Recent Publications and Patents:
Christophe Guillon, A.M. Vetrano, J. Saxena, A. Hunter, G. Verderone, T. M. Finatti, J. Wisnoski, P. W. DeMatteo, R. D. Rapp, N. D. Heindel, L. B. Joseph, D. E. Heck, J. D. Laskin, Derivatives of 1,2,4-triazolo imines acting as dual iNOS and tumor cell growth inhibitors, Bioorganic Chem.(2020), 103: 104128. Doi.org/10.1016/j.biorg.2020.104128
J. D. Laskin, D. E. Heck, C. J. Lacey, N. D. Heindel, S. C. Young , Augmenting moieties for antiinflammatory compounds: Amino acids, U. S. Patent 10,752,581 (issued August 25, 2020)
J. D. Laskin, D. E. Heck, M-T. Huang, K. Fabio, C. J. Lacey, S. C. Young, P. Mohanta, C. Guillon, N. D. Heindel, Unique Dual-Action Therapeutics, U. S. Patent 10,570,161 (issued February 25, 2020).
G. Wahler, D. E. Heck, N. D. Heindel, D. L. Laskin, J. D. Laskin, L. B. Joseph. Antioxidant/stress response in mouse epidermis following exposure to nitrogen mustard. Exp. & Mol. Pathol. (2020), 114: 104410. Doi: 10.1016/j.yexmp.2020.104410
C. D. Guillon, Y-H. Jan, D. E. Heck, T. M. Mariano, R. D. Rapp, M. Jetter, K. Kardos, M. Whittemore, E. Akyea, I. Jabin, J. D. Laskin, N. D. Heindel, Phototoxicity of 7-oxycoumarins with keratinocytes in culture. Bioorg. Chem. (2019), 89: 103014. Doi: 10.1016/j.bioorg.2019.103014
C. D. Guillon, Y-H. Jan, N. Foster, J. Ressner, D. E. Heck, J. D. Laskin, N. D. Heindel, Synthetically modified methoxsalen for enhanced cytotoxicity in light and dark reactions. Bioorg. & Med. Chem. Let. (2019), 29(4): 619-22. Doi: 10.1016/j.bmcl.2018.12.048
C. D. Guillon, Y-H. Jan, N. Foster, M. Choudhuri, J. Saxena, T. M. Mariano, D. E. Heck, J. D. Laskin, N. D. Heindel. Synthesis and evaluation of water-soluble dimethylaminoethyl ethers of methoxsalen for proliferative skin disorders. Het. Let. (2018), 8(4): 729-36.
J. D. Laskin, Y.H. Jan, M.Jetter, C. D. Guillon, T.M. Mariano, D. E. Heck, N. D Heindel, Identification of a pyranocoumarin photosensitizer that is a potent inhibitor of keratinocyte growth, Photochem. Photobiol. (2018), Jan 6. Doi: 10.1111/php. 1282 [Epub ahead of print] PMID: 29315592.
N. D. Heindel, J. L. Sturchio, J. J. Bohning, “The Professionalization of American Chemistry: How the German Ph.D. Model Crossed the Atlantic,” Chapter 14 in Igniting the Chemical Ring of Fire, S. C. Rasmussen, editor, World Scientific Publishers, London, (2018), pp. 387-426.
L. B. Joseph, G. M. Composto, R. M. Perez, H-D. Kim, R. P. Casillas, N. D. Heindel, S. C. Young, C. J. Lacey, J. Saxena, C. D. Guillon, C. R. Croutch, J. D. Laskin, D. E. Heck. Sulfur mustard induced mast cell degranulation in mouse skin is inhibited by a novel anti-inflammatory and anticholinergic bifunctional prodrug. Toxicol. Let. (2018), 293: 77-81.
Doi: 10.1016/j.toxlet.2017.11.005
C. J. Lacey, I. Wohlman, C. Guillon, J. Saxena, N. D. Heindel et al., Multi-inhibitor prodrug constructs for simultaneous delivery of anti-inflammatory agents to mustard-induced skin injury.
Ann. N Y Acad. Sci. (2016), 1378(1):174-9.
G. M. Composto, J. D. Laskin, D. L. Laskin, D. R. Gerecke, R. P Casillas, N. D. Heindel, et al., Mitigation of nitrogen mustard mediated skin injury by a novel indomethacin bifunctional prodrug. Exp. & Mol. Pathol. (2016), 100(3):522-31.
I. M. Wohlman, G. M. Composto, D. E. Heck, N. D. Heindel et al., Mustard vesicants alter ex-pression of the endocannabinoid system in mouse skin. Toxicol. Appl. Pharmacol. (2016), 303:30-44.
A. DeSantis-Rodrigues, Y. C. Chang, R. A. Hahn, I. P. Po, P. Zhou, N. D. Heindel et al., ADAM17 Inhibitors Attenuate Corneal Epithelial Detachment Induced by Mustard Exposure. Invest. Ophthalmol. Vis. Sci. (2016), 57(4): 1687-98.
J. T. Szilagyi, V. Mishin, D. E. Heck, Y.H. Jan, L. M. Aleksunes, N. D. Heindel, et al.,
Selective Targeting of Heme Protein in Cytochrome P450 and Nitric Oxide Synthase by Diphenyleneiodonium. Toxicol. Sci. (2016), 151(1): 150-9.
S. Yang, Y-H. Jan, V. Mishin, J. R. Richardson, M. H. Hossain, N. D. Heindel, D. E. Heck, D. L. Laskin, J. D. Laskin, Sulfa drugs inhibit sepiapterin reduction and chemical redox cycling by sepiapterin reductase. J. of Pharmacol. and Exper’l. Therapeutics (2015), 352(3): 529-40.
J. Saxena, D. Meloni, M-T. Huang, D. E. Heck, J. D. Laskin, N.D. Heindel, S.C. Young, Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents. Bioorg. & Med. Chem. Lett. (2015), 25(23): 5609-12.
Y-C. Chang, J. D. Wang, R. A. Hahn, M. K. Gordon L. B. Joseph, D. E. Heck, N. D. Heindel, S. C. Young, et al., Therapeutic potential of a non-steroidal bifunctional anti-inflammatory and anti-cholinergic agent against skin injury induced by sulfur mustard. Toxicology and Applied Pharmacology (2014), 280(2): 236-44.
C. D. Guillon, D. Wisnoski, J. Saxena, N. D. Heindel et al., Nω-nitro-Nω'-substituted guanidines: a simple class of Nitric Oxide Synthase inhibitors, Modern Res. in Inflammation (2014), 3(2): 48-58.
Fabio KM, Guillon CD, Lu S-F, Heindel ND, Brownstein MJ, Lacey CJ, Garippa C, Simon NG. Pharmacokinetics and metabolism of SRX246:A potent and selective vasopressin 1a antagonist. J Pharm Sci. 2013, 102: 2033-2043.
Laskin JD, Heck DE, Lacey CJ, Aponte E, Huang M-T, Heindel ND, Pharmacologically-active vanilloid carbamates, U.S.Patent 8,343,971, issued 31 December 2012
Haddad GL, Young SC, Heindel ND, Bornhop DJ, Flowers RA 2nd, Back-scattering interferometry:an ultrasensitive method for the unperturbed detection of acetylcholinesterase-inhibitor interactions, Angew Chem Int Ed Engl. 2012 Oct 29;51(44):11126-30
Heindel ND and Rapp RD, The Nineteenth-Century Horse Doctor: A Pennsylvania Dutchman’s Practical Guide to Treating Horses, Coffeetown Press, Seattle, WA, 2012, ISBN 978-1-60381-121-7
Fabio K, Guillon C, Lacey CJ, Lu S-F, Heindel ND, Ferris C F, Placzek M, Jones G, Brownstein MJ, Simon NG. Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging. Bioorg & Med Chem, 2012, 20: 1337-1345. Doi:10.1016/j.bmc/2011.12.013.
Laskin JD, Fabio K, Lacey CJ, Young S, Mohanta P, Guillon CD, Heindel ND, Huang M-T, Heck DE, Unique Dual-Action Therapeutics, U. S. Patent Pending, PCT/US2009/005961, Pub. No. US2012/0010168 A1, published January 12, 2012.
Young, SC, Fabio KM, Huang M-T, Saxena J, Harman M P, Guillon CD, Vetrano AM, Heck DE. Flowers RA II, Heindel ND and Laskin JD (2012), Investigation of anticholinergic and non-steroidal anti-inflammatory prodrugs which reduce chemically induced skin inflammation. Journal of Applied Toxicology, 2012, 32: 135-141. doi: 10.1002/jat.1645
Laskin JD, Heck DE, Heindel ND, Dimethyl amino ethyl ether psoralens and methods for their production and use. Issued 6 December 2011, U.S. Patent 8,071,642 (2011)
Young SC, Fabio KM, Guillon C, Mohanta P, Halton TA, Heck DE, Flowers RA, Laskin JD, Heindel ND, Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction, Biorg and Med Chem Lett. 2010, 20:2987-2990. PMID: 20347302 doi:10.1016/j.bmcl.2010.02.102
Shakarjian MP, Heck DE, Gray JP, Sinko PJ, Gordon MK, Casillas RP, Heindel ND, Gerecke DR, Laskin DL, Laskin JD. Mechanisms mediating the vesicant actions of sulfur mustard after cutaneous exposure. Toxicol Sci. 2010, 114(1):5-19. PMID: 19833738
Gordon MK, DeSantis A, Deshmukh M, Lacey CJ, Hahn RA, Beloni J, Anumolu SS, Schlager JJ, Gallo MA, Gerecke DR, Heindel ND, Svoboda KKH, Babin MC and Sinko PJ, Doxycycline Hydrogels as a Potential Therapy for Ocular Vesicant Injury, Journal of Ocular Pharmacology and Therapeutics, 2010, 5: 407-419.
Fabio K, Guillon CD, Lu S-F, Heindel ND, Miller MJ, Ferris CF, Brownstein MJ, Garripa C, Steiner M, Coccaro E, Damiano E, Koppel GA, Simon NG, Vasopressin Antagonists as Anxiolytics and Antidepressants: Recent Developments. Frontiers in CNS Drug Discovery, 2010, 1, 156-183.
Laskin JD, Heck DE, Huang M-T, Fabio K, Lacey CJ, Young S, Mohanta P, Guillon CD, Heindel ND, Preparation of phenyl carbonate derivatives as reversible inhibitors of acetylcholinesterase, PTC Int, Appl. (2010) WO Patent No. 2010051044 A1 20100506. Accession Number 2010:563796; CAN 152:501184
Laskin JD, Black AT, Jan YH, Sinko PJ, Heindel ND, Sunil V, Heck DE, Laskin DL. Oxidants and antioxidants in sulfur mustard-induced injury. Ann N Y Acad Sci., 2010, 1203:92-100. PMID: 20716289
Jeffrey D. Laskin, Diane E. Heck, C. Jeffrey Lacey, Erik Aponte, Mou-Tuan Huang, and Ned D. Heindel, Vanilloid Carbamates of Pharmacological Utility as Inhibitors of Fatty Acid Amide Hydrolase, Modulators of TRPV1, and Suppressors of Inflammation, Patent Pending, #RWJ 09-52, September 14, 2009.
Laskin JD, Heindel N, Heck D, Vetrano AM, Guillon C, DeMatteo P, Fluorescent Fused-Ring Triazoles that Inhibit Cell Proliferation and Uses Thereof, U.S.Patent 7,598,238 (2009)
M. P. Shakarjian, D. E. Heck, J. Gray, P. J. Sinko, M. K. Gordon, R.P. Casillas, N. D. Heindel, D. R. Gerecke, D.L. Laskin, and J. D. Laskin, Mechanisms mediating the vesicant actions of sulfur mustard after cutaneous exposure, Tox. Sci. Advanced Access, 108: 15 October 2009, pp 1-43.
C. Guillon, G. Koppel, N. Heindel /et al/. “Azetidinones as vasopressin V1a antagonists,” Bioorg. & Med. Chem., *15* (2007) 2054-2080.
C. F. Ferris, S-f Lu, T. Messenger, C. D. Guillon, N. Heindel, M. Miller, G. Koeppel, F. R. Bruns, and N. G. Simon, “Orally active vasopressin V1a receptor antagonist, SRX251, selectively blocks aggressive behavior,” Pharmacology, Biochemistry and Behavior, *83* 2006 169-174.
J. D. Laskin, C. Martey, N. D. Heindel, M. Whittemore, and D. Heck, * “*Fluorescent Tags for Amino Acid and Nucleic Acid Analysis*,”* U.S. Patent 7,150,967 (2006)
J. D. Laskin, D. Heck, N. D. Heindel, A. M. Vetrano, C. Guillon, P. DeMatteo, “Fluorescent Fused-Ring Triazoles that Inhibit Cell Proliferation,” U.S. Patent 7,105,511 (2006)
R. F. Bruns, C. Guillon, N. D. Heindel, G. A. Koppel, M. Miller, Beta-Lactamyl Vasopressin Antagonists,” U.S.Patent 7,119,083 (2006).
N. D. Heindel, Tina Masciangioli, and Eva von Schaper, eds., “Are Chemistry Journals too Expensive and Inaccessible?,” National Academies Press, ISBN 0-309-09590-5, Washington, DC, 2005.