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Molecules 2021 Oct 14;26(20). Epub 2021 Oct 14.

Department of Chemistry, Clemson University, Clemson, SC 29634, USA.

The Sterling Research Group identified pravadoline as an aminoalkylindole (AAI) non-steroidal anti-inflammatory pain reliever. As drug design progressed, the ability of AAI analogs to block prostaglandin synthesis diminished, and antinociceptive activity was found to result from action at the CB cannabinoid receptor, a G-protein-coupled receptor (GPCR) abundant in the brain. Several laboratories applied computational chemistry methods to ultimately conclude that AAI and cannabinoid ligands could overlap within a common binding pocket but that WIN55212-2 primarily utilized steric interactions via aromatic stacking, whereas cannabinoid ligands required some electrostatic interactions, particularly involving the CB helix-3 lysine. Read More

J Pharmacol Exp Ther 2022 01 8;380(1):1-14. Epub 2021 Oct 8.

Department of Pharmacology & Toxicology (J.C.D., R.K.M., M.I.D., J.E.S., H.I.A., L.D.O., A.H.L.), and Department of Medicinal Chemistry (A.H.L.), Virginia Commonwealth University, Richmond, Virginia; Department of Pharmaceutical Sciences, University of Connecticut, Mansfield, Connecticut (D.A.K.); and Department of Pharmaceutical Sciences, Texas A&M, College Station, Texas (Z.W., D.L.).

Opioid use disorder reflects a major public health crisis of morbidity and mortality in which opioid withdrawal often contributes to continued use. However, current medications that treat opioid withdrawal symptoms are limited by their abuse liability or lack of efficacy. Although cannabinoid 1 (CB) receptor agonists, including Δ-tetrahydrocannabinol, ameliorate opioid withdrawal in both clinical and preclinical studies of opioid dependence, this strategy elicits cannabimimetic side effects as well as tolerance and dependence after repeated administration. Read More

Sci Rep 2021 04 15;11(1):8232. Epub 2021 Apr 15.

Department of Pharmacology, College of Medicine, University of Arizona, Tucson, AZ, USA.

Limited evidence has suggested that terpenes found in Cannabis sativa are analgesic, and could produce an "entourage effect" whereby they modulate cannabinoids to result in improved outcomes. However this hypothesis is controversial, with limited evidence. We thus investigated Cannabis sativa terpenes alone and with the cannabinoid agonist WIN55,212 using in vitro and in vivo approaches. Read More

Int J Mol Sci 2020 Nov 23;21(22). Epub 2020 Nov 23.

Department of Neurochemistry, Maj Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Poland.

Cannabis has a long history of medical use. Although there are many cannabinoids present in cannabis, Δ9tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD) are the two components found in the highest concentrations. CBD itself does not produce typical behavioral cannabimimetic effects and was thought not to be responsible for psychotropic effects of cannabis. Read More

Talanta 2020 Nov 10;219:121336. Epub 2020 Jul 10.

The Laboratory of Cancer Biology and Cannabinoid Research, Department of Biology, Technion-Israel Institute of Technology, Haifa, 3200003, Israel. Electronic address:

Increasing evidence for the therapeutic potential of Cannabis in numerous pathological and physiological conditions has led to a surge of studies investigating the active compounds in different chemovars and their mechanisms of action, as well as their efficacy and safety. The biological effects of Cannabis have been attributed to phytocannabinoid modulation of the endocannabinoid system. In-vitro and in-vivo studies have shown that pure phytocannabinoids can alter the levels of endocannabinoids and other cannabimimetic lipids. Read More