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• W2145641802 abstract "Recently identified trace amine receptors are potential direct targets for drugs of abuse, including amphetamine and 3,4-methylenedioxymethamphetamine (MDMA). We cloned full-length rhesus monkey trace amine receptor 1 (rhTA₁) that was 96% homologous to human TA₁. The trace amines tyramine and β-phenylethylamine (PEA) and the monoamine transporter substrates (±)-amphetamine and (±)-MDMA stimulated cAMP accumulation in rhTA₁-expressing cell lines, as measured by a cAMP response element-luciferase assay. Cocaine did not stimulate cAMP accumulation in rhTA₁ cells, but it blocked [³H]PEA transport mediated by the dopamine transporter. Cotransfection with the human dopamine transporter enhanced PEA-, amphetamine-, and MDMA-mediated rhTA₁ receptor activation, but it diminished tyramine activation of rhTA₁. Because TA₁ (EGFP-rhTA₁ chimera) was largely intracellular, conceivably the dopamine transporter can facilitate access of specific agonists to intracellular TA₁. rhTA₁ mRNA expression was detected in rhesus monkey substantia nigra, implying that TA₁ may be colocalized with the dopamine transporter in dopamine neurons. In summary, primate TA₁ receptors are direct targets of trace amines, amphetamine, and MDMA. These receptors could also be indirect targets of amphetamine, MDMA, and cocaine through modification of monoamine transporter function. Conceivably, rhTA₁ receptors may be located on pre- or postsynaptic membranes. Interference with the carrier function of monoamine transporters with a consequent rise of extracellular levels of trace amines could activate these receptors. The cloning of a highly homologous TA₁ from rhesus monkey and demonstration that rhTA₁ receptors are activated by drugs of abuse, indicate that nonhuman primates may serve to model physiological and pharmacological TA₁-mediated responses in humans." @default.
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• W2145641802 date "2005-03-11" @default.
• W2145641802 modified "2023-10-10" @default.
• W2145641802 title "Primate Trace Amine Receptor 1 Modulation by the Dopamine Transporter" @default.
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• W2145641802 doi "https://doi.org/10.1124/jpet.105.084459" @default.
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