- Source: DA-Phen
DA-Phen, also known as dopamine–phenylalanine conjugate, is a synthetic dopamine prodrug which is under preclinical evaluation. Dopamine itself is hydrophilic and is unable to cross the blood–brain barrier, thus showing peripheral selectivity. DA-Phen was developed as a dopamine prodrug that would allow for entry into the central nervous system via passive diffusion and/or active transport.
DA-Phen is a conjugate of dopamine and the amino acid phenylalanine (Phe or Phen). It is slowly cleaved by brain enzymes (t½ = 460 minutes) to yield free dopamine but is also rapidly hydrolyzed in human blood plasma (t½ = 28 minutes). The drug was intended as a prodrug but may also directly interact with the dopamine D1-like and/or D2-like receptors. DA-Phen has shown centrally mediated effects in animals, including increased cognitive flexibility, improved spatial learning and memory, antidepressant- and anxiolytic-like effects, and decreased ethanol intake.
Other analogues, such as DA-Trp and DA-Leu, have also been developed and studied.
See also
Neurotransmitter prodrug
Lisdexamfetamine (dextroamphetamine–lysine conjugate)
DopAmide
Docarpamine
References
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