Search

This reflexive analysis explores feelings evoked at a participatory video screening intended to provoke policy dialogue around the health and wellbeing of Indigenous youth. The Taking Action! Proje...

α-PVP (α-pyrrolidinovalerophenone) and MDPV (3,4-methylenedioxypyrovalerone) are potent abused stimulants that are members of the synthetic cathinone class of drugs. Although these drugs are taken with recreational intent, high doses can lead to unintended adverse effects including agitation, cardiovascular effects, sympathomimetic syndromes, hallucinations, and psychoses. One possible treatment is the use of a vaccine to block or attenuate adverse medical effects. These studies report the preparation of a vaccine that generates high affinity antibodies specific for both drugs and the pharmacological testing of this vaccine in male rats. Alkylation of a hydroxy-α-PVP analog with an appropriate thiol-bearing linker afforded the hapten. When hapten-conjugated carrier protein was mixed with adjuvant, the resulting vaccine stimulated production of antibodies in male Sprague Dawley rats that were found to significantly reduce α-PVP- and MDPV-induced hyperlocomotion as well as to significantly reduce the concentrations of MDPV drugs in critical organs. The novel vaccine produced high affinity antibodies against MDPV, (R)-MDPV, (S)-MDPV, and α-PVP. Cross-reactivity testing against nine structurally similar cathinones showed very limited binding, and no binding to off-target endogenous and exogenous compounds. Antibodies generated by this bi-specific vaccine also significantly shortened the duration of locomotor activity induced by both drugs up to a dose of 5.6 mg/kg in male rats.

High specific activity (+)-amphetamine and (+)-methamphetamine were prepared by reductive dechlorination of (S)-(3′,5′-dichlorophenyl)-2-propylazide and (S)-2′6′-dichloromethamphetamine, respectively. While the latter was readily obtained by resolution of racemic 2′6′-dichloromethamphetamine using (+)-dibenzoyltartaric acid, the analogous amphetamine resisted all efforts to resolve it. Hence, the required chiral precursor was prepared by stereospecific total synthesis following methodology that had been previously developed in our Laboratories. The tritium labeled compounds had specific activity 30.1 Ci/mmol and 38.3 Ci/mmol, respectively. Copyright © 2009 John Wiley & Sons, Ltd.

Catalytic hydrogenation of 1-aminocyclopropenecarboxylic acid under tritium gas afforded [2,3-3H]1-aminocyclopropanecarboxylic acid with specific activity 26 Ci/mmol, determined by a combination of 1H and 3H NMR. Pilot radioligand binding assays indicate this compound will be a useful probe for the NMDA receptor-associated strychnine-insensitive glycine receptor.

The preparation of the δ 1 -specific ligand 7-benzylidenenaltrexone (BNTX), labeled with tritium at high specific activity (14.4 Ci/mmol) was prepared in 33% yield and >98% purity by the aldol condensation of high specific activity [15,16- 3 H]naltrexone with benzaldehyde at high dilution.