Dapoxetine(CAS 129938-20-1)

Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI) approved for treating premature ejaculation in men.盐酸达泊西汀是一种短效选择性5-羟色胺再摄取抑制剂（SSRI），用于治疗男性早泄。

Combined Keywords

CAS 129938-20-1: Dapoxetine hydrochloride, CAS 129938-20-1, Premature ejaculation treatment, SSRI, Sexual dysfunction, On-demand therapy.
CAS 129938-20-1: 盐酸达泊西汀，CAS 129938-20-1，早泄治疗，选择性5-羟色胺再摄取抑制剂，性功能障碍，按需治疗。

Chemicals Introduction

​Chemical Properties

• ​Chemical Name: Dapoxetine hydrochloride
• ​CAS Number: 129938-20-1
• ​Molecular Formula: C₂₁H₂₃NO·HCl
• ​Molecular Weight: 341.88 g/mol
• ​Appearance: White to off-white crystalline powder
• ​Solubility: Freely soluble in methanol, slightly soluble in ethanol, practically insoluble in water
• ​Melting Point: 179–183°C

化学名称: 盐酸达泊西汀
CAS号: 129938-20-1
分子式: C₂₁H₂₃NO·HCl
分子量: 341.88 g/mol
外观: 白色至类白色结晶性粉末
溶解性: 易溶于甲醇，微溶于乙醇，几乎不溶于水
熔点: 179–183°C

​Applications

1. ​Premature Ejaculation (PE):
   • First FDA-approved on-demand SSRI for PE, extending ejaculatory latency by 2–4 fold.
   • Acts by inhibiting serotonin reuptake in the central nervous system, enhancing 5-HT neurotransmission.
2. ​早泄（PE）​:
   • 全球首个获批的按需SSRI，延长射精潜伏期2-4倍。
   • 通过抑制中枢神经系统5-羟色胺再摄取，增强5-HT神经传递。
3. ​Mechanism of Action:
   • Selectively binds to serotonin transporters (SERT), increasing synaptic serotonin levels.
   • Rapid absorption (peak plasma concentration in 1.3 hours) and short half-life (~19 hours).
4. ​作用机制:
   • 选择性结合5-羟色胺转运体（SERT），提高突触间隙5-羟色胺浓度。
   • 快速吸收（达峰时间1.3小时），半衰期短（约19小时）。

​Safety & Regulatory Status

• ​Dosage: 30–60 mg orally, 1–3 hours before sexual activity.
• ​Side Effects: Common (≥5%): headache, dizziness, nausea; rare: syncope, priapism.
• ​Contraindications: Concomitant use with MAOIs, other SSRIs, or nitrates.
• ​Regulatory Approval:
  • ​China: Approved as a prescription drug for PE (brand name: 爱廷玖).
  • ​Global: Marketed as Priligy in over 50 countries.
• ​安全性与监管:
  • ​剂量: 性活动前1-3小时口服30–60 mg。
  • ​副作用: 常见（≥5%）头痛、头晕、恶心；罕见晕厥、阴茎异常勃起。
  • ​禁忌: 禁止与MAOIs、其他SSRIs或硝酸酯类药物联用。
  • ​监管批准:
    • ​中国: 批准为处方药（商品名：爱廷玖）。
    • ​全球: 以Priligy品牌在50余国上市。

​Production & Formulation

• ​Synthesis: Multi-step process involving tosylation, naphthol condensation, and mesylation.
• ​Formulation: Tablets (30/60 mg), requiring desiccation storage.
• ​生产工艺:
  • ​合成路线: 包括甲苯磺酰化、萘酚缩合、甲磺酰化等多步反应。
  • ​剂型: 片剂（30/60 mg），需避光干燥保存。

Note: Information synthesized from regulatory documents and peer-reviewed studies.