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Arthur E Jacobson

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Articles 78
Citations 685
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Recent Articles
1.
Roth H, Das M, Sulima A, Luo D, Kaska S, Prisinzano T, et al.
Molecules . 2024 May; 29(9). PMID: 38731416
The synthesis of stereochemically pure oximes, amines, saturated and unsaturated cyanomethyl compounds, and methylaminomethyl compounds at the C9 position in 3-hydroxy--phenethyl-5-phenylmorphans provided μ-opioid receptor (MOR) agonists with varied efficacy and...
2.
Santos E, Akbarali H, Bow E, Chambers D, Gutman E, Jacobson A, et al.
J Pharmacol Exp Ther . 2024 Apr; 391(2):138-151. PMID: 38637015
Low-efficacy mu opioid receptor (MOR) agonists may serve as novel candidate analgesics with improved safety relative to high-efficacy opioids. This study used a recently validated assay of pain-depressed behavior in...
3.
Shafieichaharberoud F, Lang S, Whalen C, Rivera Quiles C, Purcell L, Talbot C, et al.
Bioconjug Chem . 2023 Dec; 35(2):164-173. PMID: 38113481
Opioid use disorder (OUD) has become a public health crisis, with recent significant increases in the number of deaths due to overdose. Vaccination can provide an attractive complementary strategy to...
4.
Das M, Ward G, Sulima A, Luo D, Prisinzano T, Imler G, et al.
Molecules . 2023 Dec; 28(23). PMID: 38067439
(-)-5,9-Dimethyl-6,7-benzomorphan (normetazocine) derivatives with a -OH or -F substituent in the aromatic ring of the -phenethyl moiety were synthesized and found to have subnanomolar potency at MOR, and both were...
5.
Chambers D, Sulima A, Luo D, Prisinzano T, Jacobson A, Rice K
Molecules . 2023 Jul; 28(14). PMID: 37513283
The 5-(3-hydroxy)phenylmorphan structural class of compounds are unlike the classical morphinans, 4,5-epoxymorphinans, and 6,7-benzomorphans, in that they have an equatorially oriented aromatic ring rather than the axial orientation of that...
6.
Santos E, Nassehi N, Bow E, Chambers D, Gutman E, Jacobson A, et al.
Pharmacol Res Perspect . 2023 Jun; 11(4):e01111. PMID: 37381112
Low-efficacy mu-opioid receptor (MOR) agonists represent promising therapeutics, but existing compounds (e.g., buprenorphine, nalbuphine) span a limited range of low MOR efficacies and have poor MOR selectivity. Accordingly, new and...
7.
Lutz J, Sulima A, Gutman E, Bow E, Luo D, Kaska S, et al.
Molecules . 2023 Jun; 28(12). PMID: 37375350
All possible diastereomeric C9-hydroxymethyl-, hydroxyethyl-, and hydroxypropyl-substituted 5-phenylmorphans were synthesized to explore the three-dimensional space around the C9 substituent in our search for potent MOR partial agonists. These compounds were...
8.
Li F, Kopajtic T, Katz J, Luo D, Prisinzano T, Imler G, et al.
Molecules . 2022 Dec; 27(24). PMID: 36557961
The design of enantiopure stereoisomers of N-2-phenylcyclopropylmethyl-substituted ortho-c oxide-bridged phenylmorphans, the E and Z isomers of an N-cinnamyl moiety, and N-propyl enantiomers were based on combining the most potent oxide-bridged...
9.
Chambers D, Sulima A, Luo D, Prisinzano T, Goldberg A, Xie B, et al.
Molecules . 2022 Oct; 27(19). PMID: 36234992
Four sets of diastereomeric C9-alkenyl 5-phenylmorphans, varying in the length of the C9-alkenyl chain, were designed to examine the effect of these spatially distinct ligands on opioid receptors. Functional activity...
10.
Abucayon E, Whalen C, Torres O, Duval A, Sulima A, Antoline J, et al.
ACS Omega . 2022 Aug; 7(30):26812-26823. PMID: 35936462
The quantitation of the available antibody binding-site concentration of polyclonal antibodies in serum is critical in defining the efficacy of vaccines against substances of abuse. We have conceptualized an equilibrium...