Dextroamphetamine

Dexedrine Spansule 5, 10 and 15 mg capsules

Pharmacodynamics of amphetamine in a dopamine neuron

via AADC

Amphetamine enters the presynaptic neuron across the neuronal membrane or through DAT. Once inside, it binds to TAAR1 or enters synaptic vesicles through VMAT2. When amphetamine enters the synaptic vesicles through VMAT2, dopamine is released into the cytosol (yellow-orange area). When amphetamine binds to TAAR1, it reduces postsynaptic neuron firing rate via potassium channels and triggers protein kinase A (PKA) and protein kinase C (PKC) signaling, resulting in DAT phosphorylation. PKA-phosphorylation causes DAT to withdraw into the presynaptic neuron (internalize) and cease transport. PKC-phosphorylated DAT may either operate in reverse or, like PKA-phosphorylated DAT, internalize and cease transport. Amphetamine is also known to increase intracellular calcium, an effect which is associated with DAT phosphorylation through a CAMKIIα-dependent pathway, in turn producing dopamine efflux.

Metabolic pathways of amphetamine in humans

4-Hydroxyphenylacetone
Phenylacetone
Benzoic acid
Hippuric acid

Amphetamine
Norephedrine

4-Hydroxyamphetamine
4-Hydroxynorephedrine

Para-Hydroxylation
Para-Hydroxylation
Para-Hydroxylation

Beta-Hydroxylation
Beta-Hydroxylation

OxidativeDeamination

Oxidation
GlycineConjugation

The primary active metabolites of amphetamine are 4-hydroxyamphetamine and norephedrine;[144] however, most of an administered dose is excreted as amphetamine itself and the inactive metabolites.[2] Benzoic acid is metabolized by butyrate-CoA ligase into an intermediate product, benzoyl-CoA,[5] which is then metabolized by glycine N-acyltransferase into hippuric acid.[6]

Dextroamphetamine is a potent central nervous system (CNS) stimulant and amphetamine enantiomer that is prescribed for the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It is also used as an athletic performance and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant. Dextroamphetamine is also widely used by military air forces as a 'go-pill' during fatigue-inducing mission profiles such as night-time bombing missions. Preparations containing dextroamphetamine were also used in World War II as a treatment against fatigue.

单词	Amsustain
释义	Amsustain 英语百科 Dextroamphetamine Dextroamphetamine is a potent central nervous system (CNS) stimulant and amphetamine enantiomer that is prescribed for the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It is also used as an athletic performance and cognitive enhancer, and recreationally as an aphrodisiac and euphoriant. Dextroamphetamine is also widely used by military air forces as a 'go-pill' during fatigue-inducing mission profiles such as night-time bombing missions. Preparations containing dextroamphetamine were also used in World War II as a treatment against fatigue.
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Amsustain

Dextroamphetamine