SERT/NET-IN-1 is a SERT and NET inhibitor with blood-brain barrier permeability, exhibiting an IC50 of 11.2 nM for human SERT and 32.0 nM for human NET. It blocks 5-HT reuptake, enhancing serotonergic signaling, and also inhibits norepinephrine reuptake, boosting central noradrenergic transmission while suppressing the ejaculatory reflex. This compound extends ejaculatory latency, reduces ejaculation frequency, and maintains sexual function. SERT/NET-IN-1 shows metabolic stability across species' microsomes, has acceptable oral brain exposure in rats, and demonstrates good safety. It is applicable in research on premature ejaculation.