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An orally bioavailable parthenolide analog selectively eradicates acute myelogenous leukemia stem and progenitor cells.
TLDR
It is proposed that the novel compound DMAPT has the potential to target human LSCs in vivo, which has approximately 70% oral bioavailability and pharmacologic studies using both mouse xenograft models and spontaneous acute canine leukemias demonstrate in vivo bioactivity. Expand
Lobeline and nicotine evoke [3H]overflow from rat striatal slices preloaded with [3H]dopamine: differential inhibition of synaptosomal and vesicular [3H]dopamine uptake.
TLDR
The results suggest that, unlike nicotine, lobeline increases DA release by potent inhibition of DA uptake into synaptic vesicles, and a subsequent alteration in presynaptic DA storage. Expand
A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse.
TLDR
The development of lobeline and lobeline analogs with targeted selectivity at VMAT2 represents a novel class of therapeutic agents having good potential as efficacious treatments for methamphetamine abuse. Expand
The in vitro anti-tumor activity of some crude and purified components of blackseed, Nigella sativa L.
TLDR
TQ and DIM, which are cytotoxic for several types of human tumor cells, may be MDR substrates, and that radical generation may not be critical to their cytotoxicity activity. Expand
Residence times and half-lives of nicotine metabolites in rat brain after acute peripheral administration of [2'-(14)C]nicotine.
TLDR
It is likely that nornicotine will accumulate in brain on chronic nicotine administration based on the brain half-life of this metabolite, which is also a major alkaloidal component of tobacco. Expand
High performance liquid chromatographic analysis of the pharmacologically active quinones and related compounds in the oil of the black seed (Nigella sativa L.).
TLDR
This analytical method was used to quantify the above four constituents in a commercial sample of N. sativa seed oil, and provides a good quality control methodology for the pharmacologically active components in this widely used natural remedy. Expand
Lobeline Displaces [3H]Dihydrotetrabenazine Binding and Releases [3H]Dopamine from Rat Striatal Synaptic Vesicles: Comparison with d‐Amphetamine
TLDR
In contrast to d‐amphetamine, which is equipotent in inhibiting DA uptake and promoting release from the synaptic vesicles, lobeline more potently inhibits DA uptake (via an interaction with the DTBZ site on VMAT2) than it evokes DA release to redistribute presynaptic DA storage. Expand
Accumulation of nicotine and its metabolites in rat brain after intermittent or continuous peripheral administration of [2'-(14)C]nicotine.
TLDR
Nornicotine accumulation following repeated nicotine administration suggests that this metabolite plays a contributory role in the neuropharmacological effects of nicotine. Expand
Once weekly administration of nicotine produces long-lasting locomotor sensitization in rats via a nicotinic receptor-mediated mechanism
TLDR
Nicotinic receptor activation following once-weekly nicotine administration produces long-lasting behavioral sensitization, suggesting that even infrequent nicotine exposure initiates neuroadaptive processes associated with nicotine addiction. Expand
Lobeline inhibits the neurochemical and behavioral effects of amphetamine.
TLDR
The hypothesis that lobeline redistributes dopamine pools within the presynaptic terminal, reducing pools available for amphetamine-induced release is supported, and a role for lobeline as a potential pharmacotherapy for psychostimulant abuse is supported. Expand
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