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Dapoxetine(119356-77-3)

Premature ejaculation is one of the most common male sexual dysfunction, which will have a great impact on patients' self-esteem and marital relationship. Tricyclic antidepressants and clomipramine are the most widely used drugs for the treatment of premature ejaculation, in addition to adrenoceptor antagonists, benzodiazepines, gabapentin, etc. 5-hydroxytryptamine reuptake inhibitor is the most widely used, effective and rapidly developed drug for the treatment of premature ejaculation.

Dapoxetine, whose chemical name is (S) - (+) - N, N-dimethyl-3 - (nyl-1-oxy) - 1-amphetamine, is a new type of 5-hydroxytryptamine reuptake inhibitor. It is a water-soluble white or gray-white powder. Its chemical structure is similar to the antidepressant fluoxetine, and it is the only 5-hydroxytryptamine reuptake inhibitor without halogen atoms. The central neurotransmitters 5-hydroxytryptamine (5-HT) and dopamine and their receptors play an important role in the regulation of ejaculation. By inhibiting the 5-HT transporter, dapoxetine can effectively inhibit the reuptake of 5-HT, increase the concentration of 5-HT in the synaptic space, activate the 5-HT2C and 5-HT1A receptors in the postsynaptic membrane, and produce delayed ejaculation, thus effectively controlling the symptoms of premature ejaculation in men. Compared with other serotonin reuptake inhibitors, dapoxetine has the advantages of good curative effect, short half-life and less side effects.

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