Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs
BMC Pharmacology March 3, 2006 Dawn D. Han, Howard H. Gu 419 citations
Cocaine blocks all three monoamine transporters (DAT, NET, SERT) at similar concentrations (KI values 0.2–0.7 μM). Methylphenidate inhibits DAT and NET around 0.1 μM but requires about 1000-fold higher concentration to inhibit SERT. Amphetamine and methamphetamine are most potent at NET (KI 0.07–0.1 μM), 5- to 9-fold less potent at DAT (KI ≈ 0.6 μM), and 200- to 500-fold less potent at SERT (KI 20–40 μM). MDMA shows higher potency at SERT than at DAT. Human and mouse transporters respond similarly to each drug, with KI values within 4-fold. These relative potencies indicate which neurotransmitter systems each stimulant disrupts most.