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The pharmacodynamics of cocaine involve the complex relationships of neurotransmitters (inhibiting monoamine uptake in rats with ratios of about: serotonin:dopamine = 2:3, serotonin:norepinephrine = 2:5). [110] [15] The most extensively studied effect of cocaine on the central nervous system is the blockade of the dopamine transporter protein.
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.
Cocaine is a relatively "balanced" inhibitor, although facilitation of dopaminergic neurotransmission is what has been linked to the reinforcing and addictive effects. In addition, cocaine has some serious limitations in terms of its cardiotoxicity [188] due to its local anesthetic activity. Thousands of cocaine users are admitted to emergency ...
Illegal drugs such as cocaine and MDMA also affect dopamine, serotonin, and norepinephrine. Norepinephrine is synthesized by the body from the amino acid tyrosine, [3] and is used in the synthesis of epinephrine, which is a stimulating neurotransmitter of the central nervous system. [4]
Addictive stimuli have variable effects on dopamine receptors, depending on the particular stimulus. [58] According to one study, [59] cocaine, opioids like heroin, amphetamine, alcohol, and nicotine cause decreases in D 2 receptor quantity. A similar association has been linked to food addiction, with a low availability of dopamine receptors ...
DRIs may be divisible into two different types with different effects: (1) typical or conventional DRIs like cocaine, WIN-35428 (β-CFT), and methylphenidate that produce potent psychostimulant, euphoric, and reinforcing effects; and (2) atypical DRIs like vanoxerine (GBR-12909), modafinil, benztropine, and bupropion, which do not produce such effects or have greatly reduced such effects.
Genetic variation in this region also displays influence susceptibility to use drugs of abuse, including cocaine and alcohol consumption. [44] Nicotinic receptors containing α 6 or β 3 subunits expressed in brain regions, especially in the ventral tegmental area and substantia nigra , are important for drug behaviors due to their role in ...
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 ...