Norepinephrine–dopamine reuptake inhibitor

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Norepinephrine–dopamine reuptake inhibitors
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Further information: Norepinephrine reuptake inhibitor and Dopamine reuptake inhibitor
The skeletal structure of norepinephrine
The skeletal structure of dopamine

A norepinephrine–dopamine reuptake inhibitor (NDRI) is a

extracellular concentrations of both norepinephrine and dopamine and, therefore, an increase in adrenergic and dopaminergic neurotransmission.[1]

A closely related type of drug is a norepinephrine–dopamine releasing agent (NDRA).

List of NDRIs

The section only lists compounds that are selective for NET and DAT relative to the serotonin transporter (SERT). For a list of compounds that inhibit reuptake at all three transporters, see serotonin–norepinephrine–dopamine reuptake inhibitor.
The skeletal structure of methylphenidate

Many NDRIs exist, including the following:

substituted amphetamines have a very diverse effects profile, and many of them have significant inhibiting effects on the SERT
.

Amphetamine and many of the other substituted amphetamines are inhibitors of

synaptic cleft. Thus, amphetamine and its derivatives have a pharmacological profile that is much different than classical NDRIs, but analogous to trace amines
. Amphetamine also inhibits monoamine oxidases at very high doses, resulting in less monoamine and trace amine metabolism and consequently higher concentrations of synaptic monoamines.

Research compounds

The CA 2711977 compound
The US 2011263651 compound
Chemical makeup of CA 2711977 
Compound 5-HT-uptake IC50(μM) DA-uptake IC50(μM) NA-uptake IC50(μM)
Piperidine-4-carboxylic (3,4-dichloro-phenyl)-ethyl-amide 0.37 0.021 0.0097
Piperidine-4-carboxylic (3-bromo-4-chloro-phenyl)-ethyl-amide 0.14 0.0078 0.005
Piperidine-4-carboxylic (3-4-dibromo-phenyl)-ethyl-amide 0.12 0.0040 0.0031
Chemical makeup of US 2011263651 
Compound 5-HT-uptake IC50(μM) DA-uptake IC50(μM) NA-uptake IC50(μM)
N-(3,4-Dichloro-phenyl)-N-ethyl-4-piperidin-4-yl-butyramide 0.57 0.012 0.030
N-(3,4-Dichloro-phenyl)-N-ethyl-4-(1-methyl-piperidin-4-yl)-butyramide 0.80 0.0069 0.012

See also

References

  1. ^
    ISBN 978-0-521-75852-9
    . Retrieved 10 May 2012.
  2. PMID 15361919
    .
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