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Motor, Visual and Emotional Deficits in Mice after Closed-Head Mild Traumatic Brain Injury Are Alleviated by the Novel CB2 Inverse Agonist SMM-189
TLDR
Treatment with the CB2 inverse agonist SMM-189 after a mild TBI event can reduce its adverse consequences by beneficially modulating microglial activation, and recommend further evaluation of CB2 inverted agonists as a novel therapeutic approach for treating Mild TBI. Expand
Physiological and pharmacokinetic effects of oral 1,3-dimethylamylamine administration in men
TLDR
Findings indicate a consistent pattern of increase across subjects with regards to peak DMAA concentration, with peak values approximately 15–30 times lower than those reported in case studies linking DMAA intake with adverse events. Expand
Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist
TLDR
It is determined that SMM‐189 possesses acceptable biopharmaceutical properties indicating that the triaryl class of CB2 inverse agonists are viable compounds for continued preclinical development for the treatment of neurodegenerative disorders and traumatic brain injury. Expand
Anti-inflammatory activity of cannabinoid receptor 2 ligands in primary hPDL fibroblasts.
TLDR
The effective inhibition of LPS, TNF-α, IL-1β stimulated IL-6 and MCP-1 production by CB2R ligands in hPDLFs suggests that targeting the endocannabinoid system may lead to development of novel drugs for periodontal therapy, aiding strategies to improve oral health. Expand
Synthesis and biological evaluation of (3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-aryl/alkyl-methanone selective CB2 inverse agonist.
TLDR
In process of designing new cannabinoid ligands, it is discovered that the 2,6-dihydroxy-biphenyl-aryl methanone scaffold imparts inverse agonist activity atCB2 receptor without functional activity at CB1. Expand
Cannabinoid receptor 1 ligands revisited: Pharmacological assessment in the ACTOne system.
TLDR
The first detailed evaluation of the ACTOne assay for the pharmacological evaluation of CB1 ligands is reported, revealing some interesting deviations from previously reported functional activities of the aforementioned ligands. Expand
A sensitive and fast LC-MS/MS method for determination of β-receptor agonist JP-49b: application to a pharmacokinetic study in rats.
TLDR
High local drug concentrations coupled with minimal systemic exposure following ocular administration supports further testing of JP-49b as a localized therapy for diabetic retinopathy. Expand
Preclinical pharmacokinetics of the radiomitigator KZ-41 in rats
TLDR
KZ- 41 represents an excellent candidate for further development as an orally available agent for the mitigation of radiation injury and is consistent with the findings that KZ-41 is resistant to presystemic elimination mechanisms. Expand
Optimization of cAMP fluorescence dataset from ACTOne cannabinoid receptor 1 cell line
TLDR
The ACTOne CB1 cell line was evaluated for cAMP driven fluorescence by optimizing experimental conditions for sensitivity to forskolin and CP 55,940, reading time point, reliability of cell passage number, and pertussis inactivation of Gi/o. Expand
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