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Cocaine is a non-selective, competitive inhibitor of monoamine transporters, sharing a similar mechanism with that of methylphenidate. Cocaine interacts with DAT, SERT, and NET, although the behavioral and reinforcing effects of cocaine depend on its inhibition of DAT and the increase in extracellular dopamine. [1]
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 ...
CART is released in response to repeated dopamine release in the nucleus accumbens, and may regulate the activity of neurons in this area. [9] CART production is upregulated by CREB, [10] a protein thought to be involved with the development of drug addiction, and CART may be an important therapeutic target in the treatment of stimulant abuse.
Unlike the VTA, a single dose of cocaine induces no change in potentiation in the excitatory synapses of the NAc. [45] LTD was observed in the medium spiny neurons in the NAc following two different protocols: a daily cocaine administration for five days [9] or a single dose followed by 10–14 days of withdrawal. [10]
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 ...
Amphetamine, for example, is an indirect agonist of postsynaptic dopamine, norepinephrine, and serotonin receptors in each their respective neurons; [45] [46] it produces both neurotransmitter release into the presynaptic neuron and subsequently the synaptic cleft and prevents their reuptake from the synaptic cleft by activating TAAR1, a ...
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 ...
6531 13162 Ensembl ENSG00000142319 ENSG00000276996 ENSMUSG00000021609 UniProt Q01959 Q61327 RefSeq (mRNA) NM_001044 NM_010020 RefSeq (protein) NP_001035 NP_034150 Location (UCSC) Chr 5: 1.39 – 1.45 Mb Chr 13: 73.68 – 73.73 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse The dopamine transporter (DAT, also sodium-dependent dopamine transporter) is a membrane-spanning protein coded ...