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Chemical structure of cocaine. The biosynthesis of cocaine has long attracted the attention of biochemists and organic chemists. This interest is partly motivated by the strong physiological effects of cocaine, but a further incentive was the unusual bicyclic structure of the molecule. The biosynthesis can be viewed as occurring in two phases ...
In a Phase 2 study, TNX-1300 at 100 mg or 200 mg i.v. doses was well tolerated and interrupted cocaine effects after cocaine 50 mg i.v. challenge. [ 9 ] The enzyme is important in bioremediation , levels of cocaine in European ocean water were cited at 20 ng/L, similar levels in which swollen muscles, and in some cases broken muscle fibers of ...
Cocaine also blocks the serotonin transporter and norepinephrine transporter, inhibiting reuptake of serotonin and norepinephrine from the synaptic cleft into the pre-synaptic axon terminal and increasing activation of serotonin receptors and norepinephrine receptors in the post-synaptic neuron, contributing to the mental and physical effects ...
It is a primary metabolite of cocaine, [1] and is pharmacologically inactive. [2] It is the corresponding carboxylic acid of cocaine, its methyl ester. It is formed in the liver by the metabolism of cocaine by hydrolysis, catalysed by carboxylesterases, and subsequently excreted in the urine. It is readily synthesised by boiling cocaine ...
This effect of inducing LTP in VTA slices 24 hours after drug exposure has been shown using morphine, nicotine, ethanol, cocaine, and amphetamines. These drugs have very little in common except that they are all potentially addictive. This is evidence supporting a link between structural changes in the VTA and the development of addiction.
This receptor had been seen to modulate the rewarding effects of cocaine, and receptor antagonists had blocked the acute locomotor stimulating effect and lowered behavioral sensitization. Changes in the sigma 1 receptor have been shown to modulate dopamine release, so shifts in its expression can change the behavioral responses to cocaine with ...
The structure of cocaine with relevant structural motifs for activity at the dopamine transporter highlighted. While it was originally thought that the 2β-carbomethoxy moiety interacted with the DAT through hydrogen bonding, subsequent research has indicated that electrostatic (ionic) interactions are the primary means of interactions with the DAT.
This suggests a positive neuromodulatory action of CART on the effects of psychostimulants in rats. [18] CART is altered in the ventral tegmental area of cocaine overdose victims, and a mutation in the CART gene is associated with alcoholism. [19] By inhibiting the rewarding effects of cocaine, CART has a potential use in treating cocaine ...