2019.121875. [PMID] 31790916.
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.
2019
Comparative Pharmacokinetics of Mitragynine after Oral Administration of Mitragyna speciosa (Kratom) Leaf Extracts in Rats.
Planta medica. 85(4):340-346 [DOI] 10.1055/a-0770-3683. [PMID] 30452072.
2019
Divergent Cytotoxic and Metabolically Stimulative Functions of Sigma-2 Receptors: Structure-Activity Relationships of 6-Acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79) Derivatives.
The Journal of pharmacology and experimental therapeutics. 368(2):272-281 [DOI] 10.1124/jpet.118.253484. [PMID] 30530624.
2019
Kratom policy: The challenge of balancing therapeutic potential with public safety.
The International journal on drug policy. 70:70-77 [DOI] 10.1016/j.drugpo.2019.05.003. [PMID] 31103778.
2019
Metabolite profiling and identification of enzymes responsible for the metabolism of mitragynine, the major alkaloid of Mitragyna speciosa (kratom).
Xenobiotica; the fate of foreign compounds in biological systems. 49(11):1279-1288 [DOI] 10.1080/00498254.2018.1552819. [PMID] 30547698.
2019
Motives for using Kratom (Mitragyna speciosa Korth.) among regular users in Malaysia.
Journal of ethnopharmacology. 233:34-40 [DOI] 10.1016/j.jep.2018.12.038. [PMID] 30594604.
2019
Pharmacological characterization of mitragynine, the primary constituent in Kratom, as a potential medication for opioid use disorder
Journal of pharmacological and toxicological methods (Online). [DOI] 10.1016/j.vascn.2019.05.012. [PMID] 31963089.
2019
Simultaneous quantification of ten key Kratom alkaloids in Mitragyna speciosa leaf extracts and commercial products by ultra-performance liquid chromatography-tandem mass spectrometry.
Drug testing and analysis. 11(8):1162-1171 [DOI] 10.1002/dta.2604. [PMID] 30997725.
2019
The effects of mitragynine and morphine on schedule-controlled responding and antinociception in rats.
Psychopharmacology. 236(9):2725-2734 [DOI] 10.1007/s00213-019-05247-7. [PMID] 31098655.
2018
Structure-Based Identification of Potent Natural Product Chemotypes as Cannabinoid Receptor 1 Inverse Agonists.
Molecules (Basel, Switzerland). 23(10) [DOI] 10.3390/molecules23102630. [PMID] 30322136.
2018
Successful treatment of chronic knee pain following localization by a sigma-1 receptor radioligand and PET/MRI: a case report.
Journal of Pain Research. 11:2353-2356 [DOI] 10.2147/JPR.S167839. [PMID] 30349360.
2018
The Journey to AAPS 2020: a Reflection from Strategic Planning to PharmSci 360.
The AAPS journal. 21(1) [DOI] 10.1208/s12248-018-0273-y. [PMID] 30392015.
2017
A Role for Sigma Receptors in Stimulant Self-Administration and Addiction.
Handbook of experimental pharmacology. 244:177-218 [DOI] 10.1007/164_2016_94. [PMID] 28110353.
2017
Biodistribution and Radiation Dosimetry of 18F-FTC-146 in Humans.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 58(12):2004-2009 [DOI] 10.2967/jnumed.117.192641. [PMID] 28572487.
2017
Effects of nalfurafine on the reinforcing, thermal antinociceptive, and respiratory-depressant effects of oxycodone: modeling an abuse-deterrent opioid analgesic in rats.
Psychopharmacology. 234(17):2597-2605 [DOI] 10.1007/s00213-017-4652-3. [PMID] 28567699.
2017
Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel.
Oncotarget. 8(35):59345-59358 [DOI] 10.18632/oncotarget.19581. [PMID] 28938641.
2017
Quantification of highly selective sigma-1 receptor antagonist CM304 using liquid chromatography tandem mass spectrometry and its application to a pre-clinical pharmacokinetic study.
Drug testing and analysis. 9(8):1236-1242 [DOI] 10.1002/dta.2156. [PMID] 28039926.
2017
Radiosynthesis and First-In-Human PET/MRI Evaluation with Clinical-Grade [18F]FTC-146.
Molecular imaging and biology. 19(5):779-786 [DOI] 10.1007/s11307-017-1064-z. [PMID] 28280965.
2017
The sigma-1 receptor modulates dopamine transporter conformation and cocaine binding and may thereby potentiate cocaine self-administration in rats.
The Journal of biological chemistry. 292(27):11250-11261 [DOI] 10.1074/jbc.M116.774075. [PMID] 28495886.
2017
Visualizing Nerve Injury in a Neuropathic Pain Model with [18F]FTC-146 PET/MRI.
Theranostics. 7(11):2794-2805 [DOI] 10.7150/thno.19378. [PMID] 28824716.
2016
Blockade of Cocaine or σ Receptor Agonist Self Administration by Subtype-Selective σ Receptor Antagonists.
The Journal of pharmacology and experimental therapeutics. 358(1):109-24 [DOI] 10.1124/jpet.116.232728. [PMID] 27189970.
2016
Sigma-2 Receptors Play a Role in Cellular Metabolism: Stimulation of Glycolytic Hallmarks by CM764 in Human SK-N-SH Neuroblastoma.
The Journal of pharmacology and experimental therapeutics. 356(2):232-43 [DOI] 10.1124/jpet.115.228387. [PMID] 26574517.
2016
Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine.
Journal of medical toxicology : official journal of the American College of Medical Toxicology. 12(4):341-349 [PMID] 27752985.
View on: PubMed
2015
Characterization of CM572, a Selective Irreversible Partial Agonist of the Sigma-2 Receptor with Antitumor Activity.
The Journal of pharmacology and experimental therapeutics. 354(2):203-12 [DOI] 10.1124/jpet.115.224105. [PMID] 26034081.
2015
Design, synthesis and biological evaluation of bivalent benzoxazolone and benzothiazolone ligands as potential anti-inflammatory/analgesic agents.
Bioorganic & medicinal chemistry. 23(13):3248-59 [DOI] 10.1016/j.bmc.2015.04.057. [PMID] 25975638.
2015
Further validation to support clinical translation of [(18)F]FTC-146 for imaging sigma-1 receptors.
EJNMMI research. 5(1) [DOI] 10.1186/s13550-015-0122-2. [PMID] 26384292.
2015
In vitro opioid receptor affinity and in vivo behavioral studies of Nelumbo nucifera flower.
Journal of ethnopharmacology. 174:57-65 [DOI] 10.1016/j.jep.2015.08.006. [PMID] 26260436.
2015
The Sigma-2 Receptor and Progesterone Receptor Membrane Component 1 are Different Binding Sites Derived From Independent Genes.
EBioMedicine. 2(11):1806-13 [DOI] 10.1016/j.ebiom.2015.10.017. [PMID] 26870805.
2014
Evaluation of Phytocannabinoids from High Potency Cannabis sativa using In Vitro Bioassays to Determine Structure-Activity Relationships for Cannabinoid Receptor 1 and Cannabinoid Receptor 2.
Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents. 23(9):4295-4300 [PMID] 25419092.
View on: PubMed
2014
Evaluation of σ-1 receptor radioligand 18F-FTC-146 in rats and squirrel monkeys using PET.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 55(1):147-53 [DOI] 10.2967/jnumed.113.120261. [PMID] 24337599.
2014
Flavanones from Miconia prasina.
Phytochemistry letters. 7:130-132 [PMID] 24976876.
View on: PubMed
2014
Neuroprotective targets through which 6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a sigma receptor ligand, mitigates the effects of methamphetamine in vitro.
European journal of pharmacology. 724:193-203 [DOI] 10.1016/j.ejphar.2013.12.039. [PMID] 24380829.
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
Novel pyrazolopyrimidine derivatives targeting COXs and iNOS enzymes; design, synthesis and biological evaluation as potential anti-inflammatory agents.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 62:197-211 [DOI] 10.1016/j.ejps.2014.05.025. [PMID] 24907682.
2014
SN79, a sigma receptor antagonist, attenuates methamphetamine-induced astrogliosis through a blockade of OSMR/gp130 signaling and STAT3 phosphorylation.
Experimental neurology. 254:180-9 [DOI] 10.1016/j.expneurol.2014.01.020. [PMID] 24508558.
2013
Development and validation of a UPLC-MS/MS method for the determination of 7-hydroxymitragynine, a μ-opioid agonist, in rat plasma and its application to a pharmacokinetic study.
Biomedical chromatography : BMC. 27(12):1726-32 [DOI] 10.1002/bmc.2986. [PMID] 23893615.
2013
Heteroatom analogues of hydrocodone: synthesis and biological activity.
The Journal of organic chemistry. 78(7):2914-25 [DOI] 10.1021/jo3026753. [PMID] 23397939.
2013
Mephedrone (4-methylmethcathinone), a principal constituent of psychoactive bath salts, produces behavioral sensitization in rats.
Drug and alcohol dependence. 133(2):746-50 [DOI] 10.1016/j.drugalcdep.2013.06.014. [PMID] 23890492.
2013
Pharmacological evaluation of SN79, a sigma (σ) receptor ligand, against methamphetamine-induced neurotoxicity in vivo.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 23(8):960-71 [DOI] 10.1016/j.euroneuro.2012.08.005. [PMID] 22921523.
2013
SN79, a sigma receptor ligand, blocks methamphetamine-induced microglial activation and cytokine upregulation.
Experimental neurology. 247:134-42 [DOI] 10.1016/j.expneurol.2013.04.009. [PMID] 23631864.
2013
Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands.
Bioorganic & medicinal chemistry letters. 23(17):5011-3 [DOI] 10.1016/j.bmcl.2013.06.032. [PMID] 23867168.
2013
The evaluation of AZ66, an optimized sigma receptor antagonist, against methamphetamine-induced dopaminergic neurotoxicity and memory impairment in mice.
The international journal of neuropsychopharmacology. 16(5):1033-44 [DOI] 10.1017/S1461145712000831. [PMID] 22932447.
2013
Ultra-performance liquid chromatography tandem mass spectrometry method for the determination of AZ66, a sigma receptor ligand, in rat plasma and its application to in vivo pharmacokinetics.
Biomedical chromatography : BMC. 27(8):1034-40 [DOI] 10.1002/bmc.2901. [PMID] 23558564.
2013
σ Receptor antagonist attenuation of methamphetamine-induced neurotoxicity is correlated to body temperature modulation.
Pharmacological reports : PR. 65(2):343-9 [PMID] 23744418.
View on: PubMed
2012
A 96-well filtration method for radioligand binding analysis of σ receptor ligands.
Journal of pharmaceutical and biomedical analysis. 71:157-61 [DOI] 10.1016/j.jpba.2012.07.023. [PMID] 22910107.
2012
Antidepressive effects of the κ-opioid receptor agonist salvinorin A in a rat model of anhedonia.
Behavioural pharmacology. 23(7):710-5 [DOI] 10.1097/FBP.0b013e3283586189. [PMID] 22926298.
2012
CM156, a sigma receptor ligand, reverses cocaine-induced place conditioning and transcriptional responses in the brain.
Pharmacology, biochemistry, and behavior. 101(1):174-80 [DOI] 10.1016/j.pbb.2011.12.016. [PMID] 22234290.
2012
Determination of a highly selective mixed-affinity sigma receptor ligand, in rat plasma by ultra performance liquid chromatography mass spectrometry and its application to a pharmacokinetic study.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 891-892:1-6 [DOI] 10.1016/j.jchromb.2011.12.013. [PMID] 22406103.
2012
New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.
Journal of medicinal chemistry. 55(19):8272-8282 [DOI] 10.1021/jm300371c. [PMID] 22853801.
2012
Nonpeptide ligands of neuropeptide FF: current status and structural insights.
Future medicinal chemistry. 4(9):1085-92 [DOI] 10.4155/fmc.12.67. [PMID] 22709252.
2012
Sigma receptor antagonists attenuate acute methamphetamine-induced hyperthermia by a mechanism independent of IL-1β mRNA expression in the hypothalamus.
European journal of pharmacology. 691(1-3):103-9 [DOI] 10.1016/j.ejphar.2012.07.029. [PMID] 22820108.
2012
Synthesis and pharmacological characterization of a novel sigma receptor ligand with improved metabolic stability and antagonistic effects against methamphetamine.
The AAPS journal. 14(1):43-51 [DOI] 10.1208/s12248-011-9311-8. [PMID] 22183188.
2011
CM156, a high affinity sigma ligand, attenuates the stimulant and neurotoxic effects of methamphetamine in mice.
Neuropharmacology. 61(5-6):992-1000 [DOI] 10.1016/j.neuropharm.2011.06.028. [PMID] 21762711.
2011
Early development of sigma-receptor ligands.
Future medicinal chemistry. 3(1):79-94 [DOI] 10.4155/fmc.10.279. [PMID] 21428827.
2011
Herbal medicines for the management of opioid addiction: safe and effective alternatives to conventional pharmacotherapy?
CNS drugs. 25(12):999-1007 [DOI] 10.2165/11596830-000000000-00000. [PMID] 22133323.
2011
Mitragyna speciosa, a psychoactive tree from Southeast Asia with opioid activity.
Current topics in medicinal chemistry. 11(9):1165-75 [PMID] 21050173.
View on: PubMed
2011
N-naphthoyl-beta-naltrexamine (NNTA), a highly selective and potent activator of μ/kappa-opioid heteromers.
Proceedings of the National Academy of Sciences of the United States of America. 108(12):5098-103 [DOI] 10.1073/pnas.1016277108. [PMID] 21385944.
2011
Sigma receptor agonists: receptor binding and effects on mesolimbic dopamine neurotransmission assessed by microdialysis.
Biological psychiatry. 69(3):208-17 [DOI] 10.1016/j.biopsych.2010.07.026. [PMID] 20950794.
2011
Sigma receptors and cocaine abuse.
Current topics in medicinal chemistry. 11(9):1128-50 [PMID] 21050176.
View on: PubMed
2011
Synthesis and characterization of [³H]-SN56, a novel radioligand for the σ₁ receptor.
European journal of pharmacology. 653(1-3):1-7 [DOI] 10.1016/j.ejphar.2010.10.099. [PMID] 21130085.
2011
Synthesis and pharmacological evaluation of 6-acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a cocaine antagonist, in rodents.
The AAPS journal. 13(3):336-46 [DOI] 10.1208/s12248-011-9274-9. [PMID] 21494909.
2011
Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.
European journal of medicinal chemistry. 46(10):5154-61 [DOI] 10.1016/j.ejmech.2011.08.031. [PMID] 21899931.
2010
A novel substituted piperazine, CM156, attenuates the stimulant and toxic effects of cocaine in mice.
The Journal of pharmacology and experimental therapeutics. 333(2):491-500 [DOI] 10.1124/jpet.109.161398. [PMID] 20100904.
2010
Computational Study on the Conformations of Mitragynine and Mitragynaline.
Theochem. 945(1-3):57-63 [PMID] 21293786.
View on: PubMed
2009
(E)-Methyl 2-[(2S,3S,12bR)-3-ethyl-8-meth-oxy-1,2,3,4,6,7,12,12b-octa-hydro-indolo[2,3-a]quinolizin-2-yl]-3-methoxy-acrylate ethanol solvate.
Acta crystallographica. Section E, Structure reports online. 65(Pt 6):o1441-2 [DOI] 10.1107/S1600536809017309. [PMID] 21583280.
2009
Beta-triketone inhibitors of plant p-hydroxyphenylpyruvate dioxygenase: modeling and comparative molecular field analysis of their interactions.
Journal of agricultural and food chemistry. 57(12):5194-200 [DOI] 10.1021/jf9005593. [PMID] 19435355.
2009
Determination of mitragynine in rat plasma by LC-MS/MS: application to pharmacokinetics.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 877(24):2593-7 [DOI] 10.1016/j.jchromb.2009.06.023. [PMID] 19589735.
2009
Ligand macromolecule interactions: theoretical principles of molecular recognition.
Methods in molecular biology (Clifton, N.J.). 572:13-29 [DOI] 10.1007/978-1-60761-244-5_2. [PMID] 20694683.
2009
Phytochemical characterization of the leaves of Mitragyna speciosa grown in U.S.A.
Natural product communications. 4(7):907-10 [PMID] 19731590.
View on: PubMed
2008
Chemical function-based pharmacophore development for novel, selective kappa opioid receptor agonists.
Journal of molecular graphics & modelling. 27(2):131-9 [DOI] 10.1016/j.jmgm.2008.03.007. [PMID] 18456526.
2008
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
Journal of medicinal chemistry. 51(5):1482-6 [DOI] 10.1021/jm701357m. [PMID] 18278854.
2008
Opioid receptors and legal highs: Salvia divinorum and Kratom.
Clinical toxicology (Philadelphia, Pa.). 46(2):146-52 [DOI] 10.1080/15563650701241795. [PMID] 18259963.
2008
Self-treatment of opioid withdrawal using kratom (Mitragynia speciosa korth).
Addiction (Abingdon, England). 103(6):1048-50 [DOI] 10.1111/j.1360-0443.2008.02209.x. [PMID] 18482427.
2008
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
Journal of medicinal chemistry. 51(6):1824-30 [DOI] 10.1021/jm701040v. [PMID] 18293909.
2007
o-Naphthalenedicarboxaldehyde derivative of 7′-aminonaltrindole as a selective delta-opioid receptor affinity label.
Journal of medicinal chemistry. 50(14):3392-6 [PMID] 17555306.
View on: PubMed
2007
p-Hydroxyphenylpyruvate dioxygenase is a herbicidal target site for beta-triketones from Leptospermum scoparium.
Phytochemistry. 68(14):2004-14 [PMID] 17368492.
View on: PubMed
2007
Targeting the methyl erythritol phosphate (MEP) pathway for novel antimalarial, antibacterial and herbicidal drug discovery: inhibition of 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) enzyme.
Current pharmaceutical design. 13(11):1161-77 [PMID] 17430177.
View on: PubMed
2007
The hallucinogen derived from Salvia divinorum, salvinorin A, has kappa-opioid agonist discriminative stimulus effects in rats.
Neuropharmacology. 53(4):481-6 [PMID] 17681558.
View on: PubMed
2007
Toward Mycobacterium tuberculosis DXR inhibitor design: homology modeling and molecular dynamics simulations.
Journal of computer-aided molecular design. 21(9):511-22 [PMID] 17874041.
View on: PubMed
2006
A combined ligand-based and target-based drug design approach for G-protein coupled receptors: application to salvinorin A, a selective kappa opioid receptor agonist.
Journal of computer-aided molecular design. 20(7-8):471-93 [PMID] 17009091.
View on: PubMed
2006
A unique binding epitope for salvinorin A, a non-nitrogenous kappa opioid receptor agonist.
The FEBS journal. 273(9):1966-74 [PMID] 16640560.
View on: PubMed
2006
Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist.
Pharmacology, biochemistry, and behavior. 83(1):109-13 [PMID] 16434091.
View on: PubMed
2006
Comparative protein modeling of 1-deoxy-D-xylulose-5-phosphate reductoisomerase enzyme from Plasmodium falciparum: a potential target for antimalarial drug discovery.
Journal of chemical information and modeling. 46(3):1360-70 [PMID] 16711755.
View on: PubMed
2006
Structure-activity relationships of neuropeptide FF and related peptidic and non-peptidic derivatives.
Peptides. 27(5):990-6 [PMID] 16490282.
View on: PubMed
2005
Analgesic substances derived from natural products (natureceuticals).
Life sciences. 78(5):476-84 [PMID] 16216276.
View on: PubMed
2005
Inhibition of choline uptake by N-cyclohexylcholine, a high affinity ligand for the choline transporter at the blood-brain barrier.
Journal of drug targeting. 13(4):259-66 [PMID] 16051538.
View on: PubMed
2005
Opioid receptor function in social attachment in young domestic fowl.
Behavioural brain research. 160(2):277-85 [PMID] 15863224.
View on: PubMed
2005
Opioid receptor-like 1 (ORL1) molecular “road map” to understanding ligand interaction and selectivity.
Current topics in medicinal chemistry. 5(3):325-40 [PMID] 15857315.
View on: PubMed
2005
Solution-phase parallel synthesis of spirohydantoins.
Journal of combinatorial chemistry. 7(2):258-63 [PMID] 15762754.
View on: PubMed
2005
Specific cross-linking of Lys233 and Cys235 in the mu opioid receptor by a reporter affinity label.
Biochemistry. 44(7):2271-5 [PMID] 15709739.
View on: PubMed
2002
Naphthalene dicarboxaldehyde as an electrophilic fluorogenic moiety for affinity labeling: application to opioid receptor affinity labels with greatly improved fluorogenic properties.
Journal of medicinal chemistry. 45(14):2887-90 [PMID] 12086475.
View on: PubMed

Grants

Aug 2021 ACTIVE
Effects of cannabis on age-related cognitive decline and Alzheimers disease pathology
Role: Co-Investigator
Funding: NATL INST OF HLTH NIA
May 2021 ACTIVE
Effects of cannabis on Alzheimers disease-related pathology and cognitive decline
Role: Co-Investigator
Funding: FL DEPT OF HLTH ED ETHEL MOORE ALZHEIMER
Dec 2020 ACTIVE
Opioid use disorders: UF Pharmacy medications discovery and development
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDA
Apr 2019 ACTIVE
Kratom alkaloids: in vitro and in vivo pharmacological mechanisms
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDA
Dec 2018 – Nov 2020
Opioid use disorders: UF Pharmacy medications discovery and development
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDA
Sep 2017 – Sep 2021
Sigma Receptor Ligands as Non-Opioid Based Pain Management
Role: Principal Investigator
Funding: US ARMY MED RES ACQUISITION
May 2017 – Jun 2018
Isolation and Biological Evaluation of Opioid Receptor Modulators from Asteracea Growing in Egypt
Role: Principal Investigator
Funding: US CIVILIAN RES AND DEV FOU via US DEPT OF AG AG RES SVC
Apr 2017 – Aug 2019
Optimization of non-peptide probes for the NPFF receptor system
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDA

Education

Fellowship – Medicinal Chemistry
2001 · University of Minnesota
Ph.D. – Medicinal Chemistry
1998 · University of Georgia
B.S. – Pharmacy
1994 · Ohio Northern University

Teaching Profile

Courses Taught
2020-2021
PHA6971 Research for Master’s Thesis
2017-2021
PHA7980 Research for Doctoral Dissertation
2017-2021
PHA6935 Selected Topics in Pharmacy
2017,2020-2021
PHA6447 Drug Design
2017-2021
PHA7979 Advanced Research
2017,2020-2021
PHA6910 Supervised Research
2018-2019,2021
PHA5789C Patient Care 7
2018
CHM7979 Advanced Research
2017-2018
PHA6905C Research Procedures in Medicinal Chemistry
2017
GMS7794 Neuroscience Seminar
2020-2021
PHA5930 Sem Pharm Research
2021
PHA6894 Introduction to Graduate Studies
2021
PHA4913 Undergraduate Research in Medicinal Chemistry

Contact Details

Phones:
Business:
(352) 294-8691
Emails: